BDBM279948 US10028961, Compound 101::US10172864, Compound 101::US10946023, Compound 101
SMILES C[C@@H](Nc1nc(N[C@H](C)C(F)(F)F)nc(n1)-c1cccc(Cl)n1)C(F)(F)F
InChI Key InChIKey=QCZAWDGAVJMPTA-RNFRBKRXSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 24 hits for monomerid = 279948
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: <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 [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: 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] 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 [R132C](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: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: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 [R132C](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(Homo sapiens (Human))
China Pharmaceutical University
Curated by ChEMBL
China Pharmaceutical University
Curated by ChEMBL
Affinity DataIC50: 0.0400nMAssay Description:Inhibition of IDH1 R132C mutant (unknown origin) assessed as reduction in 2-HG levels after 90 mins in presence of NADPH by resazurin-based assayMore data for this Ligand-Target Pair
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Homo sapiens (Human))
China Pharmaceutical University
Curated by ChEMBL
China Pharmaceutical University
Curated by ChEMBL
Affinity DataIC50: 0.0400nMAssay Description:Inhibition of IDH1 R132S mutant (unknown origin) assessed as reduction in 2-HG levels after 90 mins in presence of NADPH by resazurin-based assayMore data for this Ligand-Target Pair
TargetIsocitrate dehydrogenase [NADP], mitochondrial(Homo sapiens (Human))
China Pharmaceutical University
Curated by ChEMBL
China Pharmaceutical University
Curated by ChEMBL
Affinity DataIC50: 130nMAssay Description:Inhibition of IDH2 R172K mutant (unknown origin) assessed as reduction in 2-HG levels after 90 mins in presence of NADPH by resazurin-based assayMore data for this Ligand-Target Pair
TargetIsocitrate dehydrogenase [NADP], mitochondrial(Homo sapiens (Human))
China Pharmaceutical University
Curated by ChEMBL
China Pharmaceutical University
Curated by ChEMBL
Affinity DataIC50: 7nMAssay Description:Inhibition of IDH2 R140Q mutant (unknown origin) assessed as reduction in 2-HG levels after 90 mins in presence of NADPH by resazurin-based assayMore data for this Ligand-Target Pair
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Homo sapiens (Human))
China Pharmaceutical University
Curated by ChEMBL
China Pharmaceutical University
Curated by ChEMBL
Affinity DataIC50: 0.0400nMAssay Description:Inhibition of IDH1 R132H mutant (unknown origin) assessed as reduction in 2-HG levels after 90 mins in presence of NADPH by resazurin-based assayMore data for this Ligand-Target Pair
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Homo sapiens (Human))
China Pharmaceutical University
Curated by ChEMBL
China Pharmaceutical University
Curated by ChEMBL
Affinity DataIC50: 0.0400nMAssay Description:Inhibition of IDH1 R132G mutant (unknown origin) assessed as reduction in 2-HG levels after 90 mins in presence of NADPH by resazurin-based assayMore 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
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: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 [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