EC50 (functional)
|
= 120 nM
|
Growth inhibitory activity of the compound against CCRF-CEM human lymphoblastic leukemia cells
|
ChEMBL.
|
16078850
|
EC50 (functional)
|
= 120 nM
|
Growth inhibitory activity of the compound against CCRF-CEM human lymphoblastic leukemia cells
|
ChEMBL.
|
16078850
|
EC50 (functional)
|
= 265 nM
|
Growth inhibitory activity of the compound against resistant CCRF-CEM human lymphoblastic leukemia cells with decreased uptake of MTX
|
ChEMBL.
|
16078850
|
EC50 (functional)
|
= 265 nM
|
Growth inhibitory activity of the compound against resistant CCRF-CEM human lymphoblastic leukemia cells with decreased uptake of MTX
|
ChEMBL.
|
16078850
|
EC50 (functional)
|
= 3150 nM
|
Growth inhibitory activity of the compound against MTX resistant CCRF-CEM human lymphoblastic leukemia cells with decreased polyglutamylation
|
ChEMBL.
|
16078850
|
EC50 (functional)
|
= 3150 nM
|
Growth inhibitory activity of the compound against MTX resistant CCRF-CEM human lymphoblastic leukemia cells with decreased polyglutamylation
|
ChEMBL.
|
16078850
|
EC50 (functional)
|
= 4850 nM
|
Growth inhibitory activity of the compound against MTX resistant subline of CCRF-CEM human lymphoblastic leukemia cells
|
ChEMBL.
|
16078850
|
EC50 (functional)
|
= 4850 nM
|
Growth inhibitory activity of the compound against MTX resistant subline of CCRF-CEM human lymphoblastic leukemia cells
|
ChEMBL.
|
16078850
|
GI50 (functional)
|
= 0.0000000381 M
|
Cytotoxicity of compound aganist HL-60 leukemia cell line
|
ChEMBL.
|
16078850
|
GI50 (functional)
|
= 0.0000000381 M
|
Cytotoxicity of compound aganist HL-60 leukemia cell line
|
ChEMBL.
|
16078850
|
GI50 (functional)
|
= 0.0000000478 M
|
Cytotoxicity of compound aganist SR leukemia cell line
|
ChEMBL.
|
16078850
|
GI50 (functional)
|
= 0.0000000478 M
|
Cytotoxicity of compound aganist SR leukemia cell line
|
ChEMBL.
|
16078850
|
GI50 (functional)
|
= 0.0000000783 M
|
Cytotoxicity of compound aganist SW-620 colon cancer cell line
|
ChEMBL.
|
16078850
|
GI50 (functional)
|
= 0.0000000783 M
|
Cytotoxicity of compound aganist SW-620 colon cancer cell line
|
ChEMBL.
|
16078850
|
GI50 (functional)
|
= 0.000000214 M
|
Cytotoxicity of compound aganist K-564 leukemia cell line
|
ChEMBL.
|
16078850
|
GI50 (functional)
|
= 0.000000214 M
|
Cytotoxicity of compound aganist K-564 leukemia cell line
|
ChEMBL.
|
16078850
|
GI50 (functional)
|
> 0.0001 M
|
Cytotoxicity of compound aganist 786-0 renal cancer cell line
|
ChEMBL.
|
16078850
|
GI50 (functional)
|
> 0.0001 M
|
Cytotoxicity of compound aganist 786-0 renal cancer cell line
|
ChEMBL.
|
16078850
|
IC50 (binding)
|
= 10 uM
|
Inhibition of Lactobacillus casei dihydrofolate reductase at 37 degree C pH 7.4
|
ChEMBL.
|
16078850
|
IC50 (binding)
|
= 10 uM
|
Inhibition of Lactobacillus casei dihydrofolate reductase at 37 degree C pH 7.4
|
ChEMBL.
|
16078850
|
IC50 (binding)
|
> 18 uM
|
Inhibition of human thymidylate synthetase at 37 degree C pH 7.4
|
ChEMBL.
|
16078850
|
IC50 (binding)
|
> 18 uM
|
Inhibition of human thymidylate synthetase at 37 degree C pH 7.4
|
ChEMBL.
|
16078850
|
IC50 (binding)
|
= 21 uM
|
Inhibition of human dihydrofolate reductase at 37 degree C pH 7.4
|
ChEMBL.
|
16078850
|
IC50 (binding)
|
= 21 uM
|
Inhibition of Escherichia coli dihydrofolate reductase at 37 degree C pH 7.4
|
ChEMBL.
|
16078850
|
IC50 (binding)
|
= 21 uM
|
Inhibition of human dihydrofolate reductase at 37 degree C pH 7.4
|
ChEMBL.
|
16078850
|
IC50 (binding)
|
= 21 uM
|
Inhibition of Escherichia coli dihydrofolate reductase at 37 degree C pH 7.4
|
ChEMBL.
|
16078850
|
IC50 (binding)
|
> 100 uM
|
Inhibition of Escherichia coli thymidylate synthetase at 37 degree C pH 7.4
|
ChEMBL.
|
16078850
|
IC50 (binding)
|
> 100 uM
|
Inhibition of Lactobacillus casei thymidylate synthetase at 37 degree C pH 7.4
|
ChEMBL.
|
16078850
|
IC50 (binding)
|
> 100 uM
|
Inhibition of Escherichia coli thymidylate synthetase at 37 degree C pH 7.4
|
ChEMBL.
|
16078850
|
IC50 (binding)
|
> 100 uM
|
Inhibition of Lactobacillus casei thymidylate synthetase at 37 degree C pH 7.4
|
ChEMBL.
|
16078850
|
Km (ADMET)
|
= 2
|
Km of the compound (FPGS substrate activity) for recombinant human FPGS
|
ChEMBL.
|
16078850
|
Ratio (ADMET)
|
= 0.27
|
Ratio of Vmax, rel to Km of the compound (FPGS substrate activity) for recombinant human FPGS
|
ChEMBL.
|
16078850
|
Relative growth (functional)
|
= 20 %
|
Protection of CCRF-CEM human leukemia cells against the growth inhibitory effect of MTX by 5 uM of thymidine at 5000 nM concentration of compound
|
ChEMBL.
|
16078850
|
Relative growth (functional)
|
= 20 %
|
Protection of CCRF-CEM human leukemia cells against the growth inhibitory effect of MTX by 5 uM of thymidine at 5000 nM concentration of compound
|
ChEMBL.
|
16078850
|
Relative growth (functional)
|
= 21 %
|
Protection of CCRF-CEM human leukemia cells against the growth inhibitory effect of MTX by 10 uM of hypoxanthine at 5000 nM concentration of compound
|
ChEMBL.
|
16078850
|
Relative growth (functional)
|
= 21 %
|
Protection of CCRF-CEM human leukemia cells against the growth inhibitory effect of MTX by 10 uM of hypoxanthine at 5000 nM concentration of compound
|
ChEMBL.
|
16078850
|
Relative growth (functional)
|
= 74 %
|
Protection of CCRF-CEM human leukemia cells against the growth inhibitory effect of MTX by 10 uM of hypoxanthine and 5 uM of thymidine at 5000 nM concentration of compound
|
ChEMBL.
|
16078850
|
Relative growth (functional)
|
= 74 %
|
Protection of CCRF-CEM human leukemia cells against the growth inhibitory effect of MTX by 10 uM of hypoxanthine and 5 uM of thymidine at 5000 nM concentration of compound
|
ChEMBL.
|
16078850
|
Vmax rel (ADMET)
|
= 0.54
|
Vmax, rel of the compound (FPGS substrate activity) for recombinant human FPGS
|
ChEMBL.
|
16078850
|