BDBM383860 US10280150, Cmpd No I-143::US10550099, Compound I-143

SMILES COc1cc2[nH]c(=O)c(cc2cc1Cl)[C@H](C)Nc1ncc(C#N)c(OC)n1

InChI Key

Data  15 IC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
   Substructure
Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 15 hits for monomerid = 383860   

TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H](Homo sapiens (Human))
Forma Tm2

US Patent
LigandPNGBDBM383860(US10280150, Cmpd No I-143 | US10550099, Compound I...)
Affinity DataIC50: <100nMAssay Description:Assays were performed in a 384-well black plate. An aliquot of 250 nL of compound was incubated with 10 μL of 30 nM IDH1-R132H or 10 nM IDH1-R13...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Homo sapiens (Human))
Forma Therapeutics

Curated by ChEMBL
LigandPNGBDBM383860(US10280150, Cmpd No I-143 | US10550099, Compound I...)
Affinity DataIC50:  5nMAssay Description:Inhibition of human Myc-DDK-tagged IDH1 R132L mutant expressed in human U87MG cells assessed as reduction in 2-HG levels after 24 hrs by RapidFire hi...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H](Homo sapiens (Human))
Forma Tm2

US Patent
LigandPNGBDBM383860(US10280150, Cmpd No I-143 | US10550099, Compound I...)
Affinity DataIC50: <100nMAssay Description:Assays were performed in a 384-well black plate. An aliquot of 250 nL of compound was incubated with 10 μL of 30 nM IDH1-R132H or 10 nM IDH1-R13...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132C](Homo sapiens (Human))
Forma Therapeutics

US Patent
LigandPNGBDBM383860(US10280150, Cmpd No I-143 | US10550099, Compound I...)
Affinity DataIC50: <100nMAssay Description:Assays were performed in a 384-well black plate. An aliquot of 250 nL of compound was incubated with 10 μL of 30 nM IDH1-R132H or 10 nM IDH1-R13...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Homo sapiens (Human))
Forma Therapeutics

Curated by ChEMBL
LigandPNGBDBM383860(US10280150, Cmpd No I-143 | US10550099, Compound I...)
Affinity DataIC50: <10nMAssay Description:Inhibition of IDH1 R132H mutant (unknown origin) assessed as reduction in NADPH consumption using alpha-KG as substrate incubated for 45 mins by by d...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Homo sapiens (Human))
Forma Therapeutics

Curated by ChEMBL
LigandPNGBDBM383860(US10280150, Cmpd No I-143 | US10550099, Compound I...)
Affinity DataIC50: <10nMAssay Description:Inhibition of IDH1 R132C mutant (unknown origin) assessed as reduction in NADPH consumption using alpha-KG as substrate incubated for 45 mins by by d...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Homo sapiens (Human))
Forma Therapeutics

Curated by ChEMBL
LigandPNGBDBM383860(US10280150, Cmpd No I-143 | US10550099, Compound I...)
Affinity DataIC50:  1nMAssay Description:Inhibition of human Myc-DDK-tagged IDH1 R132H mutant expressed in human U87MG cells assessed as reduction in 2-HG levels after 24 hrs by RapidFire hi...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Homo sapiens (Human))
Forma Therapeutics

Curated by ChEMBL
LigandPNGBDBM383860(US10280150, Cmpd No I-143 | US10550099, Compound I...)
Affinity DataIC50:  36nMAssay Description:Inhibition of human Myc-DDK-tagged IDH1 R132C mutant assessed as reduction in NADPH consumption pre-incubated for 15 mins followed by alpha-ketogluta...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Homo sapiens (Human))
Forma Therapeutics

Curated by ChEMBL
LigandPNGBDBM383860(US10280150, Cmpd No I-143 | US10550099, Compound I...)
Affinity DataIC50:  11nMAssay Description:Inhibition of IDH1 R132H mutant in human HCT116 cells assessed as reduction in 2-HG levels after 24 hrs by RapidFire high-throughput mass spectrometr...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Homo sapiens (Human))
Forma Therapeutics

Curated by ChEMBL
LigandPNGBDBM383860(US10280150, Cmpd No I-143 | US10550099, Compound I...)
Affinity DataIC50:  40nMAssay Description:Inhibition of IDH1 R132C mutant in human HCT116 cells assessed as reduction in 2-HG levels after 24 hrs by RapidFire high-throughput mass spectrometr...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Homo sapiens (Human))
Forma Therapeutics

Curated by ChEMBL
LigandPNGBDBM383860(US10280150, Cmpd No I-143 | US10550099, Compound I...)
Affinity DataIC50:  4nMAssay Description:Inhibition of human Myc-DDK-tagged IDH1 R132C mutant expressed in human U87MG cells assessed as reduction in 2-HG levels after 24 hrs by RapidFire hi...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Homo sapiens (Human))
Forma Therapeutics

Curated by ChEMBL
LigandPNGBDBM383860(US10280150, Cmpd No I-143 | US10550099, Compound I...)
Affinity DataIC50:  3nMAssay Description:Inhibition of human Myc-DDK-tagged IDH1 R132G mutant expressed in human U87MG cells assessed as reduction in 2-HG levels after 24 hrs by RapidFire hi...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Homo sapiens (Human))
Forma Therapeutics

Curated by ChEMBL
LigandPNGBDBM383860(US10280150, Cmpd No I-143 | US10550099, Compound I...)
Affinity DataIC50:  9nMAssay Description:Inhibition of human Myc-DDK-tagged IDH1 R132H mutant assessed as reduction in NADPH consumption pre-incubated for 15 mins followed by alpha-ketogluta...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Homo sapiens (Human))
Forma Therapeutics

Curated by ChEMBL
LigandPNGBDBM383860(US10280150, Cmpd No I-143 | US10550099, Compound I...)
Affinity DataIC50:  129nMAssay Description:Inhibition of human Myc-DDK-tagged IDH1 R132S mutant expressed in human U87MG cells assessed as reduction in 2-HG levels after 24 hrs by RapidFire hi...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132C](Homo sapiens (Human))
Forma Therapeutics

US Patent
LigandPNGBDBM383860(US10280150, Cmpd No I-143 | US10550099, Compound I...)
Affinity DataIC50: <100nMAssay Description:Assays were performed in a 384-well black plate. An aliquot of 250 nL of compound was incubated with 10 μL of 30 nM IDH1-R132H or 10 nM IDH1-R13...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent