%max (binding)
|
= 80 %
|
Partial agonist activity at human PPARgamma-LBD/Gal4 DNA binding domain by transactivation assay relative to darglitazone
|
ChEMBL.
|
23265881
|
Activity (binding)
|
|
Binding affinity to afadin- and alpha-actinin-binding protein in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis
|
ChEMBL.
|
22970990
|
Activity (binding)
|
|
Binding affinity to mouse trace amine-associated receptor 7b by chromatographic analysis
|
ChEMBL.
|
22970990
|
Activity (binding)
|
|
Binding affinity to hemopexin precursor in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis
|
ChEMBL.
|
22970990
|
Activity (functional)
|
|
Partial agonist activity at human PPARgamma-LBD expressed in HEK293T cells assessed as induction of receptor transactivation at 10 uM after 24 hrs by luciferase reporter gene assay
|
ChEMBL.
|
21030263
|
Activity (functional)
|
|
Antihyperglycemic activity in C57BL/Ks db/db mouse assessed as reduction of blood glucose level at 10 mg/kg measured from day 6 to day 14
|
ChEMBL.
|
No reference
|
Activity (binding)
|
|
Binding affinity to trace amine-associated receptor 7b in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis
|
ChEMBL.
|
22970990
|
Activity (binding)
|
|
Binding affinity to focal adhesion kinase 2 in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis
|
ChEMBL.
|
22970990
|
Activity (binding)
|
|
Transactivation of human PPARalpha LBD expressed in african green monkey Cos7 cells co-transfected with fused GAL4-DBD at 10 uM after 14 hrs by Dual-Glo Luciferase reporter gene assay
|
ChEMBL.
|
20307981
|
Activity (binding)
|
|
Transactivation of PPAR-gamma (unknown origin) expressed in HEK293 cells at 10 uM after 24 hrs by luciferase reporter gene assay
|
ChEMBL.
|
24890090
|
Activity (binding)
|
|
Binding affinity to mitochondrial ATP synthase alpha chain in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis
|
ChEMBL.
|
22970990
|
Activity (binding)
|
|
Binding affinity to mitochondrial long-chain specific acyl-CoA dehydrogenase in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis relative to rosiglitazone
|
ChEMBL.
|
22970990
|
Activity (binding)
|
|
Binding affinity to glyceraldehyde 3-phosphate dehydrogenase in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis
|
ChEMBL.
|
22970990
|
Activity (binding)
|
|
Binding affinity to RasGTPase-activating protein SynGAP in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis relative to pioglitazone
|
ChEMBL.
|
22970990
|
Activity (binding)
|
|
Binding affinity to mouse importin-7 by chromatographic analysis
|
ChEMBL.
|
22970990
|
Activity (binding)
|
|
Transactivation of GAL4-fused human PPARdelta ligand binding domain transfected in african green monkey COS7 cells at 10 uM by luciferase reporter gene assay relative to L-165041
|
ChEMBL.
|
23130964
|
Activity (binding)
|
|
Binding affinity to mouse cardiotrophin-like cytokine factor 1 by chromatographic analysis
|
ChEMBL.
|
22970990
|
Activity (binding)
|
|
Binding affinity to Huntingtin-associated protein-interacting protein in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis
|
ChEMBL.
|
22970990
|
Activity (binding)
|
|
Binding affinity to PX domain-containing protein kinase-like protein in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis relative to pioglitazone
|
ChEMBL.
|
22970990
|
Activity (binding)
|
|
Binding affinity to creatine kinase B-type in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis
|
ChEMBL.
|
22970990
|
Activity (binding)
|
|
Agonist activity at human PPAR-gamma expressed in HEK293 cells at 5 uM after 18 hrs by luciferase reporter gene assay in presence of T0070907
|
ChEMBL.
|
24597776
|
Activity (binding)
|
|
Binding affinity to mouse mitochondrial dihydrolipoyl dehydrogenase by chromatographic analysis relative to rosiglitazone
|
ChEMBL.
|
22970990
|
Activity (binding)
|
|
Activation of peroxisome proliferator-activated receptor gamma in reporter gene assay: most active
|
ChEMBL.
|
15745794
|
Activity (binding)
|
|
Binding affinity to mouse protein kinase C and casein kinase substrate in neurons protein 2 by chromatographic analysis
|
ChEMBL.
|
22970990
|
Activity (binding)
|
|
Binding affinity to L-lactate dehydrogenase B chain in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis relative to rosiglitazone
|
ChEMBL.
|
22970990
|
Activity (ADMET)
|
|
Toxicity in db/db mouse assessed as increase of body weight at 41 mg/kg administered with chow diet ad for 14 days
|
ChEMBL.
|
21130649
|
Activity (binding)
|
|
Binding affinity to mouse norrin precursor by chromatographic analysis
|
ChEMBL.
|
22970990
|
Activity (binding)
|
|
Binding affinity to mouse membrane transport protein XK by chromatographic analysis relative to pioglitazone
|
ChEMBL.
|
22970990
|
Activity (binding)
|
|
Binding affinity to neuronal acetylcholine receptor subunit alpha-10 in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis
|
ChEMBL.
|
22970990
|
Activity (functional)
|
|
Antidiabetic activity in db/db mouse assessed as reduction of blood glucose level at 41 mg/kg administered with chow diet ad for 14 days
|
ChEMBL.
|
21130649
|
Activity (binding)
|
|
Binding affinity to mitochondrial ATP synthase beta chain in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis
|
ChEMBL.
|
22970990
|
Activity (binding)
|
|
Binding affinity to mitochondrial aspartate aminotransferase in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis
|
ChEMBL.
|
22970990
|
Activity (functional)
|
|
Partial agonist activity at human PPARgamma-LBD expressed in HEK293T cells assessed as induction of receptor transactivation at 1 uM after 24 hrs by luciferase reporter gene assay
|
ChEMBL.
|
21030263
|
Activity (functional)
|
|
Agonist activity at PPARgamma expressed in HEK293 cells assessed as induction of receptor interaction with steroid receptor coactivator-1 by EYFP based reporter gene assay
|
ChEMBL.
|
16680159
|
Activity (binding)
|
|
Transactivation of GAL4-fused human PPARalpha ligand binding domain transfected in african green monkey COS7 cells at 10 uM by luciferase reporter gene assay relative to GW7647
|
ChEMBL.
|
23130964
|
Activity (binding)
|
|
Binding affinity to mouse mitochondrial 2-oxoglutarate dehydrogenase E1 component by chromatographic analysis
|
ChEMBL.
|
22970990
|
Activity (functional)
|
|
Agonist activity at PPARgamma expressed in HEK293 cells assessed as induction of receptor interaction with retinoid X-receptor alpha by EYFP based reporter gene assay
|
ChEMBL.
|
16680159
|
Activity (functional)
|
|
Antidiabetic activity in diet-induced obesity mouse assessed as reduction in fasting glucose level at 30 mg/kg, po
|
ChEMBL.
|
23414800
|
Activity (binding)
|
|
Binding affinity to Phosphoglycerate kinase 1 in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis
|
ChEMBL.
|
22970990
|
Activity (ADMET)
|
|
Toxicity in db/db mouse assessed as effect on food intake at 41 mg/kg administered with chow diet ad for 14 days
|
ChEMBL.
|
21130649
|
Activity (binding)
|
|
Binding affinity to 26S proteasome non-ATPase regulatory subunit 1 in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis
|
ChEMBL.
|
22970990
|
Activity (binding)
|
|
Binding affinity to sodium-dependent multivitamin transporter in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis
|
ChEMBL.
|
22970990
|
Activity |
|
Toxicity in diet-induced obese mouse assessed as change in body weight at 10 mg/kg, po qd administered daily via gavage for 28 days
|
LITERATURE.
|
28105274
|
Activity (binding)
|
|
Binding affinity to mouse chloride channel protein 6 after 15 mins by chromatographic analysis
|
ChEMBL.
|
22970990
|
Activity (binding)
|
|
Binding affinity to mouse interleukin-12 beta chain precursor by chromatographic analysis
|
ChEMBL.
|
22970990
|
Activity (ADMET)
|
|
Clinically relevant inhibitors of human liver microsomal P450 enzymes, isoform CYP2C8
|
ChEMBL.
|
No reference
|
Activity (binding)
|
= 6.9
|
Activation of PPAR gamma at 5 uM in Cos-7 cell reporter gene assay with 5%FBS
|
ChEMBL.
|
15664804
|
Activity (binding)
|
0
|
Activation of peroxisome proliferator-activated receptor gamma in reporter gene assay: most active
|
ChEMBL.
|
15745794
|
Activity (binding)
|
= 6.9
|
Activation of PPAR gamma at 5 uM in Cos-7 cell reporter gene assay with 5%FBS
|
ChEMBL.
|
15664804
|
Activity (functional)
|
= 10 %
|
Insulin-releasing activity in HIT-T15 cells in the presence of 16.7mM glucose at 10 microM expressed as percent activity of nateglinide
|
ChEMBL.
|
11078199
|
Activity (ADMET)
|
= 17 %
|
Toxicity in db/db mouse assessed as body weight gain at 30 mg/kg/day, po administered daily for 14 days relative to control
|
ChEMBL.
|
21377875
|
Activity (functional)
|
= 50 %
|
Antihyperglycemic activity in db/db mouse assessed as reduction in blood glucose level at 75 mg/kg, po administered once daily for 11 days
|
ChEMBL.
|
19507861
|
Activity (functional)
|
= 53 %
|
Antidiabetic activity in C57BLKS/J-m+/+Leprdb db/db mouse assessed as reduction in plasma glucose levels at 10 mg/kg, po once daily for 11 days relative to control
|
ChEMBL.
|
19530681
|
Activity (functional)
|
= 65 %
|
Antidiabetic activity in C57BLKS/J-m+/+Leprdb db/db mouse assessed as reduction in plasma triglyceride levels at 10 mg/kg, po once daily for 11 days relative to control
|
ChEMBL.
|
19530681
|
Activity (binding)
|
= 71.94 %
|
Agonist activity at PPARgamma (unknown origin) expressed in HEK293 cells assessed as receptor transactivation at 10 uM by PPRE-driven luciferase reporter gene assay
|
ChEMBL.
|
25255433
|
Activity (functional)
|
= 100 %
|
Compound was tested for insulin-sensitizing activity by measuring triglyceride accumlation from insulin regulated differentiation of 3T3-L1 cells at 10 microM expressed as percent activity of pioglitazone
|
ChEMBL.
|
11078199
|
Activity (functional)
|
= 100 %
|
Insulin-sensitizing activity; triglyceride accumlation from insulin regulated differentiation of 3T3-L1 cells at 1 microM expressed as percent activity of pioglitazone
|
ChEMBL.
|
11078199
|
Activity (binding)
|
= 100 %
|
Transactivation of human PPARgamma LBD expressed in african green monkey Cos7 cells co-transfected with fused GAL4-DBD after 14 hrs by Dual-Glo Luciferase reporter gene assay relative to pioglitazone
|
ChEMBL.
|
20307981
|
Activity (binding)
|
= 100 %
|
Activation of Gal4-tagged human PPARgamma expressed in CHO cells by luciferase reporter gene assay relative to pioglitazone
|
ChEMBL.
|
20656494
|
Activity (functional)
|
= 100 %
|
Partial agonist activity at human PPARgamma expressed in CHO cells co-transfected with Gal4-responsive luciferase reporter plasmid after 24 hrs by transactivation assay relative to pioglitazone
|
ChEMBL.
|
21377875
|
Activity (functional)
|
= 100 %
|
Compound was tested for insulin-sensitizing activity by measuring triglyceride accumlation from insulin regulated differentiation of 3T3-L1 cells at 10 microM expressed as percent activity of pioglitazone
|
ChEMBL.
|
11078199
|
Activity (functional)
|
= 100 %
|
Insulin-sensitizing activity; triglyceride accumlation from insulin regulated differentiation of 3T3-L1 cells at 1 microM expressed as percent activity of pioglitazone
|
ChEMBL.
|
11078199
|
Activity (binding)
|
= 100 %
|
Transactivation of GAL4-fused human PPARgamma ligand binding domain expressed in African green monkey COS7 cells at 10 uM after 42 hrs by dual luciferase reporter gene assay
|
LITERATURE.
|
27560282
|
Activity (ADMET)
|
= 15.5 g
|
In vivo body weight gain was observed in db/db mouse 4 weeks after oral administration (once daily) of 100 mg/kg of compound; (n=6)
|
ChEMBL.
|
15664804
|
Activity (ADMET)
|
= 96.6 g
|
In vivo body weight gain was observed in ZDF rats 4 weeks after oral administration (once daily) of 30 mg/kg of compound; (n=6)
|
ChEMBL.
|
15664804
|
Activity (ADMET)
|
= 0.2 mg/dl
|
Toxicity against KKAy mouse assessed as creatinine level at 10 mg/kg/day, po for 14 days (Rvb = 0.2 mg/dl)
|
ChEMBL.
|
23391145
|
Activity (functional)
|
= 230 mg/dl
|
Antidiabetic activity in mouse 3T3L1 cells assessed as decrease in glucose consumption from cell culture medium using 450 mg/dL D-glucose at 30 ug/mL after 24 hrs (Rvb = 310 +/- 4 mg/dl)
|
ChEMBL.
|
22608392
|
Activity (functional)
|
= 5.51 mmol/L
|
Glucose consumption in differentiated mouse 3T3L1 cells in low-glucose medium at 50 ug/ml after 24 hrs by glucose-oxidase method (Rvb =2.41 +/- 0.22 mmol/L)
|
ChEMBL.
|
21515060
|
Activity (functional)
|
= 6.75 mmol/L
|
Glucose consumption in differentiated mouse 3T3L1 cells in low-glucose medium at 100 ug/ml after 24 hrs by glucose-oxidase method (Rvb =2.35 +/- 0.19 mmol/L)
|
ChEMBL.
|
21515060
|
Activity (functional)
|
= 7.36 mmol/L
|
Glucose consumption in differentiated mouse 3T3L1 cells in high-glucose medium at 50 ug/ml after 24 hrs by glucose-oxidase method (Rvb =3.06 +/- 0.29 mmol/L)
|
ChEMBL.
|
21515060
|
Activity (functional)
|
= 8.15 mmol/L
|
Glucose consumption in differentiated mouse 3T3L1 cells in high-glucose medium at 100 ug/ml after 24 hrs by glucose-oxidase method (Rvb =3.12 +/- 0.32 mmol/L)
|
ChEMBL.
|
21515060
|
AUC (ADMET)
|
= 1753075 ng min
|
Area under plasma concentration time curve after oral administration of the compound at a dose 2.2 mg/kg
|
ChEMBL.
|
11831892
|
AUC (ADMET)
|
= 180 uM.hr
|
AUC in C57BLKS/J-m+/+Leprdb db/db mouse at 10 mg/kg, po once daily for 11 days
|
ChEMBL.
|
19530681
|
AUC (ADMET)
|
= 205 uM.hr
|
AUC in db/db mouse at 75 mg/kg, po administered once daily for 11 days
|
ChEMBL.
|
19507861
|
AUC ED50 (ADMET)
|
= 12.09 mg kg-1
|
Area under blood glucose time curve after OGTT on the 9th day of treatment
|
ChEMBL.
|
11831892
|
Average food intake (functional)
|
= 6.34 g mouse-1 day-1
|
Average food intake of the diabetic KK-Ay mice was measured from total intake amount/days/number of mice
|
ChEMBL.
|
14643306
|
Average food intake (functional)
|
= 6.34 g mouse-1 day-1
|
Average food intake of the diabetic KK-Ay mice was measured from total intake amount/days/number of mice
|
ChEMBL.
|
14643306
|
Average sample intake (functional)
|
= 23 mg kg-1 day-1
|
Average sample intake of the diabetic KK-Ay mice was measured as average food intake/average body weight of mice
|
ChEMBL.
|
14643306
|
Average sample intake (functional)
|
= 23 mg kg-1 day-1
|
Average sample intake of the diabetic KK-Ay mice was measured as average food intake/average body weight of mice
|
ChEMBL.
|
14643306
|
Blood glucose (functional)
|
= 191 mg dl-1
|
Blood glucose level of the diabetic KK-Ay mice on day 4 was measured
|
ChEMBL.
|
14643306
|
Blood glucose (functional)
|
= 191 mg dl-1
|
Blood glucose level of the diabetic KK-Ay mice on day 4 was measured
|
ChEMBL.
|
14643306
|
Blood glucose (functional)
|
= 486 mg dl-1
|
Blood glucose level of the diabetic KK-Ay mice on day 0 was measured
|
ChEMBL.
|
14643306
|
Blood glucose (functional)
|
= 486 mg dl-1
|
Blood glucose level of the diabetic KK-Ay mice on day 0 was measured
|
ChEMBL.
|
14643306
|
Body weight (functional)
|
= 52.5 g
|
Body weight of the fasted diabetic KK-Ay mice on day 10 was measured
|
ChEMBL.
|
14643306
|
Body weight (functional)
|
= 52.5 g
|
Body weight of the fasted diabetic KK-Ay mice on day 10 was measured
|
ChEMBL.
|
14643306
|
Body weight (functional)
|
= 53.6 g
|
Body weight of the non-fasted diabetic KK-Ay mice on day 4 was measured
|
ChEMBL.
|
14643306
|
Body weight (functional)
|
= 53.6 g
|
Body weight of the non-fasted diabetic KK-Ay mice on day 4 was measured
|
ChEMBL.
|
14643306
|
Body weight (functional)
|
= 55.1 g
|
Body weight of the non-fasted diabetic KK-Ay mice on day 0 was measured
|
ChEMBL.
|
14643306
|
Body weight (functional)
|
= 55.1 g
|
Body weight of the non-fasted diabetic KK-Ay mice on day 0 was measured
|
ChEMBL.
|
14643306
|
Body weight (functional)
|
= 55.8 g
|
Body weight of the non-fasted diabetic KK-Ay mice on day 7 was measured
|
ChEMBL.
|
14643306
|
Body weight (functional)
|
= 55.8 g
|
Body weight of the non-fasted diabetic KK-Ay mice on day 7 was measured
|
ChEMBL.
|
14643306
|
Change (functional)
|
= 42 %
|
Blood glucose lowering activity in hyperglycemic kk mice.
|
ChEMBL.
|
10714503
|
CL (ADMET)
|
= 1.4 ml min-1 kg-1
|
Clearance after oral administration
|
ChEMBL.
|
11831892
|
Cmax (ADMET)
|
= 4664.99999999998 ng ml-1
|
Maximum plasma concentration after oral administration of the compound at a dose 2.2 mg/kg
|
ChEMBL.
|
11831892
|
Decrease in blood glucose (functional)
|
= 14 %
|
Antihyperglycemic activity was determined in obese (ob/ob) mice by po administration at a dose of 10 mg/kg
|
ChEMBL.
|
10098657
|
Decrease in blood glucose (functional)
|
= 14 %
|
Antihyperglycemic activity was determined in obese (ob/ob) mice by po administration at a dose of 10 mg/kg
|
ChEMBL.
|
10098657
|
Delta Tm (binding)
|
= 2.5 degrees C
|
Inhibition of human recombinant soluble MAO-B assessed as change in melting temperature at 100 uM after 20 mins by SYPRO orange staining-based fluorescence assay
|
ChEMBL.
|
25600407
|
Displacement (binding)
|
= 90 %
|
Displacement of [3H]-BRL 49653 from glutathione S-transferase-Peroxisome proliferator activated receptor gamma ligand binding domain in bacterial extracts
|
ChEMBL.
|
8576907
|
Displacement (binding)
|
= 90 %
|
Displacement of [3H]-BRL 49653 from glutathione S-transferase-Peroxisome proliferator activated receptor gamma ligand binding domain in bacterial extracts
|
ChEMBL.
|
8576907
|
EC50 (binding)
|
|
Transactivation of human GAL4-fused PPARalpha ligand binding domain transfected in HEK293 cells after 18 hrs by dual luciferase reporter gene assay
|
ChEMBL.
|
23102891
|
EC50 (binding)
|
|
Transactivation of human PPARdelta expressed in African green monkey COS7 cells incubated overnight by dual-glo luciferase reporter gene assay
|
ChEMBL.
|
26595749
|
EC50 (binding)
|
|
Transactivation of GAL4-fused human PPARdelta ligand binding domain transfected in african green monkey COS7 cells by luciferase reporter gene assay
|
ChEMBL.
|
23130964
|
EC50 (binding)
|
|
Agonist activity at GAL4-tagged human PPARalpha ligand binding domain expressed in HepG2 cells assessed as transactivation at 5 to 10 uM after 20 hrs by beta-galactosidase reporter gene assay
|
ChEMBL.
|
22341573
|
EC50 (binding)
|
|
Transactivation of GAL4-fused human PPARalpha ligand binding domain transfected in african green monkey COS7 cells by luciferase reporter gene assay
|
ChEMBL.
|
23130964
|
EC50 (functional)
|
|
Partial agonist activity at human PPARalpha expressed in CHO cells co-transfected with Gal4-responsive luciferase reporter plasmid after 24 hrs by transactivation assay
|
ChEMBL.
|
21377875
|
EC50 (binding)
|
|
Transactivation of human PPARalpha expressed in African green monkey COS7 cells incubated overnight by dual-glo luciferase reporter gene assay
|
ChEMBL.
|
26595749
|
EC50 (functional)
|
= -6.23
|
Activation of peroxisome proliferator activated receptor gamma measured by induction of 50% of maximum alkaline phosphatase activity, transfection assay in CV-1 cells
|
ChEMBL.
|
9836620
|
EC50 (functional)
|
= -6.23
|
Transcriptional activation of peroxisome proliferator activated receptor gamma
|
ChEMBL.
|
10612594
|
EC50 (binding)
|
= 3.09
|
Agonist activity at FFAR1 (unknown origin) assessed as increase in ERK1/2 MAP kinase phosphorylation
|
ChEMBL.
|
25441945
|
EC50 (functional)
|
= 0.00000016 M
|
Effective concentration for 50% enhancement of insulin-induced triglyceride accumulation in 3T3-L1 cells
|
ChEMBL.
|
9599241
|
EC50 (functional)
|
= 1.6 M
|
Effective concentration for 50% enhancement of insulin-induced triglyceride accumulation in 3T3-L1 cells
|
ChEMBL.
|
9599241
|
EC50 (functional)
|
= 580 nM
|
Maximal reporter activity against human Peroxisome proliferator activated receptor gamma Gal4 chimeric in transiently transfected CV-1 cells by functional assay.
|
ChEMBL.
|
11720854
|
EC50 (functional)
|
= 580 nM
|
Maximal reporter activity against human Peroxisome proliferator activated receptor gamma Gal4 chimeric in transiently transfected CV-1 cells by functional assay.
|
ChEMBL.
|
11720854
|
EC50 (binding)
|
= 1280 nM
|
Partial agonist activity at human PPARgamma-LBD/Gal4 DNA binding domain by transactivation assay
|
ChEMBL.
|
21557540
|
EC50 (binding)
|
= 1280 nM
|
Partial agonist activity at human PPARgamma-LBD/Gal4 DNA binding domain by transactivation assay
|
ChEMBL.
|
23265881
|
EC50 (functional)
|
uM
|
Agonist activity for Human PPAR alpha receptor in transcriptional activation assay; IA means inactive at 10 uM
|
ChEMBL.
|
10691680
|
EC50 (functional)
|
uM
|
In vitro transcriptional activation of peroxisome proliferator activated delta-receptor (PPAR) expressed in CV-1 cells; Inactive
|
ChEMBL.
|
8576907
|
EC50 (functional)
|
uM
|
Agonist activity for murine PPAR alpha receptor in transcriptional activation assay; IA means inactive at 10 uM
|
ChEMBL.
|
10691680
|
EC50 (functional)
|
uM
|
Agonist activity for murine PPAR delta receptor in transcriptional activation assay; IA means inactive at 10 uM
|
ChEMBL.
|
10691680
|
EC50 (functional)
|
uM
|
In vitro transcriptional activation of peroxisome proliferator activated alpha-receptor (PPAR) expressed in CV-1 cells; Inactive
|
ChEMBL.
|
8576907
|
EC50 (functional)
|
uM
|
Agonist activity for Human PPAR delta receptor in transcriptional activation assay; IA means inactive at 10 uM
|
ChEMBL.
|
10691680
|
EC50 (functional)
|
0 uM
|
Agonist activity for murine PPAR alpha receptor in transcriptional activation assay; IA means inactive at 10 uM
|
ChEMBL.
|
10691680
|
EC50 (functional)
|
0 uM
|
Agonist activity for murine PPAR delta receptor in transcriptional activation assay; IA means inactive at 10 uM
|
ChEMBL.
|
10691680
|
EC50 (functional)
|
0 uM
|
Agonist activity for Human PPAR alpha receptor in transcriptional activation assay; IA means inactive at 10 uM
|
ChEMBL.
|
10691680
|
EC50 (functional)
|
0 uM
|
Agonist activity for Human PPAR delta receptor in transcriptional activation assay; IA means inactive at 10 uM
|
ChEMBL.
|
10691680
|
EC50 (functional)
|
0 uM
|
In vitro transcriptional activation of peroxisome proliferator activated alpha-receptor (PPAR) expressed in CV-1 cells; Inactive
|
ChEMBL.
|
8576907
|
EC50 (functional)
|
0 uM
|
In vitro transcriptional activation of peroxisome proliferator activated delta-receptor (PPAR) expressed in CV-1 cells; Inactive
|
ChEMBL.
|
8576907
|
EC50 (binding)
|
0 uM
|
In vitro transactivation of human Peroxisome proliferator activated receptor delta (hPPARdelta); Not calculated for transactivation <25% at 30 uM
|
ChEMBL.
|
14584939
|
EC50 (functional)
|
= 0.088 uM
|
Agonist activity at PPARgamma assessed as transcriptional activation
|
ChEMBL.
|
20219371
|
EC50 (binding)
|
= 0.14 uM
|
Activation of Gal4-tagged human PPARgamma expressed in CHO cells by luciferase reporter gene assay
|
ChEMBL.
|
20656494
|
EC50 (binding)
|
= 0.2 uM
|
Transactivation of GAL4-fused human PPARgamma ligand binding domain transfected in african green monkey COS7 cells by luciferase reporter gene assay
|
ChEMBL.
|
23130964
|
EC50 (binding)
|
= 0.2 uM
|
Transactivation of human PPARgamma expressed in African green monkey COS7 cells incubated overnight by dual-glo luciferase reporter gene assay
|
ChEMBL.
|
26595749
|
EC50 (binding)
|
= 0.21 uM
|
Agonist activity at human PPARgamma expressed in HEK293 cells incubated for 18 hrs by luciferase reporter gene assay
|
ChEMBL.
|
25333853
|
EC50 (binding)
|
= 0.3 uM
|
Transactivation of human PPARgamma LBD expressed in african green monkey Cos7 cells co-transfected with fused GAL4-DBD after 14 hrs by Dual-Glo Luciferase reporter gene assay
|
ChEMBL.
|
20307981
|
EC50 (binding)
|
= 0.3 uM
|
Modulation of human PPARgamma-LBD expressed in african green monkey COS7 cells co-transfected with Gal4 assessed as activation of transactivation activity by luciferase assay
|
ChEMBL.
|
21873070
|
EC50 (binding)
|
= 0.32 uM
|
Transactivation at Gal4 fused PPARgamma LBD (unknown origin) expressed in African green monkey COS7 cells after 42 hrs by luciferase assay
|
LITERATURE.
|
27569195
|
EC50 (binding)
|
= 0.39 uM
|
Agonist activity at human PPARgamma ligand binding domain expressed in COS-1 cells co-transfected with Gal4 by luciferase reporter gene assay
|
ChEMBL.
|
21130649
|
EC50 (functional)
|
= 0.39 uM
|
Partial agonist activity at human PPARgamma expressed in CHO cells co-transfected with Gal4-responsive luciferase reporter plasmid after 24 hrs by transactivation assay
|
ChEMBL.
|
21377875
|
EC50 (binding)
|
= 0.5 uM
|
Transactivation of GAL4-fused human PPARgamma ligand binding domain expressed in African green monkey COS7 cells after 42 hrs by dual luciferase reporter gene assay
|
LITERATURE.
|
27560282
|
EC50 (functional)
|
= 0.55 uM
|
Agonist activity for murine PPAR gamma receptor in transcriptional activation assay
|
ChEMBL.
|
10691680
|
EC50 (functional)
|
= 0.55 uM
|
Transactivation of PPARgamma in CV1 cells
|
ChEMBL.
|
16821769
|
EC50 (functional)
|
= 0.55 uM
|
Agonist activity for murine PPAR gamma receptor in transcriptional activation assay
|
ChEMBL.
|
10691680
|
EC50 (functional)
|
= 0.55 uM
|
Transactivation of PPARgamma in CV1 cells
|
ChEMBL.
|
16821769
|
EC50 (binding)
|
= 0.57 uM
|
Agonist activity at GAL4-tagged human PPARgamma ligand binding domain expressed in HepG2 cells assessed as transactivation after 20 hrs by beta-galactosidase reporter gene assay
|
ChEMBL.
|
22341573
|
EC50 (functional)
|
= 0.58 uM
|
Agonist activity for Human PPAR gamma receptor in transcriptional activation assay
|
ChEMBL.
|
10691680
|
EC50 (functional)
|
= 0.58 uM
|
Agonist activity for Human PPAR gamma receptor in transcriptional activation assay
|
ChEMBL.
|
10691680
|
EC50 (binding)
|
= 0.6 uM
|
Transactivation activity at Homo sapiens (human) PPARgamma
|
ChEMBL.
|
No reference
|
EC50 (functional)
|
= 0.69 uM
|
In vitro transcriptional activation of Peroxisome proliferator activated receptor gamma (PPAR) expressed in CV-1 cells
|
ChEMBL.
|
8576907
|
EC50 (functional)
|
= 0.69 uM
|
In vitro transcriptional activation of Peroxisome proliferator activated receptor gamma (PPAR) expressed in CV-1 cells
|
ChEMBL.
|
8576907
|
EC50 (binding)
|
= 0.8 uM
|
Transactivation of human GAL4-fused PPARgamma ligand binding domain transfected in HEK293 cells after 18 hrs by dual luciferase reporter gene assay
|
ChEMBL.
|
23102891
|
EC50 (functional)
|
= 0.97 uM
|
In vitro transactivation using receptor transactivation assay against hPPAR gamma
|
ChEMBL.
|
11831892
|
EC50 (binding)
|
= 0.97 uM
|
In vitro transactivation of human Peroxisome proliferator activated receptor gamma
|
ChEMBL.
|
14584939
|
EC50 (functional)
|
= 0.97 uM
|
In vitro transactivation using receptor transactivation assay against hPPAR gamma
|
ChEMBL.
|
11831892
|
EC50 (binding)
|
= 0.97 uM
|
In vitro transactivation of human Peroxisome proliferator activated receptor gamma
|
ChEMBL.
|
14584939
|
EC50 (binding)
|
= 1.6 uM
|
Displacement of Fluoromone from GST-tagged recombinant human PPARgamma ligand binding domain by LanthaScreen TR-FRET assay
|
LITERATURE.
|
27560282
|
EC50 (functional)
|
= 6.68 uM
|
In vitro transactivation using receptor transactivation assay against hPPAR alpha
|
ChEMBL.
|
11831892
|
EC50 (binding)
|
= 6.68 uM
|
In vitro transactivation of human Peroxisome proliferator activated receptor alpha (hPPARalpha)
|
ChEMBL.
|
14584939
|
EC50 (functional)
|
= 6.68 uM
|
In vitro transactivation using receptor transactivation assay against hPPAR alpha
|
ChEMBL.
|
11831892
|
EC50 (binding)
|
= 6.68 uM
|
In vitro transactivation of human Peroxisome proliferator activated receptor alpha (hPPARalpha)
|
ChEMBL.
|
14584939
|
EC50 (functional)
|
= 7.6 uM
|
Peroxisome proliferator activated receptor gamma agonistic activity in HepG2 cells.
|
ChEMBL.
|
10714503
|
ED25 (functional)
|
= 4.6 mg kg-1 day-1
|
Effective dose for 25% blood glucose decrease in genetically diabetic KKA mice.
|
ChEMBL.
|
9599241
|
ED25 (functional)
|
= 4.6 mg kg-1 day-1
|
Effective dose for 25% blood glucose decrease in genetically diabetic KKA mice.
|
ChEMBL.
|
9599241
|
ED50 (functional)
|
= 2.6 mg kg-1
|
In vivo nonfasting blood glucose in db/db mice after oral treament
|
ChEMBL.
|
14584939
|
ED50 (functional)
|
= 2.6 mg kg-1
|
In vivo nonfasting blood glucose in db/db mice after oral treament
|
ChEMBL.
|
14584939
|
ED50 (functional)
|
= 2.62 mg kg-1
|
Nonfasting blood glucose after 7 days treatment in male db/db mice
|
ChEMBL.
|
11831892
|
ED50 (functional)
|
= 2.62 mg kg-1
|
Nonfasting blood glucose after 7 days treatment in male db/db mice
|
ChEMBL.
|
11831892
|
ED50 (functional)
|
= 12 mg kg-1
|
Area under blood glucose time curve after oral glucose test in mice
|
ChEMBL.
|
14584939
|
ED50 (functional)
|
= 12 mg kg-1
|
Area under blood glucose time curve after oral glucose test in mice
|
ChEMBL.
|
14584939
|
ED50 (functional)
|
= 15 mg kg-1
|
In vivo insulin effect in db/db mice after oral treament
|
ChEMBL.
|
14584939
|
ED50 (functional)
|
= 15 mg kg-1
|
In vivo insulin effect in db/db mice after oral treament
|
ChEMBL.
|
14584939
|
ED50 (functional)
|
= 15.05 mg kg-1
|
Nonfasting insulin after 7 days treatment in male db/db mice
|
ChEMBL.
|
11831892
|
ED50 (functional)
|
= 15.05 mg kg-1
|
Nonfasting insulin after 7 days treatment in male db/db mice
|
ChEMBL.
|
11831892
|
ED50 (functional)
|
= 26.74 mg kg-1
|
Nonfasting triglycerides after 7 days treatment in male db/db mice
|
ChEMBL.
|
11831892
|
ED50 (functional)
|
= 26.74 mg kg-1
|
Nonfasting triglycerides after 7 days treatment in male db/db mice
|
ChEMBL.
|
11831892
|
ED50 (functional)
|
= 27 mg kg-1
|
In vivo nonfasting triglyceride in db/db mice after oral treament
|
ChEMBL.
|
14584939
|
ED50 (functional)
|
= 27 mg kg-1
|
In vivo nonfasting triglyceride in db/db mice after oral treament
|
ChEMBL.
|
14584939
|
ED50 (functional)
|
= 19 mg kg-1 day-1
|
Effective dose for 50% blood glucose decrease in genetically diabetic KKA mice.
|
ChEMBL.
|
9599241
|
ED50 (functional)
|
= 19 mg kg-1 day-1
|
Effective dose for 50% blood glucose decrease in genetically diabetic KKA mice.
|
ChEMBL.
|
9599241
|
Efficacy (functional)
|
= 9.17 %
|
Antidyslipidemic activity in C57BL/Ks db/db mouse assessed as reduction of serum cholesterol level at 10 mg/kg measured on day 10 to 15 relative to vehicle-treated sham control
|
ChEMBL.
|
No reference
|
Efficacy (functional)
|
= 11.1 %
|
Antidyslipidemic activity in C57BL/Ks db/db mouse assessed as increase in serum HDL-cholesterol level at 10 mg/kg measured on day 10 to 15 relative to vehicle-treated sham control
|
ChEMBL.
|
No reference
|
Efficacy (functional)
|
= 12.6 %
|
Antidyslipidemic activity in C57BL/Ks db/db mouse assessed as reduction of serum triglyceride level at 10 mg/kg measured on day 10 to 15 relative to vehicle-treated sham control
|
ChEMBL.
|
No reference
|
Efficacy (functional)
|
= 40.8 %
|
Antihyperglycemic activity in C57BL/Ks db/db mouse assessed as reduction of blood glucose AUC (0 to 120 mins) at 10 mg/kg measured on day 10 by OGTT relative to vehicle-treated sham control
|
ChEMBL.
|
No reference
|
Efficacy (functional)
|
= 46.1 %
|
Antidiabetic activity in C57BL/Ks db/db mouse assessed as restoration of altered insulin level in serum at 10 mg/kg relative to vehicle-treated sham control
|
ChEMBL.
|
No reference
|
Efficacy (functional)
|
= 52.9 %
|
Antihyperglycemic activity in C57BL/Ks db/db mouse assessed as reduction of blood glucose AUC (0 to 120 mins) at 10 mg/kg, po measured on day 15 by OGTT relative to vehicle-treated sham control
|
ChEMBL.
|
No reference
|
Efficacy (functional)
|
= 64.7 %
|
Antidiabetic activity in C57BL/Ks db/db mouse assessed as normalization of fasting blood glucose level at 10 mg/kg relative to vehicle-treated sham control
|
ChEMBL.
|
No reference
|
Efficacy (functional)
|
= 70.3 %
|
Antidiabetic activity in C57BL/Ks db/db mouse assessed as improvement of HOMA index at 10 mg/kg relative to vehicle-treated sham control
|
ChEMBL.
|
No reference
|
Emax (binding)
|
|
Transactivation of human PPARdelta expressed in African green monkey COS7 cells at 10 uM incubated overnight by dual-glo luciferase reporter assay
|
ChEMBL.
|
26595749
|
Emax (binding)
|
|
Transactivation of human PPARalpha expressed in African green monkey COS7 cells incubated overnight by dual-glo luciferase reporter assay relative to GW7647
|
ChEMBL.
|
26595749
|
Emax (binding)
|
|
Agonist activity at GAL4-tagged human PPARalpha ligand binding domain expressed in HepG2 cells assessed as transactivation at 5 to 10 uM after 20 hrs by beta-galactosidase reporter gene assay relative to Wy-14643
|
ChEMBL.
|
22341573
|
Emax (binding)
|
= 80 %
|
Partial agonist activity at human PPARgamma-LBD/Gal4 DNA binding domain by transactivation assay relative to darglitazone
|
ChEMBL.
|
21557540
|
Emax (functional)
|
= 118 %
|
Agonist activity at PPARgamma assessed as transcriptional activation relative to GI262570
|
ChEMBL.
|
20219371
|
F (ADMET)
|
= 112 %
|
Oral bioavailability
|
ChEMBL.
|
11831892
|
Fa (ADMET)
|
= 83 %
|
Drug absorption in orally dosed human
|
ChEMBL.
|
25890697
|
FC (functional)
|
= 1.37
|
In vivo inhibition of PTP1B in skeletal muscle of C57BL/Ks db/db mouse assessed as upregulation of p-IRSI protein expression at 10 mg/kg, po by Western blot analysis relative to vehicle-treated sham control
|
ChEMBL.
|
No reference
|
FC (binding)
|
= 1.64
|
Binding affinity to mouse cyclic AMP-dependent transcription factor ATF-2 by chromatographic analysis
|
ChEMBL.
|
22970990
|
FC (binding)
|
= 1.88
|
Binding affinity to mouse mitochondrial dihydrolipoyl dehydrogenase by chromatographic analysis relative to rosiglitazone
|
ChEMBL.
|
22970990
|
FC (binding)
|
= 2.26
|
Binding affinity to L-lactate dehydrogenase B chain in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis relative to rosiglitazone
|
ChEMBL.
|
22970990
|
FC (ADMET)
|
<= 4
|
Full agonist activity at PPARgamma in mouse 3T3L1 preadipocytes assessed as increase in insulin induced adipocyte differentiation by measuring triglyceride accumulation at 1 to 10 uM after 9 days by Oil-Red O staining based assay relative to control
|
LITERATURE.
|
27569195
|
FC (binding)
|
= 5.52
|
Binding affinity to mouse mitochondrial citrate synthase by chromatographic analysis relative to rosiglitazone
|
ChEMBL.
|
22970990
|
FC (binding)
|
= 5.78
|
Binding affinity to mitochondrial long-chain specific acyl-CoA dehydrogenase in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis relative to rosiglitazone
|
ChEMBL.
|
22970990
|
FC (binding)
|
= 6.16
|
Binding affinity to creatine kinase M-type in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis relative to rosiglitazone
|
ChEMBL.
|
22970990
|
FC (binding)
|
= 6.2
|
Modulation of human PPARgamma-LBD expressed in african green monkey COS7 cells co-transfected with Gal4 assessed as activation of transactivation activity at 1 uM by luciferase assay relative to control
|
ChEMBL.
|
21873070
|
FC (binding)
|
= 6.46
|
Binding affinity to triosephosphate isomerase in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis relative to rosiglitazone
|
ChEMBL.
|
22970990
|
FC (binding)
|
= 6.6
|
Agonist activity at human PPARgamma expressed in HEK293 cells assessed as induction of receptor activation at 5 uM incubated for 18 hrs by luciferase reporter gene assay relative to untreated control
|
ChEMBL.
|
25333853
|
FC (binding)
|
= 7.8
|
Agonist activity at human PPARgamma ligand binding domain expressed in COS-1 cells co-transfected with Gal4 at 10 uM by luciferase reporter gene assay relative to control
|
ChEMBL.
|
21130649
|
FC (binding)
|
= 43.1
|
Transactivation of PPARgamma (unknown origin) expressed in HEK293A cells at 150 uM after 16 to 18 hrs by luciferase reporter assay relative to control
|
ChEMBL.
|
26974385
|
fCmax (ADMET)
|
= 0.029 uM
|
Unbound Cmax in human plasma
|
ChEMBL.
|
21965623
|
Fold activation (functional)
|
= 1.77
|
Transcriptional activation of Peroxisome proliferator-activator receptor (PPAR) alpha expressed in HEK 293T cells at 50 uM
|
ChEMBL.
|
11472221
|
Fold activation (functional)
|
= 18.4
|
Transcriptional activation of Peroxisome proliferator-activator receptor (PPAR) gamma expressed in HEK 293T cells at 1 uM
|
ChEMBL.
|
11472221
|
Fold activation (binding)
|
= 1 %
|
In vitro transactivation of human Peroxisome proliferator activated receptor delta (hPPARdelta)
|
ChEMBL.
|
14584939
|
Fold activation (binding)
|
= 1 %
|
In vitro transactivation of human Peroxisome proliferator activated receptor delta (hPPARdelta)
|
ChEMBL.
|
14584939
|
Fold activation (binding)
|
= 4 %
|
In vitro transactivation of rat Peroxisome proliferator activated receptor alpha
|
ChEMBL.
|
14584939
|
Fold activation (binding)
|
= 4 %
|
In vitro transactivation of rat Peroxisome proliferator activated receptor alpha
|
ChEMBL.
|
14584939
|
Fold activation (binding)
|
= 58 %
|
In vitro transactivation of human Peroxisome proliferator activated receptor alpha (hPPARalpha)
|
ChEMBL.
|
14584939
|
Fold activation (binding)
|
= 58 %
|
In vitro transactivation of human Peroxisome proliferator activated receptor alpha (hPPARalpha)
|
ChEMBL.
|
14584939
|
Fold activation (binding)
|
= 91 %
|
In vitro transactivation of human Peroxisome proliferator activated receptor gamma
|
ChEMBL.
|
14584939
|
Fold activation (binding)
|
= 91 %
|
In vitro transactivation of human Peroxisome proliferator activated receptor gamma
|
ChEMBL.
|
14584939
|
Glucose level (ADMET)
|
= 174 mg dl-1
|
In vivo blood glucose level was observed in ZDF rats 4 weeks after oral administration (once daily) of 30 mg/kg of compound; (n=6)
|
ChEMBL.
|
15664804
|
Glucose level (ADMET)
|
= 432 mg dl-1
|
In vivo blood glucose level was observed in db/db mouse 4 weeks after oral administration (once daily) of 100 mg/kg of compound; (n=6)
|
ChEMBL.
|
15664804
|
IC50 (binding)
|
|
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Chemokine CXCR2 (IL-8B) radioligand binding (ligand: [125I] IL-8)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Adenosine A2A radioligand binding (ligand: AB-MECA)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Neuropeptide Y Y2 radioligand binding (ligand: [125I] Peptide YY)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Chemokine CCR5 radioligand binding (ligand: [125I] MIP-1alpha)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Protein Serine/Threonine Phosphatase, PPP3CA (Calcineurin, PP2B) enzyme inhibition (substrate: DiFMUP)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Protein Serine/Threonine Kinase PKCalpha enzyme inhibition (substrate: Histone)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Tachykinin NK1 radioligand binding (ligand: [3H] Substance P)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Protease, Caspase 1 enzyme inhibition (substrate: Ac-YVAD-AMC)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Chemokine CXCR1 (IL-8A)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Tachykinin NK2 radioligand binding (ligand: [3H] SR-48968)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Peptidase, Angiotensin Converting Enzyme enzyme inhibition (substrate: FAPGG)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Protein Tyrosine Kinase, LCK enzyme inhibition (substrate: Poly(Glu:Tyr))
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: CYP450, 2E1 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: CYP450, 3A4 enzyme inhibition (substrate: 7-Benzyloxy-4-(trifluoromethyl)-coumarin)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Protein Tyrosine Kinase, EGF Receptor enzyme inhibition (substrate: Poly(Glu:Tyr))
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Protease, Cathepsin G enzyme inhibition (substrate: Suc-Ala-Ala-Pro-Phe-AMC)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Adenosine A1 radioligand binding (ligand: DPCPX)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine)
|
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: Calcitonin radioligand binding (ligand: [125I] Calcitonin (salmon))
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Protein Serine/Threonine Kinase, p38alpha enzyme inhibition (substrate: Myelin Basic Protein)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Acetylcholinesterase enzyme inhibition (substrate: acetylthiocholine)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
|
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: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Nitric Oxide Synthase, Inducible (iNOS) enzyme inhibition (substrate: L-Arginine)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Cyclooxygenase COX-2 enzyme inhibition (substrate: Arachidonic acid)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: HMG-CoA Reductase enzyme inhibition (substrate: [14C]HMG-CoA)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Thromboxane Synthetase enzyme inhibition (substrate: PGH2)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Insulin radioligand binding (ligand: [125I] Insulin)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Glycine, Strychnine-Sensitive radioligand binding (ligand: [3H] Strychnine)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: CYP450, 1A2 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Protein Tyrosine Kinase, Fyn enzyme inhibition (substrate: Poly(Glu:Tyr))
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
Inhibition of human recombinant sEH using PHOME as substrate preincubated for 30 mins followed by substrate addition measured for 30 mins by fluorescence-based assay
|
ChEMBL.
|
26595749
|
IC50 (binding)
|
|
DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
Inhibition of recombinant soluble epoxide hydrolase using PHOME as substrate after 10 mins by fluorescence assay
|
ChEMBL.
|
23130964
|
IC50 (binding)
|
|
DRUGMATRIX: Cysteinyl leukotriene receptor 1 radioligand binding (ligand: [3H]LTD4)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: CYP450, 2C19 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: CYP450, 2A6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Cannabinoid CB1 radioligand binding (ligand: [3H] SR141716A)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Protein Serine/Threonine Kinase, ERK2 enzyme inhibition (substrate: Myelin Basic Protein)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Leukotriene LTC4 Synthase enzyme inhibition (substrate: LTA4)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Nitric Oxide Synthase, Neuronal (nNOS) radioligand binding (ligand: [3H]L-Arginine)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Protein Serine/Threonine Kinase, ERK1 enzyme inhibition (substrate: Myelin Basic Protein)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Bradykinin B2 radioligand binding (ligand: [3H] Bradykinin)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
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: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Estrogen ERalpha radioligand binding (ligand: [3H] Estradiol)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Estrogen ERbeta radioligand binding (ligand: [3H] Estradiol)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Platelet Activating Factor (PAF) radioligand binding (ligand: [3H] PAF)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Phosphodiesterase PDE5 enzyme inhibition (substrate: [3H]cGMP + cGMP)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Cholecystokinin CCKA radioligand binding (ligand: [3H] L-364,718)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Neuropeptide Y Y1 radioligand binding (ligand: [125I] Peptide YY)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Vasopressin V1A radioligand binding (ligand: [125I] PhenylacetylTyr(Me)PheGlnAsnArgProArgTyr)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Angiotensin AT2 radioligand binding (ligand: [125I] CGP-42112A)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
|
DRUGMATRIX: Vasoactive Intestinal Peptide VIP1 radioligand binding (ligand: [125I] VIP)
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
= 720 nM
|
Agonist activity at PPARgamma (unknown origin)
|
ChEMBL.
|
26048793
|
IC50 (binding)
|
= 855 nM
|
Displacement of fluormone PPAR-green from N-terminal His-tagged human PPARgamma-LBD after 2 hrs by fluorescence polarization assay
|
ChEMBL.
|
21030263
|
IC50 (binding)
|
= 0.114 uM
|
DRUGMATRIX: Carbonic Anhydrase II enzyme inhibition (substrate: 4-Nitrophenyl acetate (4-NPA))
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
= 0.298 uM
|
Inhibition of human recombinant MAO-B after 15 mins
|
ChEMBL.
|
20650633
|
IC50 (binding)
|
= 0.3 uM
|
Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
|
ChEMBL.
|
21965623
|
IC50 (binding)
|
= 0.7 uM
|
Displacement of [3H]rosiglitazone from mouse PPARgamma receptor by scintillation proximation assay
|
ChEMBL.
|
18752947
|
IC50 (binding)
|
= 0.7 uM
|
Displacement of [3H]rosigliatzone from PPARgamma in rat adipocytes
|
ChEMBL.
|
18482837
|
IC50 (binding)
|
= 0.8 uM
|
Displacement of [3H]rosiglitazone from PPAR gamma
|
ChEMBL.
|
17574414
|
IC50 (binding)
|
= 0.8 uM
|
Displacement of [3H]rosiglitazone from PPAR gamma
|
ChEMBL.
|
17574414
|
IC50 (binding)
|
= 1 uM
|
Displacement of [3H]rosiglitazone from rat liver mitochondrial mitoNEET by scintillation counting
|
ChEMBL.
|
20064719
|
IC50 (binding)
|
= 2 uM
|
Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
|
ChEMBL.
|
21965623
|
IC50 (binding)
|
= 7.4 uM
|
Receptor binding affinity of the compound to human Peroxisome proliferator activated receptor gamma against [3H]-ragalitazar radioligand
|
ChEMBL.
|
12672231
|
IC50 (binding)
|
= 7.4 uM
|
Receptor binding affinity of the compound to human Peroxisome proliferator activated receptor gamma against [3H]-ragalitazar radioligand
|
ChEMBL.
|
12672231
|
IC50 (binding)
|
= 8 uM
|
Inhibition of fluormone binding to human PPARgamma LBD after 2 hrs by competitive fluorescence polarization assay
|
ChEMBL.
|
22424975
|
IC50 (binding)
|
= 8.65 uM
|
Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by scintillation proximity assay
|
LITERATURE.
|
27687671
|
IC50 (binding)
|
> 10 uM
|
Receptor binding affinity of the compound to human Peroxisome proliferator activated receptor alpha against [3H]-NNC 0061-4655 radioligand
|
ChEMBL.
|
12672231
|
IC50 (binding)
|
> 10 uM
|
Receptor binding affinity of the compound to human Peroxisome proliferator activated receptor alpha against [3H]-NNC 0061-4655 radioligand
|
ChEMBL.
|
12672231
|
IC50 (binding)
|
> 10 uM
|
SUPPLEMENTARY: Inhibition of Carnitine palmitoyltransferase 1, liver isoform
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
= 13.2 uM
|
DRUGMATRIX: Aldose Reductase enzyme inhibition (substrate: DL-Glyceraldehyde)
|
ChEMBL.
|
No reference
|
IC50 (functional)
|
= 18.6 uM
|
Antiinflammatory activity in human THP1 cells assessed as inhibition of PMA-induced MCP-1 secretion incubated for 2 hrs prior to PMA challenge measured after 72 hrs by ELISA
|
ChEMBL.
|
24531227
|
IC50 (functional)
|
= 18.84 uM
|
Antiinflammatory activity in human THP1 cells assessed as inhibition of PMA-induced MCP-1 secretion preincubated for 1 hr prior PMA-challenge measured after 48 hrs by ELISA
|
ChEMBL.
|
23811092
|
IC50 (binding)
|
= 35.069 uM
|
DRUGMATRIX: Monoamine Oxidase MAO-A enzyme inhibition (substrate: Kynuramine)
|
ChEMBL.
|
No reference
|
IC50 (functional)
|
> 50 uM
|
Antiinflammatory activity in human THP1 cells assessed as inhibition of PMA-induced IL-1beta secretion preincubated for 1 hr prior PMA-challenge measured after 48 hrs by ELISA
|
ChEMBL.
|
23811092
|
IC50 (binding)
|
= 79 uM
|
Inhibition of C-terminal His6-tagged Francisella tularensis SCHU S4 FabI expressed in Escherichia coli BL21 (DE3) using CrCoA as substrate assessed as oxidation of NADH to NAD+ by fluorescence assay
|
ChEMBL.
|
23815100
|
IC50 (binding)
|
> 100 uM
|
SUPPLEMENTARY: Inhibition of Carnitine palmitoyltransferase 1, muscle isoform
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
> 100 uM
|
SUPPLEMENTARY: Inhibition of Carnitine palmitoyltransferase 2
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
> 100 uM
|
SUPPLEMENTARY
|
SUPPLEMENTARY.
|
No reference
|
IC50 (binding)
|
= 220 uM
|
Inhibition of PTP1B
|
ChEMBL.
|
19783142
|
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 (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 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 (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 (binding)
|
|
Inhibition of human MAOA expressed in Pichia pastoris at 100 uM
|
ChEMBL.
|
22282722
|
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 (binding)
|
|
Inhibition of rat MAOA expressed in Pichia pastoris at 100 uM
|
ChEMBL.
|
22282722
|
Inhibition (ADMET)
|
= -9.9 %
|
Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting
|
ChEMBL.
|
22541068
|
Inhibition (ADMET)
|
= 5.6 %
|
Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting
|
ChEMBL.
|
22541068
|
Inhibition (ADMET)
|
< 10 %
|
Time dependent inhibition of CYP1A2 (unknown origin) at 100 uM by LC/MS system
|
ChEMBL.
|
21467212
|
Inhibition (ADMET)
|
< 10 %
|
Time dependent inhibition of CYP2C9 (unknown origin) at 100 uM by LC/MS system
|
ChEMBL.
|
21467212
|
Inhibition (ADMET)
|
< 10 %
|
Time dependent inhibition of CYP2C8 (unknown origin) at 30 uM by LC/MS system
|
ChEMBL.
|
21467212
|
Inhibition (ADMET)
|
< 10 %
|
Time dependent inhibition of CYP2C19 in human liver microsomes at 100 uM by LC/MS system
|
ChEMBL.
|
21467212
|
Inhibition (ADMET)
|
< 10 %
|
Time dependent inhibition of CYP2D6 (unknown origin) at 100 uM by LC/MS system
|
ChEMBL.
|
21467212
|
Inhibition (functional)
|
= 10 %
|
Antidiabetic effect in db/db mouse assessed as increase in HDL cholesterol level at 30 mg/kg/day, po administered daily for 14 days
|
ChEMBL.
|
21377875
|
Inhibition (ADMET)
|
= 21.9 %
|
Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting
|
ChEMBL.
|
22541068
|
Inhibition (functional)
|
> 25 %
|
Hypoglycemic effect in eight week old female db/db mouse assessed as reduction in blood glucose level at 30 mg/kg, intragastric for 1 week
|
ChEMBL.
|
25724827
|
Inhibition (ADMET)
|
= 38 %
|
Time dependent inhibition of CYP2B6 (unknown origin) at 100 uM by LC/MS system
|
ChEMBL.
|
21467212
|
Inhibition (functional)
|
= 46 %
|
Antidiabetic effect in db/db mouse assessed as reduction in plasma glucose level at 30 mg/kg/day, po administered daily for 14 days
|
ChEMBL.
|
21377875
|
Inhibition (ADMET)
|
= 61 %
|
Time dependent inhibition of CYP3A4 (unknown origin) at 100 uM by LC/MS system
|
ChEMBL.
|
21467212
|
Inhibition (functional)
|
= 65 %
|
TP_TRANSPORTER: inhibition of estrone-3-sulfate uptake (Estrone-3-sulfate: 9.2 nM) by Pioglitazone at a concentration of 10uM in OATP8-expressing Xenopus oocytes
|
ChEMBL.
|
14977862
|
Inhibition (binding)
|
= 67.5 %
|
Displacement of Fluoromone from GST-tagged recombinant human PPARgamma ligand binding domain at 10 uM by LanthaScreen TR-FRET assay relative to control
|
LITERATURE.
|
27560282
|
Inhibition (functional)
|
= 69 %
|
Antidiabetic effect in db/db mouse assessed as reduction in plasma triglyceride level at 30 mg/kg/day, po administered daily for 14 days
|
ChEMBL.
|
21377875
|
Inhibition (functional)
|
= 70 %
|
TP_TRANSPORTER: inhibition of estrone-3-sulfate uptake (Estrone-3-sulfate: 9.2 nM) by Pioglitazone at a concentration of 10uM in OATP-C-expressing Xenopus oocytes
|
ChEMBL.
|
14977862
|
Ki (binding)
|
|
DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Protease, Cathepsin G enzyme inhibition (substrate: Suc-Ala-Ala-Pro-Phe-AMC)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Bradykinin B2 radioligand binding (ligand: [3H] Bradykinin)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Chemokine CXCR2 (IL-8B) radioligand binding (ligand: [125I] IL-8)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Protein Tyrosine Kinase, EGF Receptor enzyme inhibition (substrate: Poly(Glu:Tyr))
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Calcitonin radioligand binding (ligand: [125I] Calcitonin (salmon))
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Cholecystokinin CCKA radioligand binding (ligand: [3H] L-364,718)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Acetylcholinesterase enzyme inhibition (substrate: acetylthiocholine)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Platelet Activating Factor (PAF) radioligand binding (ligand: [3H] PAF)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Thromboxane Synthetase enzyme inhibition (substrate: PGH2)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Vasoactive Intestinal Peptide VIP1 radioligand binding (ligand: [125I] VIP)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
|
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: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Tachykinin NK1 radioligand binding (ligand: [3H] Substance P)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: CYP450, 2E1 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Peptidase, Angiotensin Converting Enzyme enzyme inhibition (substrate: FAPGG)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: CYP450, 2C19 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Cysteinyl leukotriene receptor 1 radioligand binding (ligand: [3H]LTD4)
|
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: Insulin radioligand binding (ligand: [125I] Insulin)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Vasopressin V1A radioligand binding (ligand: [125I] PhenylacetylTyr(Me)PheGlnAsnArgProArgTyr)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Estrogen ERalpha radioligand binding (ligand: [3H] Estradiol)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Adenosine A2A radioligand binding (ligand: AB-MECA)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Monoamine Oxidase MAO-A enzyme inhibition (substrate: Kynuramine)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Protease, Caspase 1 enzyme inhibition (substrate: Ac-YVAD-AMC)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Cannabinoid CB1 radioligand binding (ligand: [3H] SR141716A)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Protein Serine/Threonine Kinase, ERK1 enzyme inhibition (substrate: Myelin Basic Protein)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Neuropeptide Y Y1 radioligand binding (ligand: [125I] Peptide YY)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: CYP450, 1A2 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Protein Tyrosine Kinase, ERBB2 (HER2) enzyme inhibition (substrate: Poly(Glu:Tyr))
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Aldose Reductase enzyme inhibition (substrate: DL-Glyceraldehyde)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Chemokine CCR5 radioligand binding (ligand: [125I] MIP-1alpha)
|
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: Neuropeptide Y Y2 radioligand binding (ligand: [125I] Peptide YY)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: HMG-CoA Reductase enzyme inhibition (substrate: [14C]HMG-CoA)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Estrogen ERbeta radioligand binding (ligand: [3H] Estradiol)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Protein Tyrosine Kinase, LCK enzyme inhibition (substrate: Poly(Glu:Tyr))
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Glycine, Strychnine-Sensitive radioligand binding (ligand: [3H] Strychnine)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Protein Serine/Threonine Kinase, p38alpha enzyme inhibition (substrate: Myelin Basic Protein)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Protein Serine/Threonine Kinase, ERK2 enzyme inhibition (substrate: Myelin Basic Protein)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Chemokine CXCR1 (IL-8A)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Carbonic Anhydrase II enzyme inhibition (substrate: 4-Nitrophenyl acetate (4-NPA))
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Nitric Oxide Synthase, Inducible (iNOS) enzyme inhibition (substrate: L-Arginine)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Phosphodiesterase PDE5 enzyme inhibition (substrate: [3H]cGMP + cGMP)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Leukotriene LTC4 Synthase enzyme inhibition (substrate: LTA4)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Adenosine A1 radioligand binding (ligand: DPCPX)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Cyclooxygenase COX-2 enzyme inhibition (substrate: Arachidonic acid)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Protein Serine/Threonine Phosphatase, PPP3CA (Calcineurin, PP2B) enzyme inhibition (substrate: DiFMUP)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Protein Serine/Threonine Kinase PKCalpha enzyme inhibition (substrate: Histone)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Tachykinin NK2 radioligand binding (ligand: [3H] SR-48968)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: CYP450, 3A4 enzyme inhibition (substrate: 7-Benzyloxy-4-(trifluoromethyl)-coumarin)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
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: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Protein Tyrosine Kinase, Fyn enzyme inhibition (substrate: Poly(Glu:Tyr))
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Nitric Oxide Synthase, Neuronal (nNOS) radioligand binding (ligand: [3H]L-Arginine)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
|
DRUGMATRIX: Angiotensin AT2 radioligand binding (ligand: [125I] CGP-42112A)
|
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: CYP450, 2A6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
|
ChEMBL.
|
No reference
|
Ki (binding)
|
= -5.91
|
In vitro binding to peroxisome proliferator activated receptor gamma (PPAR gamma) using [3H]-BRL 49653 as radioligand in scintillation proximity assay (SPA)
|
ChEMBL.
|
9836620
|
Ki (binding)
|
= -5.91
|
Binding affinity against Peroxisome proliferator activated receptor gamma (PPAR gamma)
|
ChEMBL.
|
10612594
|
Ki (binding)
|
nM
|
Binding affinity against Peroxisome Proliferator activated receptor alpha (PPAR alpha); Not active
|
ChEMBL.
|
10612594
|
Ki (binding)
|
nM
|
Binding affinity against Peroxisome proliferator activated receptor delta (PPAR delta); Not active
|
ChEMBL.
|
10612594
|
Ki (binding)
|
0 nM
|
Binding affinity against Peroxisome Proliferator activated receptor alpha (PPAR alpha); Not active
|
ChEMBL.
|
10612594
|
Ki (binding)
|
0 nM
|
Binding affinity against Peroxisome proliferator activated receptor delta (PPAR delta); Not active
|
ChEMBL.
|
10612594
|
Ki (binding)
|
= 199.4 nM
|
Inhibition of human recombinant soluble MAO-B expressed in Pichia pastoris incubated for 30 mins prior to substrate addition measured after 60 mins by MAO-Glo assay
|
ChEMBL.
|
25600407
|
Ki (binding)
|
= 270.8 nM
|
Inhibition of human recombinant microsomal MAO-B expressed in Pichia pastoris incubated for 30 mins prior to substrate addition measured after 60 mins by MAO-Glo assay
|
ChEMBL.
|
25600407
|
Ki (binding)
|
= 630 nM
|
Binding affinity to human Peroxisome proliferator activated receptor gamma using scintillation proximity assay
|
ChEMBL.
|
11720854
|
Ki (binding)
|
= 630 nM
|
Binding affinity to human Peroxisome proliferator activated receptor gamma using scintillation proximity assay
|
ChEMBL.
|
11720854
|
Ki (binding)
|
= 0.37 uM
|
Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by Cheng-Prusoff analysis
|
LITERATURE.
|
27687671
|
Ki (binding)
|
= 0.5 uM
|
Competitive inhibition of human MAOB expressed in Pichia pastoris
|
ChEMBL.
|
22282722
|
Ki (binding)
|
= 2.1 uM
|
Competitive inhibition of rat MAOB expressed in Pichia pastoris
|
ChEMBL.
|
22282722
|
Log EC50 (functional)
|
= 6.23
|
Activation of peroxisome proliferator activated receptor gamma measured by induction of 50% of maximum alkaline phosphatase activity, transfection assay in CV-1 cells
|
ChEMBL.
|
9836620
|
Log EC50 (functional)
|
= 6.23
|
Transcriptional activation of peroxisome proliferator activated receptor gamma
|
ChEMBL.
|
10612594
|
Log Ki (binding)
|
= 5.91
|
In vitro binding to peroxisome proliferator activated receptor gamma (PPAR gamma) using [3H]-BRL 49653 as radioligand in scintillation proximity assay (SPA)
|
ChEMBL.
|
9836620
|
Log Ki (binding)
|
= 5.91
|
Binding affinity against Peroxisome proliferator activated receptor gamma (PPAR gamma)
|
ChEMBL.
|
10612594
|
Max (functional)
|
= 1 %
|
Fold activation relative to maximum activation obtained with carbacyclin
|
ChEMBL.
|
11831892
|
Max (functional)
|
= 1 %
|
Fold activation relative to maximum activation obtained with carbacyclin
|
ChEMBL.
|
11831892
|
Max (functional)
|
= 57.8 %
|
Fold activation relative to maximum hPPAR alpha activation obtained with WY14643
|
ChEMBL.
|
11831892
|
Max (functional)
|
= 57.8 %
|
Fold activation relative to maximum hPPAR alpha activation obtained with WY14643
|
ChEMBL.
|
11831892
|
Max (functional)
|
= 90.8 %
|
Fold activation relative to maximum activation obtained with rosiglitazone
|
ChEMBL.
|
11831892
|
Max (functional)
|
= 90.8 %
|
Fold activation relative to maximum activation obtained with rosiglitazone
|
ChEMBL.
|
11831892
|
Max reduction (functional)
|
= 21 %
|
Maximum achieved triglycerides reduction relative to vehicle treated control group
|
ChEMBL.
|
11831892
|
Max reduction (functional)
|
= 21 %
|
In vivo nonfasting triglyceride in db/db mice after oral treament
|
ChEMBL.
|
14584939
|
Max reduction (functional)
|
= 21 %
|
Maximum achieved triglycerides reduction relative to vehicle treated control group
|
ChEMBL.
|
11831892
|
Max reduction (functional)
|
= 21 %
|
In vivo nonfasting triglyceride in db/db mice after oral treament
|
ChEMBL.
|
14584939
|
Max reduction (functional)
|
= 39 %
|
Maximum achieved blood glucose reduction relative to vehicle treated control group
|
ChEMBL.
|
11831892
|
Max reduction (functional)
|
= 39 %
|
Area under blood glucose time curve after oral glucose test in mice
|
ChEMBL.
|
14584939
|
Max reduction (functional)
|
= 39 %
|
Maximum achieved blood glucose reduction relative to vehicle treated control group
|
ChEMBL.
|
11831892
|
Max reduction (functional)
|
= 39 %
|
Area under blood glucose time curve after oral glucose test in mice
|
ChEMBL.
|
14584939
|
Max reduction (functional)
|
= 53 %
|
Maximum achieved blood glucose reduction relative to vehicle treated control group
|
ChEMBL.
|
11831892
|
Max reduction (functional)
|
= 53 %
|
In vivo nonfasting blood glucose in db/db mice after oral treament
|
ChEMBL.
|
14584939
|
Max reduction (functional)
|
= 53 %
|
Maximum achieved blood glucose reduction relative to vehicle treated control group
|
ChEMBL.
|
11831892
|
Max reduction (functional)
|
= 53 %
|
In vivo nonfasting blood glucose in db/db mice after oral treament
|
ChEMBL.
|
14584939
|
Max reduction (functional)
|
= 54 %
|
Maximum achieved insulin reduction relative to vehicle treated control group
|
ChEMBL.
|
11831892
|
Max reduction (functional)
|
= 54 %
|
In vivo insulin effect in db/db mice after oral treament
|
ChEMBL.
|
14584939
|
Max reduction (functional)
|
= 54 %
|
Maximum achieved insulin reduction relative to vehicle treated control group
|
ChEMBL.
|
11831892
|
Max reduction (functional)
|
= 54 %
|
In vivo insulin effect in db/db mice after oral treament
|
ChEMBL.
|
14584939
|
MED (functional)
|
= 300 uM kg-1
|
Minimum effective dose required for significant reduction in blood glucose in ob/ob mice
|
ChEMBL.
|
8576907
|
MED (functional)
|
= 300 uM kg-1
|
Minimum effective dose required for significant reduction in blood glucose in ob/ob mice
|
ChEMBL.
|
8576907
|
MED (functional)
|
= 200 uM.kg/diet
|
Minimum effective dose for anti-hyperglycaemic activity was determined in C57B1/6 ob/ob obese mouse
|
ChEMBL.
|
No reference
|
MED (functional)
|
= 200 uM.kg/diet
|
Minimum effective dose for anti-hyperglycaemic activity was determined in C57B1/6 ob/ob obese mouse
|
ChEMBL.
|
No reference
|
PB (ADMET)
|
= 353 pmol
|
Covalent binding in human liver microsomes measured per mg of protein using radiolabelled compound at 10 uM after 1 hr incubation by liquid scintillation counting
|
ChEMBL.
|
21467212
|
Potency (functional)
|
1.7291 uM
|
PubChem BioAssay. qHTS for small molecule inhibitors of Yes1 kinase: Primary Screen. (Class of assay: confirmatory)
|
ChEMBL.
|
No reference
|
Potency (functional)
|
2.5119 uM
|
PubChem BioAssay. qHTS Assay for Inhibitors of the Human Apurinic/apyrimidinic Endonuclease 1 (APE1). (Class of assay: confirmatory)
|
ChEMBL.
|
No reference
|
Potency (functional)
|
= 15.8489 um
|
PUBCHEM_BIOASSAY: qHTS Assay for Inhibitors of Aldehyde Dehydrogenase 1 (ALDH1A1). (Class of assay: confirmatory) [Related pubchem assays: 1030 (qHTS Validation Assay for Inhibitors of aldehyde dehydrogenase 1 (ALDH1A1))]
|
ChEMBL.
|
No reference
|
Rate of decrease (functional)
|
= 41 %
|
IIn vivo decrease in insulin in obese mice(ob/ob) at 10 mg/kg/day peroral administration for 2 weeks
|
ChEMBL.
|
10098657
|
Rate of decrease (functional)
|
= 41 %
|
IIn vivo decrease in insulin in obese mice(ob/ob) at 10 mg/kg/day peroral administration for 2 weeks
|
ChEMBL.
|
10098657
|
Rate of decrease (functional)
|
= 43 %
|
In vivo decrease in insulin in obese mice(ob/ob) at 3 mg/kg/day peroral administration for 2 weeks
|
ChEMBL.
|
10098657
|
Rate of decrease (functional)
|
= 43 %
|
In vivo decrease in insulin in obese mice(ob/ob) at 3 mg/kg/day peroral administration for 2 weeks
|
ChEMBL.
|
10098657
|
Rate of decrease (functional)
|
= 64 %
|
In vivo decrease in glucose in obese mice(ob/ob) at 3 mg/kg/day peroral administration for 2 weeks
|
ChEMBL.
|
10098657
|
Rate of decrease (functional)
|
= 64 %
|
In vivo decrease in glucose in obese mice(ob/ob) at 3 mg/kg/day peroral administration for 2 weeks
|
ChEMBL.
|
10098657
|
Rate of decrease (functional)
|
= 75 %
|
In vivo decrease in glucose in obese mice(ob/ob) at 10 mg/kg/day peroral administration for 2 weeks
|
ChEMBL.
|
10098657
|
Rate of decrease (functional)
|
= 75 %
|
In vivo decrease in glucose in obese mice(ob/ob) at 10 mg/kg/day peroral administration for 2 weeks
|
ChEMBL.
|
10098657
|
Rate of decrease (functional)
|
= 85 %
|
In vivo decrease in triglyceride in obese mice(ob/ob) by 3 mg/kg/day peroral administration for 2 weeks
|
ChEMBL.
|
10098657
|
Rate of decrease (functional)
|
= 85 %
|
In vivo decrease in triglyceride in obese mice(ob/ob) by 3 mg/kg/day peroral administration for 2 weeks
|
ChEMBL.
|
10098657
|
Rate of decrease (functional)
|
= 99 %
|
In vivo decrease in glucose in obese mice(ob/ob) by 10 mg/kg/day peroral administration for 2 weeks
|
ChEMBL.
|
10098657
|
Rate of decrease (functional)
|
= 99 %
|
In vivo decrease in glucose in obese mice(ob/ob) by 10 mg/kg/day peroral administration for 2 weeks
|
ChEMBL.
|
10098657
|
Reduction (functional)
|
0 %
|
Percent reduction in area under glucose tolerance curve (AUC) was determined at 100 micromol/kg dose of diet in mice; IA = No significant activity
|
ChEMBL.
|
7966158
|
Reduction (functional)
|
= 35 %
|
Percent reduction in area under glucose tolerance curve at 300 uM/kg dose in diet of mice.
|
ChEMBL.
|
7966158
|
Reduction (functional)
|
= 35 %
|
Percent reduction in area under glucose tolerance curve at 300 uM/kg dose in diet of mice.
|
ChEMBL.
|
7966158
|
Reduction (functional)
|
= 62 %
|
Percent reduction in area under glucose tolerance curve (AUC) was determined at 1000 micromol/kg dose of diet in mice
|
ChEMBL.
|
7966158
|
Reduction (functional)
|
= 62 %
|
Percent reduction in area under glucose tolerance curve (AUC) was determined at 1000 micromol/kg dose of diet in mice
|
ChEMBL.
|
7966158
|
Reduction (functional)
|
= 63 %
|
Percent reduction in area under glucose tolerance curve (AUC) was determined at 3000 micromol/kg dose of diet in mice
|
ChEMBL.
|
7966158
|
Reduction (functional)
|
= 63 %
|
Percent reduction in area under glucose tolerance curve (AUC) was determined at 3000 micromol/kg dose of diet in mice
|
ChEMBL.
|
7966158
|
RLU (functional)
|
= 2.1
|
Agonist activity at human PPARgamma expressed in human HEK293 cells assessed as SHP promoter transactivation at 100 nM by luciferase reporter gene assay relative to vehicle-treated control
|
ChEMBL.
|
22424975
|
RLU (functional)
|
= 2.2
|
Agonist activity at human PPARgamma expressed in human HEK293 cells at 100 nM by luciferase reporter gene assay relative to vehicle-treated control
|
ChEMBL.
|
22424975
|
RLU (functional)
|
= 2.8
|
Agonist activity at human PPARgamma expressed in human HEK293 cells assessed as ABCA1 promoter transactivation at 100 nM by luciferase reporter gene assay relative to vehicle-treated control
|
ChEMBL.
|
22424975
|
T/C (functional)
|
= 0.49
|
Compound was evaluated for Antihyperglycemic activity in KKAy mice, glucose level for the treated group (T) over the anti-hyperglycaemic activity
|
ChEMBL.
|
8978836
|
T/C (functional)
|
= 0.49
|
Compound was evaluated for Antihyperglycemic activity in KKAy mice, glucose level for the treated group (T) over the anti-hyperglycaemic activity
|
ChEMBL.
|
8978836
|
T1/2 (ADMET)
|
= 228 min
|
Oral half life of the compound was reported
|
ChEMBL.
|
11831892
|
Triglyceride level (ADMET)
|
= 73 mg dl-1
|
In vivo triglyceride level was observed in db/db mouse 4 weeks after oral administration (once daily) of 100 mg/kg of compound; (n=6)
|
ChEMBL.
|
15664804
|
Triglyceride level (ADMET)
|
= 109 mg dl-1
|
In vivo triglyceride level was observed in ZDF rats 4 weeks after oral administration (once daily) of 30 mg/kg of compound; (n=6)
|
ChEMBL.
|
15664804
|
Vss (ADMET)
|
= 0.22 l kg-1
|
Volume of distribution during steady state
|
ChEMBL.
|
11831892
|