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Found 1424 with Last Name = 'ashwell' and Initial = 's'
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Astrazeneca R&D Boston

Curated by ChEMBL
LigandPNGBDBM50325177(5-methyl-8-(1H-pyrrol-2-yl)-[1,2,4]triazolo[4,3-a]...)
Affinity DataIC50:  0.100nMAssay Description:Inhibition of Chk1More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Astrazeneca R&D Boston

Curated by ChEMBL
LigandPNGBDBM50325177(5-methyl-8-(1H-pyrrol-2-yl)-[1,2,4]triazolo[4,3-a]...)
Affinity DataIC50:  0.100nMAssay Description:Inhibition of His6-CHK1 expressed in baculovirus infected Sf9 cellsMore data for this Ligand-Target Pair
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 [R132H](Homo sapiens (Human))
Forma Therapeutics

US Patent
LigandPNGBDBM50506474(Ft-2102 | Olutasidenib | US11311527, Cpd ID 1 | US...)
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
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Homo sapiens (Human))
Forma Therapeutics

Curated by ChEMBL
LigandPNGBDBM50503260(CHEMBL4456610 | US11311527, Cpd ID I-27 | US113762...)
Affinity DataIC50:  2nMAssay 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
LigandPNGBDBM50503280(CHEMBL4469055 | US11311527, Cpd ID I-26 | US113762...)
Affinity DataIC50: <2nMAssay 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
LigandPNGBDBM50503280(CHEMBL4469055 | US11311527, Cpd ID I-26 | US113762...)
Affinity DataIC50: <2nMAssay 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
LigandPNGBDBM50503263(CHEMBL4464313 | US11311527, Cpd ID I-23 | US113762...)
Affinity DataIC50: <2nMAssay 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
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Astrazeneca R&D Boston

Curated by ChEMBL
LigandPNGBDBM50379546(CHEMBL2012879)
Affinity DataIC50:  3nMAssay Description:Inhibition of Chk1More data for this Ligand-Target Pair
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
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Astrazeneca R&D Boston

Curated by ChEMBL
LigandPNGBDBM50243148(1-(3-((S)-piperidin-3-ylcarbamoyl)-5-(thiophen-2-y...)
Affinity DataIC50:  3nMAssay Description:Inhibition of Chk1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Astrazeneca R&D Boston

Curated by ChEMBL
LigandPNGBDBM50243624((R)-1-(3-(azepan-3-ylcarbamoyl)-5-phenylthiophen-2...)
Affinity DataIC50:  3nMAssay Description:Inhibition of Chk1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132C](Homo sapiens (Human))
Forma Therapeutics

US Patent
LigandPNGBDBM195601(GSK321 | US11311527, Cpd ID GSK321 | US11376246, C...)
Affinity DataIC50:  3.80nMAssay 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
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
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Astrazeneca R&D Boston

Curated by ChEMBL
LigandPNGBDBM50379547(CHEMBL2012859)
Affinity DataIC50:  4nMAssay Description:Inhibition of Chk1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Astrazeneca R&D Boston

Curated by ChEMBL
LigandPNGBDBM50325145(5-methyl-8-(1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a...)
Affinity DataIC50:  4nMAssay Description:Inhibition of His6-CHK1 expressed in baculovirus infected Sf9 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Homo sapiens (Human))
Forma Therapeutics

Curated by ChEMBL
LigandPNGBDBM50506480(CHEMBL4437754 | US11311527, Cpd ID I-20 | US113762...)
Affinity DataIC50:  4nMAssay 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
LigandPNGBDBM383892(US10280150, Cmpd No I-175 | US10550099, Compound I...)
Affinity DataIC50:  4nMAssay 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
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Astrazeneca R&D Boston

Curated by ChEMBL
LigandPNGBDBM50243151((S)-1-(3-(piperidin-3-ylcarbamoyl)-5-(pyridin-4-yl...)
Affinity DataIC50:  4nMAssay Description:Inhibition of Chk1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Homo sapiens (Human))
Forma Therapeutics

Curated by ChEMBL
LigandPNGBDBM383892(US10280150, Cmpd No I-175 | US10550099, Compound I...)
Affinity DataIC50:  4nMAssay 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
LigandPNGBDBM50503280(CHEMBL4469055 | US11311527, Cpd ID I-26 | US113762...)
Affinity DataIC50:  4nMAssay 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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H](Homo sapiens (Human))
Forma Therapeutics

US Patent
LigandPNGBDBM195601(GSK321 | US11311527, Cpd ID GSK321 | US11376246, C...)
Affinity DataIC50:  4.80nMAssay 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
TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H](Homo sapiens (Human))
Forma Therapeutics

US Patent
LigandPNGBDBM195601(GSK321 | US11311527, Cpd ID GSK321 | US11376246, C...)
Affinity DataIC50:  4.80nMAssay Description:Please see paper.More data for this Ligand-Target Pair
TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132H](Homo sapiens (Human))
Forma Therapeutics

US Patent
LigandPNGBDBM195601(GSK321 | US11311527, Cpd ID GSK321 | US11376246, C...)
Affinity DataIC50:  4.80nMAssay 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
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Astrazeneca R&D Boston

Curated by ChEMBL
LigandPNGBDBM50379548(CHEMBL2012858)
Affinity DataIC50:  5nMAssay Description:Inhibition of Chk1More data for this Ligand-Target Pair
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:  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
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Astrazeneca R&D Boston

Curated by ChEMBL
LigandPNGBDBM50243047(1-(3-((S)-piperidin-3-ylcarbamoyl)-5-(3-carbamoylp...)
Affinity DataIC50:  5nMAssay Description:Inhibition of Chk1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Astrazeneca R&D Boston

Curated by ChEMBL
LigandPNGBDBM50389803(AZD7762 | CHEMBL2041933)
Affinity DataIC50:  5nMAssay Description:Inhibition of human recombinant CHK1 expressed in insect cells using biotinylaminohexanoyl-KKVSRSGLYRSPMPENLNRPR as substrate after 2 hrs by scintill...More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Astrazeneca R&D Boston

Curated by ChEMBL
LigandPNGBDBM50243201((S)-1-(5-(4-carbamoylphenyl)-3-(piperidin-3-ylcarb...)
Affinity DataIC50:  5nMAssay Description:Inhibition of Chk1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetIsocitrate dehydrogenase [NADP] cytoplasmic [R132C](Homo sapiens (Human))
Forma Therapeutics

US Patent
LigandPNGBDBM50506474(Ft-2102 | Olutasidenib | US11311527, Cpd ID 1 | US...)
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
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Homo sapiens (Human))
Forma Therapeutics

Curated by ChEMBL
LigandPNGBDBM50503263(CHEMBL4464313 | US11311527, Cpd ID I-23 | US113762...)
Affinity DataIC50:  6nMAssay 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
LigandPNGBDBM377646(4-({[6-chloro-2-oxo-7-(pyridin-2-ylmethoxy)-1,2- |...)
Affinity DataIC50:  6nMAssay 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
LigandPNGBDBM50506474(Ft-2102 | Olutasidenib | US11311527, Cpd ID 1 | US...)
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
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Astrazeneca R&D Boston

Curated by ChEMBL
LigandPNGBDBM50325161(5-methyl-8-(4-(piperazin-1-ylmethyl)phenyl)-[1,2,4...)
Affinity DataIC50:  6nMAssay Description:Inhibition of His6-CHK1 expressed in baculovirus infected Sf9 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Astrazeneca R&D Boston

Curated by ChEMBL
LigandPNGBDBM50379549(CHEMBL2012857)
Affinity DataIC50:  6nMAssay Description:Inhibition of Chk1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Astrazeneca R&D Boston

Curated by ChEMBL
LigandPNGBDBM50243102((S)-1-(5-(4-(methylsulfonyl)phenyl)-3-(piperidin-3...)
Affinity DataIC50:  6nMAssay Description:Inhibition of Chk1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Astrazeneca R&D Boston

Curated by ChEMBL
LigandPNGBDBM50389806(CHEMBL2070714)
Affinity DataIC50:  6nMAssay Description:Inhibition of human recombinant CHK1 expressed in insect cells using biotinylaminohexanoyl-KKVSRSGLYRSPMPENLNRPR as substrate after 2 hrs by scintill...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Astrazeneca R&D Boston

Curated by ChEMBL
LigandPNGBDBM50389817(CHEMBL2070702)
Affinity DataIC50:  6nMAssay Description:Inhibition of human recombinant CHK1 expressed in insect cells using biotinylaminohexanoyl-KKVSRSGLYRSPMPENLNRPR as substrate after 2 hrs by scintill...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Astrazeneca R&D Boston

Curated by ChEMBL
LigandPNGBDBM50243049((S)-1-(5-(4-cyanophenyl)-3-(piperidin-3-ylcarbamoy...)
Affinity DataIC50:  6nMAssay Description:Inhibition of Chk1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Astrazeneca R&D Boston

Curated by ChEMBL
LigandPNGBDBM50243150(1-(3-((S)-piperidin-3-ylcarbamoyl)-5-(pyridin-3-yl...)
Affinity DataIC50:  6nMAssay Description:Inhibition of Chk1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Astrazeneca R&D Boston

Curated by ChEMBL
LigandPNGBDBM50243149(1-(3-((S)-piperidin-3-ylcarbamoyl)-5-(thiophen-3-y...)
Affinity DataIC50:  6nMAssay Description:Inhibition of Chk1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Astrazeneca R&D Boston

Curated by ChEMBL
LigandPNGBDBM50243049((S)-1-(5-(4-cyanophenyl)-3-(piperidin-3-ylcarbamoy...)
Affinity DataIC50:  6nMAssay Description:Inhibition of human recombinant CHK1 expressed in insect cells using biotinylaminohexanoyl-KKVSRSGLYRSPMPENLNRPR as substrate after 2 hrs by scintill...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Homo sapiens (Human))
Forma Therapeutics

Curated by ChEMBL
LigandPNGBDBM377574(4-{[(1S)-1-(6-chloro-2-oxo- | US10266495, Compound...)
Affinity DataIC50:  7nMAssay 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
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Astrazeneca R&D Boston

Curated by ChEMBL
LigandPNGBDBM50325162(5-methyl-8-(3-(piperazin-1-ylmethyl)phenyl)-[1,2,4...)
Affinity DataIC50:  7nMAssay Description:Inhibition of His6-CHK1 expressed in baculovirus infected Sf9 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Astrazeneca R&D Boston

Curated by ChEMBL
LigandPNGBDBM50243258((S)-1-(5-phenyl-3-(piperidin-3-ylcarbamoyl)thiophe...)
Affinity DataIC50:  7nMAssay Description:Inhibition of Chk1More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Astrazeneca R&D Boston

Curated by ChEMBL
LigandPNGBDBM50243147((S)-1-(5-(4-acetylphenyl)-3-(piperidin-3-ylcarbamo...)
Affinity DataIC50:  7nMAssay Description:Inhibition of Chk1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Astrazeneca R&D Boston

Curated by ChEMBL
LigandPNGBDBM50389804(CHEMBL2070716)
Affinity DataIC50:  7nMAssay Description:Inhibition of human recombinant CHK1 expressed in insect cells using biotinylaminohexanoyl-KKVSRSGLYRSPMPENLNRPR as substrate after 2 hrs by scintill...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Astrazeneca R&D Boston

Curated by ChEMBL
LigandPNGBDBM50242821((S)-1-(5-(4-hydroxyphenyl)-3-(piperidin-3-ylcarbam...)
Affinity DataIC50:  7nMAssay Description:Inhibition of Chk1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Astrazeneca R&D Boston

Curated by ChEMBL
LigandPNGBDBM50243258((S)-1-(5-phenyl-3-(piperidin-3-ylcarbamoyl)thiophe...)
Affinity DataIC50:  7nMAssay Description:Inhibition of Chk1More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Astrazeneca R&D Boston

Curated by ChEMBL
LigandPNGBDBM50243258((S)-1-(5-phenyl-3-(piperidin-3-ylcarbamoyl)thiophe...)
Affinity DataIC50:  7nMAssay Description:Inhibition of human recombinant CHK1 expressed in insect cells using biotinylaminohexanoyl-KKVSRSGLYRSPMPENLNRPR as substrate after 2 hrs by scintill...More data for this Ligand-Target Pair
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