AC50 (functional)
|
= 0.0619 uM
|
PUBCHEM_BIOASSAY: Inhibitors of Epstein-Barr LMP1 inducible NF-kappaB luciferase reporter Measured in Cell-Based System Using Plate Reader - 2122-01_Inhibitor_Dose_CherryPick_Activity. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504586]
|
ChEMBL.
|
No reference
|
Activity (ADMET)
|
|
Toxicity in mouse in po dosed CD1 mouse assessed as leukopenia administered once daily starting shortly post implantation continued for 8 days relative to vehicle-treated control
|
ChEMBL.
|
533880
|
Activity (binding)
|
|
Inhibition of human liver MAOB
|
ChEMBL.
|
18834112
|
Activity (binding)
|
|
Inhibition of human recombinant MAOB at 100 uM by fluorimetric method
|
ChEMBL.
|
18834112
|
Activity (ADMET)
|
|
Toxicity in mouse in po dosed CD1 mouse assessed as change in body weight administered once daily starting shortly post implantation continued for 8 days relative to vehicle-treated control
|
ChEMBL.
|
533880
|
Activity (functional)
|
0
|
Cytostatic activity in human HeLa S3 cells assessed as inhibition of cell growth after 48 hrs by XTT assay
|
ChEMBL.
|
18078757
|
Average survived (functional)
|
= 15.17 day
|
Average days survival of female CDF1 mice bearing lymphocytic leukemia, when 10 E-6 tumor cells were injected intraperitonealy,dosed for 9 days at 20 mg/kg.
|
ChEMBL.
|
3918171
|
CC50 (functional)
|
= 0.00009 M
|
In vitro cell cytotoxicity against 143-B cell lines(Human osteosarcoma cell line)
|
ChEMBL.
|
12620076
|
CC50 (functional)
|
= 0.000095 M
|
In vitro cell cytotoxicity was determined against KBALB cell line
|
ChEMBL.
|
15027876
|
CC50 (functional)
|
= 0.0001 M
|
In vitro cell cytotoxicity was determined against KBALB-STK cell line
|
ChEMBL.
|
15027876
|
CC50 (functional)
|
= 0.0001 M
|
In vitro cell cytotoxicity against 143B-LTK cell lines expressed in HSV-1 TK
|
ChEMBL.
|
12620076
|
Cytotoxicity (functional)
|
= 0.0001 ug ml-1
|
Evaluated for cytotoxicity against murine embryo fibroblasts (MEF)
|
ChEMBL.
|
11123990
|
EC50 (functional)
|
= 0.00751 uM
|
Cytotoxicity against human Ramos cells assessed as reduction in cell viability after 72 hrs by MTS assay
|
ChEMBL.
|
27032331
|
EC50 (functional)
|
= 0.596 um
|
PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Confirmation HTS to Identify Compounds Cytotoxic to BJeLR RAS-Dependent Fibroblast. (Class of assay: confirmatory) [Related pubchem assays: 1674 (Project Summary), 1554 (Primary HTS)]
|
ChEMBL.
|
No reference
|
EC50 (functional)
|
= 0.689 um
|
PUBCHEM_BIOASSAY: Luminescence Microorganism-Based Dose Confirmation HTS to Identify Inhibitors of Streptokinase Promotor Activity. (Class of assay: confirmatory) [Related pubchem assays: 1677 (Project Summary), 1662 (Primary HTS)]
|
ChEMBL.
|
No reference
|
EC50 (functional)
|
= 0.91 uM
|
Antiparasitic activity against Toxoplasma gondii ATCC 50839 infected in HFF cells after 72 hrs by beta-galactosidase reporter gene assay
|
ChEMBL.
|
17698618
|
EC50 (functional)
|
= 0.96 uM
|
Antiparasitic activity against artemisinin-resistant Toxoplasma gondii STL500-10A infected in HFF cells after 72 hrs by beta-galactosidase reporter gene assay
|
ChEMBL.
|
17698618
|
EC50 (functional)
|
= 1.13 uM
|
Antiparasitic activity against artemisinin-resistant Toxoplasma gondii KN200-1 infected in HFF cells after 72 hrs by beta-galactosidase reporter gene assay
|
ChEMBL.
|
17698618
|
EC50 (functional)
|
= 1.19 uM
|
Antiparasitic activity against artemisinin-resistant Toxoplasma gondii KN200-6 infected in HFF cells after 72 hrs by beta-galactosidase reporter gene assay
|
ChEMBL.
|
17698618
|
EC50 (functional)
|
= 9.74 uM
|
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
|
ChEMBL.
|
19917528
|
EC50 (functional)
|
= 10.26 uM
|
Cytotoxicity against human HeLa cells after 72 hrs by MTT assay
|
ChEMBL.
|
19917528
|
EC50 (functional)
|
= 18.84 uM
|
Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay
|
ChEMBL.
|
19917528
|
EC50 (functional)
|
= 57.036 um
|
PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compounds Cytotoxic to BJ-TERT RAS-Independent Fibroblast. (Class of assay: confirmatory) [Related pubchem assays: 1674 (Project Summary), 1554 (Primary HTS)]
|
ChEMBL.
|
No reference
|
EC50 (functional)
|
= 60.8 uM
|
Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTS assay
|
ChEMBL.
|
27032331
|
EC50 (functional)
|
> 150 um
|
PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Response HTS to Identify Compounds Cytotoxic to BJ-TERT-LT-ST RAS-Independent Fibroblast. (Class of assay: confirmatory) [Related pubchem assays: 1674 (Project Summary), 1554 (Primary HTS)]
|
ChEMBL.
|
No reference
|
ED50 (functional)
|
= 84 mg kg-1 day-1
|
Antitumor activity against transplanted tumor sarcoma 180 expressed as effective dose.
|
ChEMBL.
|
2521251
|
GI (functional)
|
= 25.8 uM
|
Anticancer activity against human ACHN cells by SRB assay
|
ChEMBL.
|
20732810
|
GI (functional)
|
= 40.7 uM
|
Anticancer activity against human PC3 cells by SRB assay
|
ChEMBL.
|
20732810
|
GI50 (functional)
|
-6.602
|
PUBCHEM_BIOASSAY: NCI human tumor cell line growth inhibition assay. Data for the P388 Leukemia cell line. (Class of assay: confirmatory)
|
ChEMBL.
|
No reference
|
GI50 (functional)
|
-6.495
|
PUBCHEM_BIOASSAY: NCI human tumor cell line growth inhibition assay. Data for the SN12C Renal cell line. (Class of assay: confirmatory)
|
ChEMBL.
|
No reference
|
GI50 (functional)
|
-6.492
|
PUBCHEM_BIOASSAY: NCI human tumor cell line growth inhibition assay. Data for the NCI-H23 Non-Small Cell Lung cell line. (Class of assay: confirmatory)
|
ChEMBL.
|
No reference
|
GI50 (functional)
|
-6.489
|
PUBCHEM_BIOASSAY: NCI human tumor cell line growth inhibition assay. Data for the SF-539 Central Nervous System cell line. (Class of assay: confirmatory)
|
ChEMBL.
|
No reference
|
GI50 (functional)
|
-6.439
|
PUBCHEM_BIOASSAY: NCI human tumor cell line growth inhibition assay. Data for the ACHN Renal cell line. (Class of assay: confirmatory)
|
ChEMBL.
|
No reference
|
GI50 (functional)
|
-6.314
|
PUBCHEM_BIOASSAY: NCI human tumor cell line growth inhibition assay. Data for the DU-145 Prostate cell line. (Class of assay: confirmatory)
|
ChEMBL.
|
No reference
|
GI50 (functional)
|
-6.249
|
PUBCHEM_BIOASSAY: NCI human tumor cell line growth inhibition assay. Data for the HL-60(TB) Leukemia cell line. (Class of assay: confirmatory)
|
ChEMBL.
|
No reference
|
GI50 (functional)
|
-6.21
|
PUBCHEM_BIOASSAY: NCI human tumor cell line growth inhibition assay. Data for the UO-31 Renal cell line. (Class of assay: confirmatory)
|
ChEMBL.
|
No reference
|
GI50 (functional)
|
-5.992
|
PUBCHEM_BIOASSAY: NCI human tumor cell line growth inhibition assay. Data for the HOP-92 Non-Small Cell Lung cell line. (Class of assay: confirmatory)
|
ChEMBL.
|
No reference
|
GI50 (functional)
|
-5.831
|
PUBCHEM_BIOASSAY: NCI human tumor cell line growth inhibition assay. Data for the MDA-N Breast cell line. (Class of assay: confirmatory)
|
ChEMBL.
|
No reference
|
GI50 (functional)
|
-4.443
|
PUBCHEM_BIOASSAY: NCI human tumor cell line growth inhibition assay. Data for the MALME-3M Melanoma cell line. (Class of assay: confirmatory)
|
ChEMBL.
|
No reference
|
GI50 (functional)
|
-4.176
|
PUBCHEM_BIOASSAY: NCI human tumor cell line growth inhibition assay. Data for the SK-MEL-5 Melanoma cell line. (Class of assay: confirmatory)
|
ChEMBL.
|
No reference
|
GI50 (functional)
|
-4.124
|
PUBCHEM_BIOASSAY: NCI human tumor cell line growth inhibition assay. Data for the HL-60(TB) Leukemia cell line. (Class of assay: confirmatory)
|
ChEMBL.
|
No reference
|
GI50 (functional)
|
-4.101
|
PUBCHEM_BIOASSAY: NCI human tumor cell line growth inhibition assay. Data for the SF-539 Central Nervous System cell line. (Class of assay: confirmatory)
|
ChEMBL.
|
No reference
|
GI50 (functional)
|
-4.076
|
PUBCHEM_BIOASSAY: NCI human tumor cell line growth inhibition assay. Data for the NCI-H23 Non-Small Cell Lung cell line. (Class of assay: confirmatory)
|
ChEMBL.
|
No reference
|
GI50 (functional)
|
-4.034
|
PUBCHEM_BIOASSAY: NCI human tumor cell line growth inhibition assay. Data for the ACHN Renal cell line. (Class of assay: confirmatory)
|
ChEMBL.
|
No reference
|
GI50 (functional)
|
-4.032
|
PUBCHEM_BIOASSAY: NCI human tumor cell line growth inhibition assay. Data for the DU-145 Prostate cell line. (Class of assay: confirmatory)
|
ChEMBL.
|
No reference
|
GI50 (functional)
|
-4.009
|
PUBCHEM_BIOASSAY: NCI human tumor cell line growth inhibition assay. Data for the UO-31 Renal cell line. (Class of assay: confirmatory)
|
ChEMBL.
|
No reference
|
GI50 (functional)
|
-4
|
PUBCHEM_BIOASSAY: NCI human tumor cell line growth inhibition assay. Data for the MDA-N Breast cell line. (Class of assay: confirmatory)
|
ChEMBL.
|
No reference
|
GI50 (functional)
|
-4
|
PUBCHEM_BIOASSAY: NCI human tumor cell line growth inhibition assay. Data for the SN12C Renal cell line. (Class of assay: confirmatory)
|
ChEMBL.
|
No reference
|
GI50 (functional)
|
-4
|
PUBCHEM_BIOASSAY: NCI human tumor cell line growth inhibition assay. Data for the HOP-92 Non-Small Cell Lung cell line. (Class of assay: confirmatory)
|
ChEMBL.
|
No reference
|
GI50 (functional)
|
-4
|
PUBCHEM_BIOASSAY: NCI human tumor cell line growth inhibition assay. Data for the MALME-3M Melanoma cell line. (Class of assay: confirmatory)
|
ChEMBL.
|
No reference
|
GI50 (functional)
|
= 5
|
Anticancer activity against human OVCAR4 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 5
|
Anticancer activity against human SK-MEL-2 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 5
|
Anticancer activity against human SW620 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 5
|
Anticancer activity against human NCI-H226 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 5
|
Anticancer activity against human EKVX cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 5.1
|
Anticancer activity against human MALME-3M cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 5.2
|
Anticancer activity against human OVCAR5 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 5.2
|
Anticancer activity against human KM12 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 5.3
|
Anticancer activity against human TK10 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 5.4
|
Anticancer activity against human MDA-MB-231 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 5.4
|
Anticancer activity against human RXF393 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 5.5
|
Anticancer activity against human MDA-MB-435 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 5.5
|
Anticancer activity against human UACC257 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 5.6
|
Anticancer activity against human OVCAR-3 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 5.6
|
Anticancer activity against human IGROV1 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 5.6
|
Anticancer activity against human HT-29 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 5.6
|
Anticancer activity against human NCI-H522 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 5.7
|
Anticancer activity against human SKOV3 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 5.7
|
Anticancer activity against human SK-MEL-28 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 5.7
|
Anticancer activity against human SNB19 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 5.7
|
Anticancer activity against human HCT15 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 5.8
|
Anticancer activity against human COLO205 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 5.9
|
Anticancer activity against human T47D cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 5.9
|
Anticancer activity against human MDA-N cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 5.9
|
Anticancer activity against human NCI/ADR-RES cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 5.9
|
Anticancer activity against human A498 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 6
|
Anticancer activity against human BT549 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 6.1
|
Anticancer activity against human HOP92 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 6.1
|
Anticancer activity against human K562 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 6.3
|
Anticancer activity against human NCI-H322M cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 6.3
|
Anticancer activity against human NCI-H23 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 6.5
|
Anticancer activity against human PC3 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 6.6
|
Anticancer activity against human DU145 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 6.7
|
Anticancer activity against human SN12C cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 6.7
|
Anticancer activity against human SK-MEL-5 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 6.7
|
Anticancer activity against human SNB75 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 6.7
|
Anticancer activity against human HL-60(TB) cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 6.8
|
Anticancer activity against human M14 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 6.9
|
Anticancer activity against human UO31 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 6.9
|
Anticancer activity against human OVCAR8 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 6.9
|
Anticancer activity against human U251 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 6.9
|
Anticancer activity against human HCT116 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 7
|
Anticancer activity against human 786-0 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 7.4
|
Anticancer activity against human UACC62 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 7.4
|
Anticancer activity against human SF295 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 7.4
|
Anticancer activity against human MOLT4 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 7.5
|
Anticancer activity against human Caki1 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 7.5
|
Anticancer activity against human ACHN cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 7.6
|
Anticancer activity against human LOXIMVI cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 7.6
|
Anticancer activity against human HOP62 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 7.9
|
Anticancer activity against human SF268 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 7.9
|
Anticancer activity against human A549 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 7.9
|
Anticancer activity against human SR cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 8.2
|
Anticancer activity against human CCRF-CEM cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 8.2
|
Anticancer activity against human MCF7 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 8.4
|
Anticancer activity against human SF539 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 8.7
|
Anticancer activity against human NCI-H460 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 9
|
Anticancer activity against human HCC2998 cells after 48 hrs by sulforhodamine B assay
|
ChEMBL.
|
19744858
|
GI50 (functional)
|
= 0.0006 uM
|
In vitro concentration required for 50% inhibition of growth of human leukemia cell line CCRF-CEM with hPAP (0.2 unit/mL)
|
ChEMBL.
|
11597404
|
GI50 (functional)
|
= 0.0006 uM
|
In vitro concentration required for 50% inhibition of growth of human leukemia cell line CCRF-CEM with hPAP (0.2 unit/mL)
|
ChEMBL.
|
11597404
|
GI50 (functional)
|
= 0.002 uM
|
In vitro concentration required for 50% inhibition of growth of human leukemia cell line CCRF-CEM without hPAP (0.2 unit/mL)
|
ChEMBL.
|
11597404
|
GI50 (functional)
|
= 0.002 uM
|
In vitro concentration required for 50% inhibition of growth of human leukemia cell line CCRF-CEM without hPAP (0.2 unit/mL)
|
ChEMBL.
|
11597404
|
GI50 (functional)
|
= 0.16 uM
|
Anticancer activity against human MDA-MB-231 cells by SRB assay
|
ChEMBL.
|
20732810
|
GI50 (functional)
|
= 2.1 uM
|
Anticancer activity against human ACHN cells by SRB assay
|
ChEMBL.
|
20732810
|
GI50 (functional)
|
= 4.97 uM
|
Anticancer activity against human PC3 cells by SRB assay
|
ChEMBL.
|
20732810
|
IC50 (binding)
|
|
DRUGMATRIX: Leukotriene LTC4 Synthase enzyme inhibition (substrate: LTA4)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: CYP450, 2A6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Aldose Reductase enzyme inhibition (substrate: DL-Glyceraldehyde)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Protein Tyrosine Kinase, LCK enzyme inhibition (substrate: Poly(Glu:Tyr))
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Angiotensin AT2 radioligand binding (ligand: [125I] CGP-42112A)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Nitric Oxide Synthase, Inducible (iNOS) enzyme inhibition (substrate: L-Arginine)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Monoamine Oxidase MAO-A enzyme inhibition (substrate: Kynuramine)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Carbonic Anhydrase II enzyme inhibition (substrate: 4-Nitrophenyl acetate (4-NPA))
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Insulin radioligand binding (ligand: [125I] Insulin)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Estrogen ERalpha radioligand binding (ligand: [3H] Estradiol)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Protein Tyrosine Kinase, Fyn enzyme inhibition (substrate: Poly(Glu:Tyr))
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Adenosine A2A radioligand binding (ligand: AB-MECA)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Protein Tyrosine Kinase, EGF Receptor enzyme inhibition (substrate: Poly(Glu:Tyr))
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Cysteinyl leukotriene receptor 1 radioligand binding (ligand: [3H]LTD4)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Protease, Caspase 1 enzyme inhibition (substrate: Ac-YVAD-AMC)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Thromboxane Synthetase enzyme inhibition (substrate: PGH2)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Platelet Activating Factor (PAF) radioligand binding (ligand: [3H] PAF)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Chemokine CCR5 radioligand binding (ligand: [125I] MIP-1alpha)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Adenosine A1 radioligand binding (ligand: DPCPX)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Acetylcholinesterase enzyme inhibition (substrate: acetylthiocholine)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Cannabinoid CB1 radioligand binding (ligand: [3H] SR141716A)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Calcitonin radioligand binding (ligand: [125I] Calcitonin (salmon))
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: HMG-CoA Reductase enzyme inhibition (substrate: [14C]HMG-CoA)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: CYP450, 2C19 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Protein Serine/Threonine Kinase PKCalpha enzyme inhibition (substrate: Histone)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Protein Serine/Threonine Kinase, p38alpha enzyme inhibition (substrate: Myelin Basic Protein)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Estrogen ERbeta radioligand binding (ligand: [3H] Estradiol)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Protein Serine/Threonine Kinase, ERK2 enzyme inhibition (substrate: Myelin Basic Protein)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Tachykinin NK2 radioligand binding (ligand: [3H] SR-48968)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Protein Serine/Threonine Kinase, ERK1 enzyme inhibition (substrate: Myelin Basic Protein)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Cyclooxygenase COX-2 enzyme inhibition (substrate: Arachidonic acid)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Glycine, Strychnine-Sensitive radioligand binding (ligand: [3H] Strychnine)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: CYP450, 2E1 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: CYP450, 1A2 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Neuropeptide Y Y1 radioligand binding (ligand: [125I] Peptide YY)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Peptidase, Matrix Metalloprotease-1 (MMP-1) enzyme inhibition (substrate: Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Chemokine CXCR1 (IL-8A)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Vasopressin V1A radioligand binding (ligand: [125I] PhenylacetylTyr(Me)PheGlnAsnArgProArgTyr)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Cholecystokinin CCKA radioligand binding (ligand: [3H] L-364,718)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Protease, Cathepsin G enzyme inhibition (substrate: Suc-Ala-Ala-Pro-Phe-AMC)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Phosphodiesterase PDE5 enzyme inhibition (substrate: [3H]cGMP + cGMP)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Protease, Matrix Metalloprotease-9 (MMP-9) enzyme inhibition (substrate: Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Chemokine CXCR2 (IL-8B) radioligand binding (ligand: [125I] IL-8)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: CYP450, 3A4 enzyme inhibition (substrate: 7-Benzyloxy-4-(trifluoromethyl)-coumarin)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Vasoactive Intestinal Peptide VIP1 radioligand binding (ligand: [125I] VIP)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Peptidase, Angiotensin Converting Enzyme enzyme inhibition (substrate: FAPGG)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Neuropeptide Y Y2 radioligand binding (ligand: [125I] Peptide YY)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Nitric Oxide Synthase, Neuronal (nNOS) radioligand binding (ligand: [3H]L-Arginine)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Protein Serine/Threonine Phosphatase, PPP3CA (Calcineurin, PP2B) enzyme inhibition (substrate: DiFMUP)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Tachykinin NK1 radioligand binding (ligand: [3H] Substance P)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Peptidase, ELA2 (Neutrophil Elastase 2) enzyme inhibition (substrate: N-MeOSuc-Ala-Ala-Pro-Val-pNA)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Bradykinin B2 radioligand binding (ligand: [3H] Bradykinin)
|
ChEMBL.
|
No reference
|
IC50 (functional)
|
= 0.0000000005 M
|
Compound was evaluated in vitro for its concentration required for 50% inhibition (IC50) of growth of L1210 mouse leukemia cells in culture.
|
ChEMBL.
|
6228661
|
IC50 (functional)
|
= 0.64 nM
|
Growth inhibition in L1210 mouse leukemia cells after 48 h treatment
|
ChEMBL.
|
11728193
|
IC50 (functional)
|
= 0.76 nM
|
Comparative inhibition of L5178Y cell growth in vitro (concentration required for 50% inhibition)
|
ChEMBL.
|
6779007
|
IC50 (functional)
|
= 4.1 nM
|
Growth inhibition in L1210 mouse leukemia cells after 24 h treatment
|
ChEMBL.
|
11728193
|
IC50 (binding)
|
= 7.9 nM
|
Thymidylate synthase inhibition in L1210 mouse leukemia cells after 2 h treatment
|
ChEMBL.
|
11728193
|
IC50 (binding)
|
= 20 nM
|
Thymidylate synthase inhibition in thymidine kinase deficient /TK cells after 2 h treatment
|
ChEMBL.
|
11728193
|
IC50 (functional)
|
= 23 nM
|
Growth inhibition in L1210 mouse leukemia cells after 8 h treatment
|
ChEMBL.
|
11728193
|
IC50 (functional)
|
= 45 nM
|
Growth inhibition in L1210 mouse leukemia cells after 2 h treatment
|
ChEMBL.
|
11728193
|
IC50 (functional)
|
= 58 nM
|
Cytotoxic concentration of the compound was tested in non prostate specific antigen (PSA) producing human TSU cells
|
ChEMBL.
|
12161157
|
IC50 (functional)
|
= 69.2 nM
|
Cytotoxic concentration of the compound was tested in prostate specific antigen (PSA) producing human LNCaP cells
|
ChEMBL.
|
12161157
|
IC50 (binding)
|
= 260 nM
|
Thymidylate synthase inhibition in wild type LM cells after 2 h treatment
|
ChEMBL.
|
11728193
|
IC50 (binding)
|
= 5400 nM
|
Thymidylate synthase inhibition in thymidine kinase deficient LM cells after 2 h treatment
|
ChEMBL.
|
11728193
|
IC50 (functional)
|
= 0.0003 ug ml-1
|
Evaluated for the inhibition of tumor cell growth of murine leukemia malignant tumor cell line (L1210/0)
|
ChEMBL.
|
11123990
|
IC50 (functional)
|
= 0.0003 ug ml-1
|
Evaluated for the inhibition of tumor cell growth of Human T-Lymphocyte cells (CEM/0)
|
ChEMBL.
|
11123990
|
IC50 (functional)
|
= 0.0008 ug ml-1
|
Evaluated for the inhibition of tumor cell growth of murine mammary carcinoma malignant tumor cell line (FM3A/0)
|
ChEMBL.
|
11123990
|
IC50 (functional)
|
= 1 ug ml-1
|
Tested for cytotoxicity against antigen negative T-24 bladder carcinoma cells having only 3-5% antigen expression
|
ChEMBL.
|
8496926
|
IC50 (functional)
|
= 2.6 ug ml-1
|
Evaluated for the inhibition of tumor cell growth of Human T-Lymphocyte cells (Molt4/C8)
|
ChEMBL.
|
11123990
|
IC50 (ADMET)
|
= 0 uM
|
Cytotoxicity against mouse L1210/0 cells after 48 hrs
|
ChEMBL.
|
17341060
|
IC50 (binding)
|
= 0.0004 uM
|
Inhibition of thymidylate synthase in mouse L1210 cells assessed as inhibition of tritium release from [5-3H]deoxyuridine after preincubation for 4 hrs by liquid scintillation counting
|
ChEMBL.
|
21330014
|
IC50 (binding)
|
= 0.0004 uM
|
Inhibition of thymidylate synthase in mouse L1210 cells assessed as inhibition of tritium release from [5-3H]deoxyuridine after preincubation for 24 hrs by liquid scintillation counting
|
ChEMBL.
|
21330014
|
IC50 (binding)
|
= 0.0006 uM
|
Inhibition of thymidylate synthase in mouse L1210 cells assessed as inhibition of tritium release from [5-3H]deoxyuridine after preincubation for 15 mins by liquid scintillation counting
|
ChEMBL.
|
21330014
|
IC50 (binding)
|
= 0.0006 uM
|
Inhibition of thymidylate synthase in mouse L1210 cells assessed as inhibition of tritium release from [5-3H]deoxycytidine after preincubation for 15 mins by liquid scintillation counting
|
ChEMBL.
|
21330014
|
IC50 (functional)
|
= 0.00063 uM
|
Cytostatic activity against mouse L1210 cells in presence of 500 uM uracil
|
ChEMBL.
|
21330014
|
IC50 (binding)
|
= 0.0007 uM
|
Inhibition of thymidylate synthase in mouse L1210 cells assessed as inhibition of tritium release from [5-3H]deoxycytidine after preincubation for 4 hrs by liquid scintillation counting
|
ChEMBL.
|
21330014
|
IC50 (binding)
|
= 0.0007 uM
|
Inhibition of thymidylate synthase in mouse L1210 cells assessed as inhibition of tritium release from [5-3H]deoxycytidine after preincubation for 24 hrs by liquid scintillation counting
|
ChEMBL.
|
21330014
|
IC50 (functional)
|
= 0.0011 uM
|
Cytostatic activity against mouse L1210 cells after 2 days by coulter counting analysis
|
ChEMBL.
|
21330014
|
IC50 (functional)
|
= 0.002 uM
|
In vitro growth inhibition of L5178Y-Parental murine leukemia cells
|
ChEMBL.
|
11101356
|
IC50 (functional)
|
= 0.002 uM
|
In vitro growth inhibition of L5178Y-Parental murine leukemia cells by incorporation of [14C]-Thd.
|
ChEMBL.
|
11101356
|
IC50 (functional)
|
= 0.002 uM
|
In vitro cytotoxicity of compounds were determined on Inhibition of human leukemia cell line(CCRF-CEM) .
|
ChEMBL.
|
8917645
|
IC50 (functional)
|
= 0.0023 uM
|
Cytostatic activity against mouse L1210 cells in presence of 500 uM uridine
|
ChEMBL.
|
21330014
|
IC50 (functional)
|
= 0.0024 uM
|
In vitro growth inhibition of L5178Y-Parental murine leukemia cells by incorporation of [14C]-Leu.
|
ChEMBL.
|
11101356
|
IC50 (functional)
|
= 0.0051 uM
|
Cytostatic activity against mouse L1210 cells in presence of 20 uM 2'-deoxyuridine
|
ChEMBL.
|
21330014
|
IC50 (functional)
|
= 0.009 uM
|
Inhibitory concentration of compound was calculated on L5178Y cells by [14C]-Leu incorporation
|
ChEMBL.
|
8246229
|
IC50 (functional)
|
= 0.009 uM
|
Inhibitory concentration of compound was calculated on L5178Y cells by [14C]-Leu incorporation
|
ChEMBL.
|
8246229
|
IC50 (functional)
|
= 0.0094 uM
|
Cytostatic activity against mouse FM3A cells after 2 days by coulter counting analysis
|
ChEMBL.
|
21330014
|
IC50 (functional)
|
= 0.012 uM
|
Cytostatic activity against mouse L1210 cells ATCC CCL219 assessed as growth reduction after 72 hrs
|
ChEMBL.
|
17997319
|
IC50 (functional)
|
= 0.012 uM
|
Cytostatic activity against human HL60 cells ATCC CCL 240 assessed as growth reduction after 72 hrs
|
ChEMBL.
|
17997319
|
IC50 (functional)
|
= 0.012 uM
|
Cytostatic activity in mouse L1210 cells assessed as inhibition of cell growth after 72 hrs
|
ChEMBL.
|
18078757
|
IC50 (functional)
|
= 0.012 uM
|
Cytostatic activity in human HL60 cells assessed as inhibition of cell growth after 72 hrs
|
ChEMBL.
|
18078757
|
IC50 (functional)
|
= 0.012 uM
|
In vitro cytotoxicity of compounds were determined on murine leukemia cell line (L1210).
|
ChEMBL.
|
8917645
|
IC50 (functional)
|
= 0.012 uM
|
Cytostatic activity against mouse L1210 cells ATCC CCL219 assessed as growth reduction after 72 hrs
|
ChEMBL.
|
17997319
|
IC50 (functional)
|
= 0.012 uM
|
Cytostatic activity against human HL60 cells ATCC CCL 240 assessed as growth reduction after 72 hrs
|
ChEMBL.
|
17997319
|
IC50 (functional)
|
= 0.012 uM
|
Cytostatic activity in mouse L1210 cells assessed as inhibition of cell growth after 72 hrs
|
ChEMBL.
|
18078757
|
IC50 (functional)
|
= 0.012 uM
|
Cytostatic activity in human HL60 cells assessed as inhibition of cell growth after 72 hrs
|
ChEMBL.
|
18078757
|
IC50 (functional)
|
= 0.0124 uM
|
Cytotoxicity against human A549 cells after 72 hrs by microplate reader method
|
ChEMBL.
|
22847019
|
IC50 (functional)
|
= 0.015 uM
|
Inhibitory concentration of compound rwas calculated on L5178Y cells by [3H]-Thd incorporation
|
ChEMBL.
|
8246229
|
IC50 (functional)
|
= 0.015 uM
|
Compound was tested for its inhibitory effect on the growth of NUGC-3 tumor cell line from stomach.
|
ChEMBL.
|
No reference
|
IC50 (functional)
|
= 0.015 uM
|
Inhibitory concentration of compound rwas calculated on L5178Y cells by [3H]-Thd incorporation
|
ChEMBL.
|
8246229
|
IC50 (functional)
|
= 0.017 uM
|
Cytostatic activity against human CCRF-CEM cells ATCC CCL 119 assessed as growth reduction after 72 hrs
|
ChEMBL.
|
17997319
|
IC50 (functional)
|
= 0.017 uM
|
Cytostatic activity in human CCRF-CEM cells assessed as inhibition of cell growth after 72 hrs
|
ChEMBL.
|
18078757
|
IC50 (functional)
|
= 0.017 uM
|
Cytostatic activity against human CCRF-CEM cells ATCC CCL 119 assessed as growth reduction after 72 hrs
|
ChEMBL.
|
17997319
|
IC50 (functional)
|
= 0.017 uM
|
Cytostatic activity in human CCRF-CEM cells assessed as inhibition of cell growth after 72 hrs
|
ChEMBL.
|
18078757
|
IC50 (functional)
|
= 0.02 uM
|
Inhibitory concentration of compound was calculated on L5178Y cells by using clonal assay
|
ChEMBL.
|
8246229
|
IC50 (functional)
|
< 0.02 uM
|
Tested in vitro for the inhibition of cell growth of mouse leukemia L1210 cell (ATCC CCL 219)
|
ChEMBL.
|
11909716
|
IC50 (functional)
|
= 0.02 uM
|
Inhibitory concentration of compound was calculated on L5178Y cells by using clonal assay
|
ChEMBL.
|
8246229
|
IC50 (functional)
|
= 0.021 uM
|
Cytostatic activity against human HeLa cells in presence of 20 uM 2'-deoxyuridine
|
ChEMBL.
|
21330014
|
IC50 (functional)
|
= 0.025 uM
|
Inhibitory concentration of compound was calculated on L5178Y cells by using growth assay
|
ChEMBL.
|
8246229
|
IC50 (functional)
|
= 0.025 uM
|
Inhibitory concentration of compound was calculated on L5178Y cells by using growth assay
|
ChEMBL.
|
8246229
|
IC50 (functional)
|
= 0.026 uM
|
Cytotoxicity against human A2780 cells after 5 days by MTT assay
|
ChEMBL.
|
22738636
|
IC50 (binding)
|
= 0.043 uM
|
Inhibition of cellular thymidylate synthase activity of murine leukemia cell line (L1210) in intact cells.
|
ChEMBL.
|
8917645
|
IC50 (functional)
|
= 0.047 uM
|
Cytotoxicity against human A549 cells assessed as cell viability after 72 hrs by WST-8 assay
|
ChEMBL.
|
22248856
|
IC50 (functional)
|
= 0.049 uM
|
Compound was tested for its inhibitory effect on the growth of HCT-15 tumor cell line from colon.
|
ChEMBL.
|
No reference
|
IC50 (functional)
|
= 0.061 uM
|
Cytostatic activity against human HeLa cells in presence of 500 uM uridine
|
ChEMBL.
|
21330014
|
IC50 (functional)
|
= 0.092 uM
|
Compound was tested for its inhibitory effect on the growth of DLD-1 tumor cell line from colon.
|
ChEMBL.
|
No reference
|
IC50 (functional)
|
= 0.11 uM
|
Cytostatic activity against human HeLa cells in presence of 500 uM uracil
|
ChEMBL.
|
21330014
|
IC50 (functional)
|
= 0.12 uM
|
Compound was tested for its inhibitory effect on the growth of MKN-28 tumor cell line from stomach.
|
ChEMBL.
|
No reference
|
IC50 (functional)
|
= 0.12 uM
|
Compound was tested for its inhibitory effect on the growth of T24 tumor cell line from bladder.
|
ChEMBL.
|
No reference
|
IC50 (functional)
|
= 0.12 uM
|
Compound was tested for its inhibitory effect on the growth of HT-1080 sarcoma tumor cell line.
|
ChEMBL.
|
No reference
|
IC50 (functional)
|
= 0.13 uM
|
In vitro growth inhibition of FdUrd resistant L5178Y-Resistant murine leukemia cells by incorporation of [14C]-Thd.
|
ChEMBL.
|
11101356
|
IC50 (functional)
|
= 0.13 uM
|
Compound was tested for its inhibitory effect on the growth of SW-48 tumor cell line from colon.
|
ChEMBL.
|
No reference
|
IC50 (functional)
|
= 0.14 uM
|
In vitro growth inhibition of FdUrd resistant L5178Y-Resistant murine leukemia cells
|
ChEMBL.
|
11101356
|
IC50 (functional)
|
= 0.15 uM
|
In vitro growth inhibition of FdUrd resistant L5178Y-Resistant murine leukemia cells by incorporation of [14C]-Leu.
|
ChEMBL.
|
11101356
|
IC50 (functional)
|
= 0.18 uM
|
Cytostatic activity against human HT1080 cells by MTT assay
|
ChEMBL.
|
17804231
|
IC50 (functional)
|
= 0.18 uM
|
Cytostatic activity against human HT1080 cells by MTT assay
|
ChEMBL.
|
17804231
|
IC50 (functional)
|
= 0.21 uM
|
Cytotoxicity against human MDA-MB-231 cells overexpressing urokinase plasminogen activator
|
ChEMBL.
|
20363130
|
IC50 (functional)
|
= 0.29 uM
|
Cytostatic activity against human CCRFCEM cells by MTT assay
|
ChEMBL.
|
17804231
|
IC50 (functional)
|
= 0.29 uM
|
Cytostatic activity against human CCRFCEM cells by MTT assay
|
ChEMBL.
|
17804231
|
IC50 (functional)
|
= 0.34 uM
|
Cytostatic activity against Mycoplasma hyorhinis-infected mouse L1210 cells after 48 hrs by cell counting
|
ChEMBL.
|
21892829
|
IC50 (functional)
|
= 0.5 uM
|
Inhibitory concentration of compound rwas calculated on 3T3 cells by [3H]-Thd incorporation
|
ChEMBL.
|
8246229
|
IC50 (functional)
|
= 0.5 uM
|
Tested in vitro for the inhibition of cell growth of human T lymphoblastoid CCRF-CEM cell line (ATCC CCL 119)
|
ChEMBL.
|
11909716
|
IC50 (functional)
|
= 0.5 uM
|
Inhibitory concentration of compound rwas calculated on 3T3 cells by [3H]-Thd incorporation
|
ChEMBL.
|
8246229
|
IC50 (functional)
|
= 0.6 uM
|
Inhibitory concentration of compound was calculated on 3T3 cells by using clonal assay
|
ChEMBL.
|
8246229
|
IC50 (functional)
|
= 0.6 uM
|
Inhibitory concentration of compound was calculated on 3T3 cells by using clonal assay
|
ChEMBL.
|
8246229
|
IC50 (functional)
|
= 0.65 uM
|
Compound was tested for its inhibitory effect on the growth of COLO 320DM tumor cell line from colon.
|
ChEMBL.
|
No reference
|
IC50 (functional)
|
= 0.8 uM
|
Cytostatic activity against human CEM cells expressing human ENT1 transporter after 72 hrs by cell counting in presence of NBMPR
|
ChEMBL.
|
21892829
|
IC50 (functional)
|
= 1 uM
|
Inhibitory concentration was calculated on 3T3 cells by using growth assay
|
ChEMBL.
|
8246229
|
IC50 (functional)
|
= 1 uM
|
Compound was tested for its inhibitory effect on the growth of A-549 tumor cell line from lung.
|
ChEMBL.
|
No reference
|
IC50 (functional)
|
= 1 uM
|
Inhibitory concentration was calculated on 3T3 cells by using growth assay
|
ChEMBL.
|
8246229
|
IC50 (functional)
|
= 2 uM
|
Inhibitory concentration of compound was calculated on L5178Y cells by [14C]-Leu incorporation
|
ChEMBL.
|
8246229
|
IC50 (functional)
|
= 2 uM
|
Inhibitory concentration of compound was calculated on L5178Y cells by [14C]-Leu incorporation
|
ChEMBL.
|
8246229
|
IC50 (functional)
|
= 3.2 uM
|
Inhibitory concentration of compound was calculated on 3T3 cells by [14C]-Leu incorporation
|
ChEMBL.
|
8246229
|
IC50 (functional)
|
= 3.2 uM
|
Inhibitory concentration of compound was calculated on 3T3 cells by [14C]-Leu incorporation
|
ChEMBL.
|
8246229
|
IC50 (functional)
|
= 3.5 uM
|
Compound was tested for its inhibitory effect on the growth of MKN-45 tumor cell line from stomach.
|
ChEMBL.
|
No reference
|
IC50 (functional)
|
= 4 uM
|
Inhibitory concentration of compound rwas calculated on L5178Y cells by [3H]-Thd incorporation
|
ChEMBL.
|
8246229
|
IC50 (functional)
|
= 4 uM
|
Inhibitory concentration of compound rwas calculated on L5178Y cells by [3H]-Thd incorporation
|
ChEMBL.
|
8246229
|
IC50 (functional)
|
= 4.1 uM
|
Tested for cytotoxicity against antigen negative T-24 bladder carcinoma cells having only 3-5% antigen expression
|
ChEMBL.
|
8496926
|
IC50 (functional)
|
= 5 uM
|
Inhibitory concentration of compound was calculated on L5178Y cells by using growth assay
|
ChEMBL.
|
8246229
|
IC50 (functional)
|
= 5 uM
|
Inhibitory concentration of compound was calculated on L5178Y cells by using clonal assay
|
ChEMBL.
|
8246229
|
IC50 (functional)
|
= 5 uM
|
Inhibitory concentration of compound was calculated on L5178Y cells by using growth assay
|
ChEMBL.
|
8246229
|
IC50 (functional)
|
= 5 uM
|
Inhibitory concentration of compound was calculated on L5178Y cells by using clonal assay
|
ChEMBL.
|
8246229
|
IC50 (functional)
|
= 5.31 uM
|
Antiproliferative activity against human HeLa cells assessed as cell viability after 48 hrs by MTT assay
|
ChEMBL.
|
26994842
|
IC50 (binding)
|
= 7.3 uM
|
Inhibition of cellular thymidylate synthase activity of mouse fibroblast (L929 TK-) in intact cells.
|
ChEMBL.
|
8917645
|
IC50 (functional)
|
= 7.7 uM
|
In vitro cytotoxicity of compounds were determined on mouse fibroblast (L929 TK-).
|
ChEMBL.
|
8917645
|
IC50 (functional)
|
= 8.5 uM
|
Cytostatic activity against human HeLa cells in presence of 20 uM thymidine
|
ChEMBL.
|
21330014
|
IC50 (binding)
|
= 11 uM
|
Inhibition of cellular thymidylate synthase activity of mouse fibroblast (L929 TK-) in permeabilised cells.
|
ChEMBL.
|
8917645
|
IC50 (functional)
|
= 12.19 uM
|
Cytotoxicity against human MCF7 cells after 72 hrs by SRB assay
|
ChEMBL.
|
23867603
|
IC50 (functional)
|
= 12.19 uM
|
Cytotoxicity against human MCF7cells after 72 hrs by SRB assay
|
ChEMBL.
|
27073055
|
IC50 (functional)
|
= 19.07 uM
|
Antiproliferative activity against human LoVo cells assessed as growth inhibition after 72 hrs by SRB method
|
ChEMBL.
|
25644674
|
IC50 (ADMET)
|
= 22.46 uM
|
Antiproliferative activity against human MRC5 cells assessed as cell viability after 48 hrs by MTT assay
|
ChEMBL.
|
26994842
|
IC50 (ADMET)
|
= 23.9 uM
|
Antiproliferative activity against mouse BALB/3T3 cells assessed as growth inhibition after 72 hrs by SRB method
|
ChEMBL.
|
25644674
|
IC50 (functional)
|
> 25 uM
|
Tested in vitro for the inhibition of cell growth of murine L929 cells (ATCC CCL 1)
|
ChEMBL.
|
11909716
|
IC50 (functional)
|
> 25 uM
|
Tested in vitro for the inhibition of cell growth of human cervix carcinoma HeLa S3 cell (ATCC CCL 2.2)
|
ChEMBL.
|
11909716
|
IC50 (ADMET)
|
= 30 uM
|
Cytotoxicity against mouse RAW264.7 cells after 72 hrs by resazurin assay
|
ChEMBL.
|
21536448
|
IC50 (functional)
|
> 40 uM
|
Compound was tested for its inhibitory effect on the growth of PANC-1 tumor cell line from pancreas.
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
= 59 uM
|
Inhibition of cellular thymidylate synthase activity of murine leukemia cell line (L1210) in permeabilised cells.
|
ChEMBL.
|
8917645
|
IC50 (functional)
|
= 60 uM
|
Inhibitory concentration of compound was calculated on 3T3 cells by using clonal assay
|
ChEMBL.
|
8246229
|
IC50 (functional)
|
= 60 uM
|
Inhibitory concentration of compound rwas calculated on 3T3 cells by [3H]-Thd incorporation
|
ChEMBL.
|
8246229
|
IC50 (functional)
|
= 60 uM
|
Inhibitory concentration of compound was calculated on 3T3 cells by using clonal assay
|
ChEMBL.
|
8246229
|
IC50 (functional)
|
= 60 uM
|
Inhibitory concentration of compound rwas calculated on 3T3 cells by [3H]-Thd incorporation
|
ChEMBL.
|
8246229
|
IC50 (functional)
|
= 66.3 uM
|
In vitro cytotoxicity of compounds were determined on Inhibition of human leukemia cell line (CEM-TK)
|
ChEMBL.
|
8917645
|
IC50 (functional)
|
= 100 uM
|
Cytostatic activity against mouse L1210 cells in presence of 20 uM thymidine
|
ChEMBL.
|
21330014
|
IC50 (functional)
|
= 115.12 uM
|
Antiproliferative activity against human HT-29 cells assessed as growth inhibition after 72 hrs by SRB method
|
ChEMBL.
|
25644674
|
IC50 (functional)
|
= 150 uM
|
Inhibitory concentration was calculated on 3T3 cells by using growth assay
|
ChEMBL.
|
8246229
|
IC50 (functional)
|
= 150 uM
|
Inhibitory concentration was calculated on 3T3 cells by using growth assay
|
ChEMBL.
|
8246229
|
IC50 (functional)
|
= 250 uM
|
Inhibitory concentration of compound was calculated on 3T3 cells by [14C]-Leu incorporation
|
ChEMBL.
|
8246229
|
IC50 (functional)
|
= 250 uM
|
Inhibitory concentration of compound was calculated on 3T3 cells by [14C]-Leu incorporation
|
ChEMBL.
|
8246229
|
IC50 (ADMET)
|
= 500 uM
|
Cytostatic activity against human WI38 cells MTT assay
|
ChEMBL.
|
17804231
|
IC50 (binding)
|
> 1000 uM
|
Inhibition of human CNT2 expressed in COS7 cells assessed as reduction in sodium-dependent [14C]-inosine uptake in presence of Na+ by liquid scintillation counting method
|
ChEMBL.
|
25815140
|
ID50 (functional)
|
= 0.0000043 M
|
Inhibition of L1210 leukemia cells, after exposure to compound for period of 8-9 hr
|
ChEMBL.
|
3397995
|
ID50 (functional)
|
= 0.001 ug ml-1
|
Inhibitory concentration required to reduce cell growth of Murine Leukemia L1210 cells
|
ChEMBL.
|
6092636
|
ID50 (functional)
|
= 0.001 ug ml-1
|
Dose of the compound inhibiting L1210/0 murine leukemia cell proliferation by 50%
|
ChEMBL.
|
6708047
|
ID50 (functional)
|
= 0.003 ug ml-1
|
Inhibitory concentration required to reduce [14C-2]-dUrd incorporation into cellular DNA by 50% in Murine Leukemia L1210 cells
|
ChEMBL.
|
6092636
|
ID50 (functional)
|
= 0.004 ug ml-1
|
Evaluation for antitumor activity against human lymphoblast Raji cells
|
ChEMBL.
|
3027328
|
ID50 (functional)
|
= 0.02 ug ml-1
|
Dose of the compound inhibiting L1210/0 murine leukemia cell proliferation by 50% in presence of 125 ug/mL of dUrd.
|
ChEMBL.
|
6708047
|
ID50 (functional)
|
= 0.02 ug ml-1
|
Evaluation of cytostatic activity by using antitumor assays against murine leukemia L1210 cells
|
ChEMBL.
|
3027328
|
ID50 (functional)
|
= 1.55 ug ml-1
|
Evaluation of antitumor activity against thymidine kinase deficient Raji cell line
|
ChEMBL.
|
3027328
|
ID50 (functional)
|
= 1.75 ug ml-1
|
Dose of the compound inhibiting L1210/Br-dUrd murine leukemia cell proliferation by 50%
|
ChEMBL.
|
6708047
|
ID50 (functional)
|
= 1.8 ug ml-1
|
Evaluation of antitumor activity against mutant murine leukemia L1210 cells
|
ChEMBL.
|
3027328
|
ID50 (functional)
|
= 34 ug ml-1
|
Dose of the compound inhibiting L1210/0 murine leukemia cell proliferation by 50% in presence of 5 ug/mL of dThd.
|
ChEMBL.
|
6708047
|
ID50 (functional)
|
= 80 ug ml-1
|
Inhibitory concentration required to reduce [3H-methyl]-dThd C incorporation into cellular DNA by 50% in Murine Leukemia L1210 cells
|
ChEMBL.
|
6092636
|
ILS (functional)
|
= 9 %
|
The compound was tested for increase in life span for mice implanted intraperitoneally with P-388/FU Leukemia cell line at 67 mg/kg
|
ChEMBL.
|
7966151
|
ILS (functional)
|
= 9 %
|
Percentage increase in life span of treated mice implanted intraperitoneally with P-388 leukemia resistant cells compared with controls at a dose of 67 mg/kg.
|
ChEMBL.
|
7853342
|
ILS (functional)
|
= 18 %
|
The compound was tested for increase in life span for mice implanted intraperitoneally with P-388/FU Leukemia cell line at 150 mg/kg
|
ChEMBL.
|
7966151
|
ILS (functional)
|
= 18 %
|
The compound was tested for increase in life span for mice implanted intraperitoneally with P-388/FU Leukemia cell line at 100 mg/kg
|
ChEMBL.
|
7966151
|
ILS (functional)
|
= 18 %
|
Percentage increase in life span of treated mice implanted intraperitoneally with P-388 leukemia resistant cells compared with controls at a dose of 150 mg/kg.
|
ChEMBL.
|
7853342
|
ILS (functional)
|
= 18 %
|
Percentage increase in life span of treated mice implanted intraperitoneally with P-388 leukemia resistant cells compared with controls at a dose of 100 mg/kg.
|
ChEMBL.
|
7853342
|
ILS (functional)
|
= 45 %
|
The compound was tested for increase in life span for mice implanted intraperitoneally with P-388/0 Leukemia cell line at 67 mg/kg
|
ChEMBL.
|
7966151
|
ILS (functional)
|
= 45 %
|
Percentage increase in life span of treated mice implanted intraperitoneally with P-388 leukemia sensitive cells compared with controls at a dose of 67 mg/kg.
|
ChEMBL.
|
7853342
|
ILS (functional)
|
= 73 %
|
The compound was tested for increase in life span for mice implanted intraperitoneally with P-388/0 Leukemia cell line at 100 mg/kg
|
ChEMBL.
|
7966151
|
ILS (functional)
|
= 73 %
|
Percentage increase in life span of treated mice implanted intraperitoneally with P-388 leukemia sensitive cells compared with controls at a dose of 100 mg/kg.
|
ChEMBL.
|
7853342
|
ILS (functional)
|
= 82 %
|
The compound was tested for increase in life span for mice implanted intraperitoneally with P-388/0 Leukemia cell line at 150 mg/kg
|
ChEMBL.
|
7966151
|
ILS (functional)
|
= 82 %
|
Percentage increase in life span of treated mice implanted intraperitoneally with P-388 leukemia sensitive cells compared with controls at a dose of 150 mg/kg.
|
ChEMBL.
|
7853342
|
Inhibition (ADMET)
|
|
Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins
|
ChEMBL.
|
22931300
|
Inhibition (ADMET)
|
|
Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins
|
ChEMBL.
|
22931300
|
Inhibition (ADMET)
|
|
Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins
|
ChEMBL.
|
22931300
|
Inhibition (binding)
|
|
Compound was tested for its inhibition against Thymidylate synthase up to concentration of 1 mM; IA means inactive
|
ChEMBL.
|
6779007
|
Inhibition (ADMET)
|
|
Inhibition of human CYP2C19 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 3-butyryl-7-methoxycoumarin as substrate after 30 mins
|
ChEMBL.
|
22931300
|
Inhibition (ADMET)
|
|
Inhibition of human CYP2C9 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-methoxy-4-trifluoromethylcoumarin-3-acetic acid as substrate after 30 mins
|
ChEMBL.
|
22931300
|
Inhibition (ADMET)
|
|
Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins
|
ChEMBL.
|
22931300
|
Inhibition (binding)
|
= 17 %
|
Inhibition of human CNT2 expressed in COS7 cells assessed as reduction in sodium-dependent [14C]-inosine uptake at 100 uM in presence of Na+ by liquid scintillation counting method
|
ChEMBL.
|
25815140
|
Inhibition (binding)
|
< 50 %
|
Inhibition of human CNT2 expressed in COS7 cells assessed as reduction in sodium-dependent [14C]-inosine uptake at 1000 uM in presence of Na+ by liquid scintillation counting method
|
ChEMBL.
|
25815140
|
Inhibition (functional)
|
= 95 %
|
Cytotoxicity against mouse S180 cells at 0.001 uM after 18 to 42 hrs relative to control
|
ChEMBL.
|
214555
|
Inhibition (functional)
|
= 100 %
|
Cytotoxicity against mouse S180 cells at 400 uM after 18 to 42 hrs relative to control
|
ChEMBL.
|
563459
|
Inhibition (ADMET)
|
= 109.162083 %
|
Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
ChEMBL.
|
23571415
|
Inhibition (ADMET)
|
= 116.2599728 %
|
Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
ChEMBL.
|
23571415
|
Ki (binding)
|
|
DRUGMATRIX: Platelet Activating Factor (PAF) radioligand binding (ligand: [3H] PAF)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Cysteinyl leukotriene receptor 1 radioligand binding (ligand: [3H]LTD4)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Protein Serine/Threonine Kinase, p38alpha enzyme inhibition (substrate: Myelin Basic Protein)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Protein Tyrosine Kinase, LCK enzyme inhibition (substrate: Poly(Glu:Tyr))
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Acetylcholinesterase enzyme inhibition (substrate: acetylthiocholine)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: CYP450, 2C19 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Peptidase, Matrix Metalloprotease-1 (MMP-1) enzyme inhibition (substrate: Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Cholecystokinin CCKA radioligand binding (ligand: [3H] L-364,718)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Vasopressin V1A radioligand binding (ligand: [125I] PhenylacetylTyr(Me)PheGlnAsnArgProArgTyr)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Leukotriene LTC4 Synthase enzyme inhibition (substrate: LTA4)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Cannabinoid CB1 radioligand binding (ligand: [3H] SR141716A)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Neuropeptide Y Y2 radioligand binding (ligand: [125I] Peptide YY)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Protease, Cathepsin G enzyme inhibition (substrate: Suc-Ala-Ala-Pro-Phe-AMC)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Carbonic Anhydrase II enzyme inhibition (substrate: 4-Nitrophenyl acetate (4-NPA))
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Estrogen ERalpha radioligand binding (ligand: [3H] Estradiol)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Protein Serine/Threonine Phosphatase, PPP3CA (Calcineurin, PP2B) enzyme inhibition (substrate: DiFMUP)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: CYP450, 2A6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Calcitonin radioligand binding (ligand: [125I] Calcitonin (salmon))
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Tachykinin NK1 radioligand binding (ligand: [3H] Substance P)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Chemokine CXCR2 (IL-8B) radioligand binding (ligand: [125I] IL-8)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Chemokine CCR5 radioligand binding (ligand: [125I] MIP-1alpha)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Protein Serine/Threonine Kinase, ERK2 enzyme inhibition (substrate: Myelin Basic Protein)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Tachykinin NK2 radioligand binding (ligand: [3H] SR-48968)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Adenosine A1 radioligand binding (ligand: DPCPX)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Neuropeptide Y Y1 radioligand binding (ligand: [125I] Peptide YY)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Aldose Reductase enzyme inhibition (substrate: DL-Glyceraldehyde)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Bradykinin B2 radioligand binding (ligand: [3H] Bradykinin)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: CYP450, 1A2 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Chemokine CXCR1 (IL-8A)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Glycine, Strychnine-Sensitive radioligand binding (ligand: [3H] Strychnine)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Protease, Matrix Metalloprotease-9 (MMP-9) enzyme inhibition (substrate: Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Phosphodiesterase PDE5 enzyme inhibition (substrate: [3H]cGMP + cGMP)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Angiotensin AT2 radioligand binding (ligand: [125I] CGP-42112A)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Cyclooxygenase COX-2 enzyme inhibition (substrate: Arachidonic acid)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Protease, Caspase 1 enzyme inhibition (substrate: Ac-YVAD-AMC)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Insulin radioligand binding (ligand: [125I] Insulin)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Protein Serine/Threonine Kinase PKCalpha enzyme inhibition (substrate: Histone)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: HMG-CoA Reductase enzyme inhibition (substrate: [14C]HMG-CoA)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Monoamine Oxidase MAO-A enzyme inhibition (substrate: Kynuramine)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Protein Serine/Threonine Kinase, ERK1 enzyme inhibition (substrate: Myelin Basic Protein)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Adenosine A2A radioligand binding (ligand: AB-MECA)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: CYP450, 2E1 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Vasoactive Intestinal Peptide VIP1 radioligand binding (ligand: [125I] VIP)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Protein Tyrosine Kinase, Fyn enzyme inhibition (substrate: Poly(Glu:Tyr))
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Thromboxane Synthetase enzyme inhibition (substrate: PGH2)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Peptidase, ELA2 (Neutrophil Elastase 2) enzyme inhibition (substrate: N-MeOSuc-Ala-Ala-Pro-Val-pNA)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Peptidase, Angiotensin Converting Enzyme enzyme inhibition (substrate: FAPGG)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: CYP450, 3A4 enzyme inhibition (substrate: 7-Benzyloxy-4-(trifluoromethyl)-coumarin)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Nitric Oxide Synthase, Neuronal (nNOS) radioligand binding (ligand: [3H]L-Arginine)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Estrogen ERbeta radioligand binding (ligand: [3H] Estradiol)
|
ChEMBL.
|
No reference
|
Km (binding)
|
= 0.631 mM
|
Michaelis -Menten constant (Km) against horse liver thymidine phosphorylase
|
ChEMBL.
|
7401121
|
Km (binding)
|
= 96 uM
|
Activity of human thymidine kinase 1 assessed as ATP utilization by luciferase-based assay
|
ChEMBL.
|
17325220
|
Km (binding)
|
= 113 uM
|
Activity of Vaccinia virus WR thymidine kinase assessed as ATP utilization by luciferase-based assay
|
ChEMBL.
|
17325220
|
Km (binding)
|
= 113 uM
|
Activity of Vaccinia virus WR thymidine kinase assessed as ATP utilization by luciferase-based assay
|
ChEMBL.
|
17325220
|
Median life span (functional)
|
= 8.3 day
|
Median life span of the treated L1210 leukemia mice to that of control mice after intraperitoneal administration of 100 mg/kg of compound in a q.d. 1-9 schedule; 8.3/8.2
|
ChEMBL.
|
7288823
|
Median life span (functional)
|
= 10.5 day
|
Median life span of the treated P388 leukemia mice to that of control mice after intraperitoneal administration of 50 mg/kg of compound in a q.d. 1-9 schedule; 10.5/10.9
|
ChEMBL.
|
7288823
|
Median life span (functional)
|
= 11.4 day
|
Median life span of the treated P388 leukemia mice to that of control mice after intraperitoneal administration of 100 mg/kg of compound in a q.d. 1-9 schedule; 11.4/11.3
|
ChEMBL.
|
7288823
|
Median life span (functional)
|
= 12 day
|
Median life span of the treated P388 leukemia mice to that of control mice after intraperitoneal administration of 200 mg/kg of compound in a q.d. 1-5 schedule 12.0/11.9
|
ChEMBL.
|
7288823
|
Median life span (functional)
|
= 13.1 day
|
Median life span of the treated P388 leukemia mice to that of control mice after intraperitoneal administration of 600 mg/kg of compound in a q.d. 1-5 schedule; 13.1/12.0
|
ChEMBL.
|
7288823
|
Median life span (functional)
|
= 14.3 day
|
Median life span of the treated P388 leukemia mice to that of control mice after intraperitoneal administration of 400 mg/kg of compound in a q.d. 1-5 schedule; 14.3/11.9
|
ChEMBL.
|
7288823
|
MIC (functional)
|
= 1 uM
|
Antimicrobial activity against Escherichia coli ATCC 25922 after 20 hrs
|
ChEMBL.
|
17526755
|
MST (functional)
|
= 12 day
|
The compound was tested for mean survival time for 15 mice implanted Intraperitoneally with P-388/FU Leukemia cell line at 67 mg/kg
|
ChEMBL.
|
7966151
|
MST (functional)
|
= 12 day
|
Median survival time of 15 mice implanted intraperitoneally with P-388 leukemia resistant cells at a dose of 67 mg/kg.
|
ChEMBL.
|
7853342
|
MST (functional)
|
= 13 day
|
The compound was tested for mean survival time for 15 mice implanted Intraperitoneally with P-388/FU Leukemia cell line at 150 mg/kg
|
ChEMBL.
|
7966151
|
MST (functional)
|
= 13 day
|
The compound was tested for mean survival time for 15 mice implanted Intraperitoneally with P-388/FU Leukemia cell line at 100 mg/kg
|
ChEMBL.
|
7966151
|
MST (functional)
|
= 13 day
|
Median survival time of 15 mice implanted intraperitoneally with P-388 leukemia resistant cells at a dose of 150 mg/kg.
|
ChEMBL.
|
7853342
|
MST (functional)
|
= 13 day
|
Median survival time of 15 mice implanted intraperitoneally with P-388 leukemia resistant cells at a dose of 100 mg/kg.
|
ChEMBL.
|
7853342
|
MST (functional)
|
= 16 day
|
The compound was tested for mean survival time for 15 mice implanted Intraperitoneally with P-388/0 Leukemia cell line at 67 mg/kg
|
ChEMBL.
|
7966151
|
MST (functional)
|
= 16 day
|
Median survival time of 15 mice implanted intraperitoneally with P-388 leukemia sensitive cells at a dose of 67 mg/kg.
|
ChEMBL.
|
7853342
|
MST (functional)
|
= 19 day
|
The compound was tested for mean survival time for 15 mice implanted Intraperitoneally with P-388/0 Leukemia cell line at 100 mg/kg
|
ChEMBL.
|
7966151
|
MST (functional)
|
= 19 day
|
Median survival time of 15 mice implanted intraperitoneally with P-388 leukemia sensitive cells at a dose of 100 mg/kg.
|
ChEMBL.
|
7853342
|
MST (functional)
|
= 20 day
|
The compound was tested for mean survival time for 15 mice implanted Intraperitoneally with P-388/0 Leukemia cell line at 150 mg/kg
|
ChEMBL.
|
7966151
|
MST (functional)
|
= 20 day
|
Median survival time of 15 mice implanted intraperitoneally with P-388 leukemia sensitive cells at a dose of 150 mg/kg.
|
ChEMBL.
|
7853342
|
Potency (functional)
|
= 0.004 um
|
PUBCHEM_BIOASSAY: qHTS Assay for Modulators of Lamin A Splicing. (Class of assay: confirmatory)
|
ChEMBL.
|
No reference
|
Potency (functional)
|
= 0.0045 um
|
PUBCHEM_BIOASSAY: qHTS Assay for Modulators of Lamin A Splicing. (Class of assay: confirmatory)
|
ChEMBL.
|
No reference
|
Potency (functional)
|
0.0056 uM
|
PUBCHEM_BIOASSAY: S16 Schwann cell PMP22 intronic element beta-lactamase assay. (Class of assay: confirmatory)
|
ChEMBL.
|
No reference
|
Potency (functional)
|
0.0731 uM
|
PubChem BioAssay. A quantitative high throughput screen for small molecules that induce DNA re-replication in SW480 colon adenocarcinoma cells. (Class of assay: confirmatory)
|
ChEMBL.
|
No reference
|
Potency (functional)
|
0.1018 uM
|
PUBCHEM_BIOASSAY: S16 Schwann cell PMP22 intronic element firefly luciferase assay. (Class of assay: confirmatory)
|
ChEMBL.
|
No reference
|
Potency (functional)
|
= 0.1778 um
|
PUBCHEM_BIOASSAY: qHTS Assay for Enhancers of SMN2 Splice Variant Expression. (Class of assay: confirmatory)
|
ChEMBL.
|
No reference
|
Potency (functional)
|
0.2909 uM
|
PUBCHEM_BIOASSAY: qHTS for Inhibitors of binding or entry into cells for Lassa Virus. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID463114, AID540249]
|
ChEMBL.
|
No reference
|
Potency (functional)
|
0.3349 uM
|
PubChem BioAssay: Tox21. qHTS assay for small molecule agonists of the antioxidant response element (ARE) signaling pathway. (Class of assay: confirmatory)
|
ChEMBL.
|
No reference
|
Potency (functional)
|
= 0.3548 um
|
PUBCHEM_BIOASSAY: qHTS Assay for Modulators of Lamin A Splicing. (Class of assay: confirmatory)
|
ChEMBL.
|
No reference
|
Potency (functional)
|
0.4611 uM
|
PubChem BioAssay. qHTS for induction of synthetic lethality in tumor cells producing 2HG: qHTS for the HT-1080-NT fibrosarcoma cell line. (Class of assay: confirmatory)
|
ChEMBL.
|
No reference
|
Potency (functional)
|
0.5805 uM
|
PUBCHEM_BIOASSAY: Nrf2 qHTS screen for inhibitors. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493153, AID493163, AID504648]
|
ChEMBL.
|
No reference
|
Potency (functional)
|
= 1.2589 um
|
PUBCHEM_BIOASSAY: qHTS Assay for Enhancers of SMN2 Splice Variant Expression. (Class of assay: confirmatory)
|
ChEMBL.
|
No reference
|
Potency (functional)
|
4.2527 uM
|
PubChem BioAssay: Tox21. qHTS assay to identify small molecule agonists of the androgen receptor (AR) signaling pathway. (Class of assay: confirmatory)
|
ChEMBL.
|
No reference
|
Potency (functional)
|
7.0795 uM
|
PubChem BioAssay. qHTS Assay for Inhibitors of the Human Apurinic/apyrimidinic Endonuclease 1 (APE1). (Class of assay: confirmatory)
|
ChEMBL.
|
No reference
|
Potency (functional)
|
16.5113 uM
|
PUBCHEM_BIOASSAY: Primary qHTS for delayed death inhibitors of the malarial parasite plastid, 48 hour incubation. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID488752, AID488774, AID504848, AID504850]
|
ChEMBL.
|
No reference
|
Potency (functional)
|
18.526 uM
|
PUBCHEM_BIOASSAY: Primary qHTS for delayed death inhibitors of the malarial parasite plastid, 96 hour incubation. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID488745, AID488752, AID488774, AID504848, AID504850]
|
ChEMBL.
|
No reference
|
Potency (functional)
|
19.0115 uM
|
PUBCHEM_BIOASSAY: Primary qHTS for delayed death inhibitors of the malarial parasite plastid, 96 hour incubation. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID488745, AID488752, AID488774, AID504848, AID504850]
|
ChEMBL.
|
No reference
|
Potency (functional)
|
21.3313 uM
|
PUBCHEM_BIOASSAY: Primary qHTS for delayed death inhibitors of the malarial parasite plastid, 48 hour incubation. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID488752, AID488774, AID504848, AID504850]
|
ChEMBL.
|
No reference
|
Potency (functional)
|
29.8493 uM
|
PubChem BioAssay: Tox21. qHTS assay to identify small molecule agonists of the androgen receptor (AR) signaling pathway using the MDA cell line. (Class of assay: confirmatory)
|
ChEMBL.
|
No reference
|
Potency (functional)
|
= 35.4813 um
|
PUBCHEM_BIOASSAY: qHTS Assay for the Inhibitors of Schistosoma Mansoni Peroxiredoxins. (Class of assay: confirmatory) [Related pubchem assays: 1011 (Confirmation Concentration-Response Assay for Inhibitors of the Schistosoma mansoni Redox Cascade ), 448 (Schistosoma Mansoni Peroxiredoxins (Prx2) and thioredoxin glutathione reductase (TGR) coupled assay)]
|
ChEMBL.
|
No reference
|
Ratio (binding)
|
= 0.96
|
Ratio of Vmax to Km for Vaccinia virus WR thymidine kinase
|
ChEMBL.
|
17325220
|
Ratio (functional)
|
= 3.33
|
Ratio of GI50 without hPAP/ GI50 with hPAP
|
ChEMBL.
|
11597404
|
Ratio (binding)
|
= 5
|
Ratio of Vmax to Km for human thymidine kinase 1
|
ChEMBL.
|
17325220
|
Reduction (functional)
|
= 26 %
|
Percent reduction against sarcoma 180J tumor growth in mice when administered intraperitoneally at dose 12.5 mg/kg
|
ChEMBL.
|
6447210
|
Reduction (functional)
|
= 61 %
|
Percent reduction against sarcoma 180J tumor growth in mice when administered intraperitoneally at dose 25 mg/kg
|
ChEMBL.
|
6447210
|
Reduction (functional)
|
= 85 %
|
Percent reduction against sarcoma 180J tumor growth in mice when administered intraperitoneally at dose 50 mg/kg
|
ChEMBL.
|
6447210
|
Reduction (functional)
|
= 93 %
|
Percent reduction against sarcoma 180J tumor growth in mice when administered intraperitoneally at dose 200 mg/kg
|
ChEMBL.
|
6447210
|
Reduction (functional)
|
= 93 %
|
Percent reduction against sarcoma 180J tumor growth in mice when administered intraperitoneally at dose 100 mg/kg
|
ChEMBL.
|
6447210
|
Survival (functional)
|
= 51 %
|
The compound was evaluated for survival of L1210 cells, when compound was exposed for a period of 8-9 h 1X (10e -6)M conc
|
ChEMBL.
|
3397995
|
Survival (functional)
|
= 62 %
|
The compound was evaluated for survival of L1210 cells, when compound was exposed for a period of 8-9 h 1X (10e -7)M conc
|
ChEMBL.
|
3397995
|
Survival (functional)
|
= 68 %
|
The compound was evaluated for survival of L1210 cells, when compound was exposed for a period of 8-9 h 5*(10e -8)M conc
|
ChEMBL.
|
3397995
|
Survival (functional)
|
= 76 %
|
The compound was evaluated for survival of L1210 cells, when compound was exposed for a period of 8-9 h 1X (10e -8)Mconc
|
ChEMBL.
|
3397995
|
Survival (functional)
|
= 89 %
|
The compound was evaluated for survival of L1210 cells, when compound was exposed for a period of 1 hr 5*(10e -5)M conc
|
ChEMBL.
|
3397995
|
Survival (functional)
|
= 92 %
|
The compound was evaluated for survival of L1210 cells, when compound was exposed for a period of 1 hr 1X (10e -5)M conc
|
ChEMBL.
|
3397995
|
Survival (functional)
|
= 94 %
|
The compound was evaluated for survival of L1210 cells, when compound was exposed for a period of 1 hr 1X (10e -6)M conc
|
ChEMBL.
|
3397995
|
Survival (functional)
|
= 98 %
|
The compound was evaluated for survival of L1210 cells, when compound was exposed for a period of 1 hr 1X (10e -7)Mconc
|
ChEMBL.
|
3397995
|
Survival (functional)
|
= 100 %
|
The compound was evaluated for survival of L1210 cells, when compound was exposed for a period of 8-9 h 1X (10e -9)M conc
|
ChEMBL.
|
3397995
|
T/C (functional)
|
= 96 %
|
Life span ratio of P388 leukemia mice treated to that of control mice at dose 50mg/kg, ip
|
ChEMBL.
|
7288823
|
T/C (functional)
|
= 100 %
|
Life span ratio of P388 leukemia mice treated to that of control mice at dose 100mg/kg, ip
|
ChEMBL.
|
7288823
|
T/C (functional)
|
= 100 %
|
Life span ratio of P388 leukemia mice treated to that of control mice at dose 200mg/kg, ip
|
ChEMBL.
|
7288823
|
T/C (functional)
|
= 101 %
|
Life span ratio of L1210 leukemia mice treated to that of control mice at dose 100mg/kg, ip
|
ChEMBL.
|
7288823
|
T/C (functional)
|
= 109 %
|
Life span ratio of P388 leukemia mice treated to that of control mice at dose 600mg/kg, ip
|
ChEMBL.
|
7288823
|
T/C (functional)
|
= 120 %
|
Life span ratio of P388 leukemia mice treated to that of control mice at dose 400mg/kg, ip
|
ChEMBL.
|
7288823
|
T/C (functional)
|
= 149 %
|
Evaluated for the antitumor activity in the P388 lymphocytic leukemia in female CDF1 mice injected intraperinonealy with 10 E-6 tumor cells dosed for 9 days at 20 mg/kg
|
ChEMBL.
|
3918171
|
Vmax (binding)
|
= 108 microM/min/mg
|
Activity of Vaccinia virus WR thymidine kinase assessed as ATP utilization by luciferase-based assay
|
ChEMBL.
|
17325220
|
Vmax (binding)
|
= 108 microM/min/mg
|
Activity of Vaccinia virus WR thymidine kinase assessed as ATP utilization by luciferase-based assay
|
ChEMBL.
|
17325220
|
Vmax (binding)
|
= 472 microM/min/mg
|
Activity of human thymidine kinase 1 assessed as ATP utilization by luciferase-based assay
|
ChEMBL.
|
17325220
|
Weight change (functional)
|
= -10 %
|
The compound was tested for change in weight for mice implanted intraperitoneally with P-388/FU Leukemia cell line at 150 mg/kg
|
ChEMBL.
|
7966151
|
Weight change (functional)
|
= -10 %
|
The compound was tested for change in weight for mice implanted intraperitoneally with P-388/FU Leukemia cell line at 100 mg/kg
|
ChEMBL.
|
7966151
|
Weight change (functional)
|
= -10 %
|
Average percentage weight change on day 5 in mice implanted intraperitoneally with P-388 leukemia resistant cells at a dose of 150 mg/kg.
|
ChEMBL.
|
7853342
|
Weight change (functional)
|
= -10 %
|
Average percentage weight change on day 5 in mice implanted intraperitoneally with P-388 leukemia resistant cells at a dose of 100 mg/kg.
|
ChEMBL.
|
7853342
|
Weight change (functional)
|
= -6 %
|
The compound was tested for change in weight for mice implanted intraperitoneally with P-388/FU Leukemia cell line at 67 mg/kg
|
ChEMBL.
|
7966151
|
Weight change (functional)
|
= -6 %
|
Average percentage weight change on day 5 in mice implanted intraperitoneally with P-388 leukemia resistant cells at a dose of 67 mg/kg.
|
ChEMBL.
|
7853342
|
Weight change (functional)
|
= -5 %
|
The compound was tested for change in weight for mice implanted intraperitoneally with P-388/0 Leukemia cell line at 150 mg/kg
|
ChEMBL.
|
7966151
|
Weight change (functional)
|
= -5 %
|
Average percentage weight change on day 5 in mice implanted intraperitoneally with P-388 leukemia sensitive cells at a dose of 150 mg/kg.
|
ChEMBL.
|
7853342
|
Weight change (functional)
|
= -4 %
|
The compound was tested for change in weight for mice implanted intraperitoneally with P-388/0 Leukemia cell line at 100 mg/kg
|
ChEMBL.
|
7966151
|
Weight change (functional)
|
= -4 %
|
Average percentage weight change on day 5 in mice implanted intraperitoneally with P-388 leukemia sensitive cells at a dose of 100 mg/kg at a dose of 100 mg/kg.
|
ChEMBL.
|
7853342
|
Weight change (functional)
|
= -2 %
|
The compound was tested for change in weight for mice implanted intraperitoneally with P-388/0 Leukemia cell line at 67 mg/kg
|
ChEMBL.
|
7966151
|
Weight change (functional)
|
= -2 %
|
Average percentage weight change on day 5 in mice implanted intraperitoneally with P-388 leukemia sensitive cells at a dose of 67 mg/kg.
|
ChEMBL.
|
7853342
|
Weight change (functional)
|
= -0.7 g
|
Average weight change in treated P388 leukemia mice to that of control mice on administration of 600 mg/kg of compound in a q. d. 1-5 schedule
|
ChEMBL.
|
7288823
|
Weight change (functional)
|
= -0.5 g
|
Average weight change in treated L1210 leukemia mice to that of control mice on administration of 100 mg/kg of compound in a q. d. 1-9 schedule
|
ChEMBL.
|
7288823
|
Weight change (functional)
|
= -0.3 g
|
Average weight change in treated P388 leukemia mice to that of control mice on administration of 400 mg/kg of compound in a q. d. 1-5 schedule
|
ChEMBL.
|
7288823
|
Weight change (functional)
|
= 0.6 g
|
Average weight change in treated P388 leukemia mice to that of control mice on administration of 100 mg/kg of compound in a q. d. 1-9 schedule
|
ChEMBL.
|
7288823
|
Weight change (functional)
|
= 0.8 g
|
Average weight change in treated P388 leukemia mice to that of control mice on administration of 200 mg/kg of compound in a q. d. 1-5 schedule
|
ChEMBL.
|
7288823
|
Weight change (functional)
|
= 1 g
|
Average weight change in treated P388 leukemia mice to that of control mice on administration of 50 mg/kg of compound in a q. d. 1-9 schedule
|
ChEMBL.
|
7288823
|