BDBM279977 US10028961, Compound 130::US10172864, Compound 130::US10946023, Compound 130
SMILES CC(Nc1nc(NC(C)C(F)(F)F)nc(n1)-c1cccc(Cl)n1)C(F)(F)F
InChI Key InChIKey=QCZAWDGAVJMPTA-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 14 hits for monomerid = 279977
TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H](Homo sapiens (Human))
Agios Pharmaceuticals
US Patent
Agios Pharmaceuticals
US Patent
Affinity DataIC50: <50nMpH: 6.5 T: 2°CAssay Description:In the primary reaction, the reduction of α-KG acid to 2-HG is accompanied by a concomitant oxidation of NADPH to NADP. The amount of NADPH rema...More data for this Ligand-Target Pair
3D Structure (crystal)TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132C](Homo sapiens (Human))
Agios Pharmaceuticals
US Patent
Agios Pharmaceuticals
US Patent
Affinity DataIC50: <50nMpH: 6.5 T: 2°CAssay Description:In the primary reaction, the reduction of α-KG acid to 2-HG is accompanied by a concomitant oxidation of NADPH to NADP. The amount of NADPH rema...More data for this Ligand-Target Pair
TargetIsocitrate dehydrogenase [NADP], mitochondrial [R140Q](Homo sapiens (Human))
Agios Pharmaceuticals
US Patent
Agios Pharmaceuticals
US Patent
Affinity DataIC50: <50nMpH: 7.5 T: 2°CAssay Description:Compounds are assayed for IDH2 R140Q inhibitory activity through a cofactor depletion assay. Compounds are preincubated with enzyme, then the reactio...More data for this Ligand-Target Pair
TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H](Homo sapiens (Human))
Agios Pharmaceuticals
US Patent
Agios Pharmaceuticals
US Patent
Affinity DataIC50: <50nMpH: 7.5 T: 2°CAssay Description:A test compound is prepared as 10 mM stock in DMSO and diluted to 50× final concentration in DMSO, for a 50 μl reaction mixture. IDH enzyme acti...More data for this Ligand-Target Pair
TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H](Homo sapiens (Human))
Agios Pharmaceuticals
US Patent
Agios Pharmaceuticals
US Patent
Affinity DataIC50: <50nMAssay Description:In the primary reaction, the reduction of α-KG acid to 2-HG is accompanied by a concomitant oxidation of NADPH to NADP. The amount of NADPH rema...More data for this Ligand-Target Pair
TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H](Homo sapiens (Human))
Agios Pharmaceuticals
US Patent
Agios Pharmaceuticals
US Patent
Affinity DataIC50: <50nMAssay Description:In the primary reaction, the reduction of α-KG acid to 2-HG is accompanied by a concomitant oxidation of NADPH to NADP. The amount of NADPH rema...More data for this Ligand-Target Pair
TargetIsocitrate dehydrogenase [NADP], mitochondrial [R140Q](Homo sapiens (Human))
Agios Pharmaceuticals
US Patent
Agios Pharmaceuticals
US Patent
Affinity DataIC50: <50nMAssay Description:Compounds are assayed for IDH2 R140Q inhibitory activity through a cofactor depletion assay. Compounds are preincubated with enzyme, then the reactio...More data for this Ligand-Target Pair
TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H](Homo sapiens (Human))
Agios Pharmaceuticals
US Patent
Agios Pharmaceuticals
US Patent
Affinity DataIC50: <50nMAssay Description:A test compound is prepared as 10 mM stock in DMSO and diluted to 50× final concentration in DMSO, for a 50 μl reaction mixture. IDH enzyme acti...More data for this Ligand-Target Pair
TargetIsocitrate dehydrogenase [NADP], mitochondrial(Homo sapiens (Human))
Agios Pharmaceuticals
Curated by ChEMBL
Agios Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 8nMAssay Description:Inhibition of IDH2 R140Q mutant (unknown origin) transfected using lentiviral expression system in human U87MG cells assessed as reduction in 2-HG co...More data for this Ligand-Target Pair
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Homo sapiens (Human))
Agios Pharmaceuticals
Curated by ChEMBL
Agios Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 0.300nMAssay Description:Inhibition of IDH1 R132H mutant in glioma patient-derived human TS603 neurosphere cells assessed as reduction in 2-HG content using alpha-ketoglutara...More data for this Ligand-Target Pair
TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H](Homo sapiens (Human))
Agios Pharmaceuticals
US Patent
Agios Pharmaceuticals
US Patent
Affinity DataIC50: <50nMAssay Description:A test compound is prepared as 10 mM stock in DMSO and diluted to 50× final concentration in DMSO, for a 50 μl reaction mixture. IDH enzyme acti...More data for this Ligand-Target Pair
TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H](Homo sapiens (Human))
Agios Pharmaceuticals
US Patent
Agios Pharmaceuticals
US Patent
Affinity DataIC50: <50nMAssay Description:In the primary reaction, the reduction of α-KG acid to 2-HG is accompanied by a concomitant oxidation of NADPH to NADP. The amount of NADPH rema...More data for this Ligand-Target Pair
TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132C](Homo sapiens (Human))
Agios Pharmaceuticals
US Patent
Agios Pharmaceuticals
US Patent
Affinity DataIC50: <50nMAssay Description:In the primary reaction, the reduction of α-KG acid to 2-HG is accompanied by a concomitant oxidation of NADPH to NADP. The amount of NADPH rema...More data for this Ligand-Target Pair
TargetIsocitrate dehydrogenase [NADP], mitochondrial [R140Q](Homo sapiens (Human))
Agios Pharmaceuticals
US Patent
Agios Pharmaceuticals
US Patent
Affinity DataIC50: <50nMAssay Description:Compounds are assayed for IDH2 R140Q inhibitory activity through a cofactor depletion assay. Compounds are preincubated with enzyme, then the reactio...More data for this Ligand-Target Pair