Compile Data Set for Download or QSAR
Report error Found 28 Enz. Inhib. hit(s) for PDB: 6U4J
TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Forma Therapeutics

US Patent
LigandPNGBDBM50506474(Ft-2102 | Olutasidenib | US11376246, Compound 1 | ...)
Affinity DataIC50: 1nMAssay Description:Compound 1 was not initially reported as having the greatest biochemical potency compared to reports for certain other small molecule inhibitors of m...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/31/2023
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132C](Human)
Forma Therapeutics

US Patent
LigandPNGBDBM50506474(Ft-2102 | Olutasidenib | US11376246, Compound 1 | ...)
Affinity DataIC50: 5.10nMAssay Description:Compound 1 was not initially reported as having the greatest biochemical potency compared to reports for certain other small molecule inhibitors of m...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/31/2023
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Human)
Forma Therapeutics

Curated by ChEMBL
LigandPNGBDBM50506474(Ft-2102 | Olutasidenib | US11376246, Compound 1 | ...)
Affinity DataIC50: 6nMAssay 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:
2/19/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Human)
Forma Therapeutics

Curated by ChEMBL
LigandPNGBDBM50506474(Ft-2102 | Olutasidenib | US11376246, Compound 1 | ...)
Affinity DataIC50: 9nMAssay 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:
2/19/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Human)
Forma Therapeutics

Curated by ChEMBL
LigandPNGBDBM50506474(Ft-2102 | Olutasidenib | US11376246, Compound 1 | ...)
Affinity DataIC50: 9nMAssay 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:
2/19/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Forma Therapeutics

US Patent
LigandPNGBDBM50506474(Ft-2102 | Olutasidenib | US11376246, Compound 1 | ...)
Affinity DataIC50: 10nMAssay Description:Compound 1 was not initially reported as having the greatest biochemical potency compared to reports for certain other small molecule inhibitors of m...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/31/2023
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132L](Human)
Forma Therapeutics

US Patent
LigandPNGBDBM50506474(Ft-2102 | Olutasidenib | US11376246, Compound 1 | ...)
Affinity DataIC50: 10nMAssay Description:Compound 1 was not initially reported as having the greatest biochemical potency compared to reports for certain other small molecule inhibitors of m...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/31/2023
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132S](Human)
Forma Therapeutics

US Patent
LigandPNGBDBM50506474(Ft-2102 | Olutasidenib | US11376246, Compound 1 | ...)
Affinity DataIC50: 10nMAssay Description:Compound 1 was not initially reported as having the greatest biochemical potency compared to reports for certain other small molecule inhibitors of m...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/31/2023
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Forma Therapeutics

US Patent
LigandPNGBDBM50506474(Ft-2102 | Olutasidenib | US11376246, Compound 1 | ...)
Affinity DataIC50: 12.9nMAssay 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:
3/20/2023
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Forma Therapeutics

US Patent
LigandPNGBDBM50506474(Ft-2102 | Olutasidenib | US11376246, Compound 1 | ...)
Affinity DataIC50: 14.3nMAssay 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:
3/20/2023
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Human)
Forma Therapeutics

Curated by ChEMBL
LigandPNGBDBM50506474(Ft-2102 | Olutasidenib | US11376246, Compound 1 | ...)
Affinity DataIC50: 21nMAssay 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:
2/19/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Human)
Forma Therapeutics

Curated by ChEMBL
LigandPNGBDBM50506474(Ft-2102 | Olutasidenib | US11376246, Compound 1 | ...)
Affinity DataIC50: 21nMAssay Description:Inhibition of recombinant human Myc-DDK-tagged IDH1 R132H mutant using alpha-ketoglutarate as substrate preincubated for 15 mins followed by substrat...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/19/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Forma Therapeutics

US Patent
LigandPNGBDBM50506474(Ft-2102 | Olutasidenib | US11376246, Compound 1 | ...)
Affinity DataIC50: 21.2nMAssay Description:Please see paper.More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/5/2022
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Forma Therapeutics

US Patent
LigandPNGBDBM50506474(Ft-2102 | Olutasidenib | US11376246, Compound 1 | ...)
Affinity DataIC50: 21.2nMAssay Description:The cellular potency of Compound 1 in suppressing intracellular 2-HG levels was determined in cell lines expressing five different mutated IDH-1 prot...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/6/2022
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H](Human)
Forma Therapeutics

US Patent
LigandPNGBDBM50506474(Ft-2102 | Olutasidenib | US11376246, Compound 1 | ...)
Affinity DataIC50: 21.2nMAssay Description:Compound 1 was not initially reported as having the greatest biochemical potency compared to reports for certain other small molecule inhibitors of m...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/31/2023
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Human)
Forma Therapeutics

Curated by ChEMBL
LigandPNGBDBM50506474(Ft-2102 | Olutasidenib | US11376246, Compound 1 | ...)
Affinity DataIC50: 39nMAssay 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:
2/19/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Human)
Forma Therapeutics

Curated by ChEMBL
LigandPNGBDBM50506474(Ft-2102 | Olutasidenib | US11376246, Compound 1 | ...)
Affinity DataIC50: 42nMAssay 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:
2/19/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132G](Human)
Forma Therapeutics

US Patent
LigandPNGBDBM50506474(Ft-2102 | Olutasidenib | US11376246, Compound 1 | ...)
Affinity DataIC50: 50nMAssay Description:Compound 1 was not initially reported as having the greatest biochemical potency compared to reports for certain other small molecule inhibitors of m...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/31/2023
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132C](Human)
Forma Therapeutics

US Patent
LigandPNGBDBM50506474(Ft-2102 | Olutasidenib | US11376246, Compound 1 | ...)
Affinity DataIC50: 50nMAssay Description:Compound 1 was not initially reported as having the greatest biochemical potency compared to reports for certain other small molecule inhibitors of m...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/31/2023
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132C](Human)
Forma Therapeutics

US Patent
LigandPNGBDBM50506474(Ft-2102 | Olutasidenib | US11376246, Compound 1 | ...)
Affinity DataIC50: 67.1nMAssay 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:
3/20/2023
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132C](Human)
Forma Therapeutics

US Patent
LigandPNGBDBM50506474(Ft-2102 | Olutasidenib | US11376246, Compound 1 | ...)
Affinity DataIC50: 77nMAssay 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:
3/20/2023
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Human)
Forma Therapeutics

Curated by ChEMBL
LigandPNGBDBM50506474(Ft-2102 | Olutasidenib | US11376246, Compound 1 | ...)
Affinity DataIC50: 94nMAssay 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:
2/19/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132C](Human)
Forma Therapeutics

US Patent
LigandPNGBDBM50506474(Ft-2102 | Olutasidenib | US11376246, Compound 1 | ...)
Affinity DataIC50: 114nMAssay Description:Compound 1 was not initially reported as having the greatest biochemical potency compared to reports for certain other small molecule inhibitors of m...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/31/2023
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Human)
Forma Therapeutics

Curated by ChEMBL
LigandPNGBDBM50506474(Ft-2102 | Olutasidenib | US11376246, Compound 1 | ...)
Affinity DataIC50: 114nMAssay Description:Inhibition of recombinant human Myc-DDK-tagged IDH1 R132C mutant using alpha-ketoglutarate as substrate preincubated for 15 mins followed by substrat...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/19/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Human)
Forma Therapeutics

Curated by ChEMBL
LigandPNGBDBM50506474(Ft-2102 | Olutasidenib | US11376246, Compound 1 | ...)
Affinity DataIC50: 922nMAssay Description:Compound 1 was not initially reported as having the greatest biochemical potency compared to reports for certain other small molecule inhibitors of m...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/31/2023
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132C](Human)
Forma Therapeutics

US Patent
LigandPNGBDBM50506474(Ft-2102 | Olutasidenib | US11376246, Compound 1 | ...)
Affinity DataIC50: 5.22E+3nMAssay Description:The cellular potency of Compound 1 in suppressing intracellular 2-HG levels was determined in cell lines expressing five different mutated IDH-1 prot...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/6/2022
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132C](Human)
Forma Therapeutics

US Patent
LigandPNGBDBM50506474(Ft-2102 | Olutasidenib | US11376246, Compound 1 | ...)
Affinity DataIC50: 5.22E+3nMAssay Description:Please see paper.More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/5/2022
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Human)
Forma Therapeutics

Curated by ChEMBL
LigandPNGBDBM50506474(Ft-2102 | Olutasidenib | US11376246, Compound 1 | ...)
Affinity DataIC50: 2.24E+4nMAssay Description:Inhibition of wild-type IDH1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/19/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)