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 InChIKey=DIDCUOGCZYTDKE-UHFFFAOYSA-N

Data  15 IC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 15 hits for monomerid = 383860   

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
In Depth
Date in BDB:
2/21/2020
Entry Details
Go to 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
In Depth
Date in BDB:
2/21/2020
Entry Details
Go to 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
In Depth
Date in BDB:
11/7/2020
Entry Details
Go to 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
In Depth
Date in BDB:
11/7/2020
Entry Details
Go to US Patent

TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Human)
China Pharmaceutical University

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
In Depth
Date in BDB:
2/18/2021
Entry Details Article
PubMed
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Human)
China Pharmaceutical University

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
In Depth
Date in BDB:
2/18/2021
Entry Details Article
PubMed
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Human)
China Pharmaceutical University

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
In Depth
Date in BDB:
2/21/2021
Entry Details Article
PubMed
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Human)
China Pharmaceutical University

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
In Depth
Date in BDB:
2/21/2021
Entry Details Article
PubMed
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Human)
China Pharmaceutical University

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
In Depth
Date in BDB:
2/21/2021
Entry Details Article
PubMed
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Human)
China Pharmaceutical University

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
In Depth
Date in BDB:
2/21/2021
Entry Details Article
PubMed
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Human)
China Pharmaceutical University

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
In Depth
Date in BDB:
2/21/2021
Entry Details Article
PubMed
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Human)
China Pharmaceutical University

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
In Depth
Date in BDB:
2/21/2021
Entry Details Article
PubMed
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Human)
China Pharmaceutical University

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
In Depth
Date in BDB:
2/21/2021
Entry Details Article
PubMed
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Human)
China Pharmaceutical University

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
In Depth
Date in BDB:
2/21/2021
Entry Details Article
PubMed
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Human)
China Pharmaceutical University

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
In Depth
Date in BDB:
2/21/2021
Entry Details Article
PubMed