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Assay Detail

CHEMBL4256244

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Binding
Inhibition of wild type IDH1/IDH1 R132H mutant heterodimer (unknown origin) after 16 hrs in presence of NADPH by diaphorase/resazurin coupled fluorescence assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Isocitrate dehydrogenase [NADP] cytoplasmic (CHEMBL2007625)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1 Mutant Cancers.
Popovici-Muller J, Lemieux RM, Artin E, Saunders JO, Salituro FG, Travins J, Cianchetta G, Cai Z, Zhou D, Cui D, Chen P, Straley K, Tobin E, Wang F, David MD, Penard-Lacronique V, Quivoron C, Saada V, de Botton S, Gross S, Dang L, Yang H, Utley L, Chen Y, Kim H, Jin S, Gu Z, Yao G, Luo Z, Lv X, Fang C, Yan L, Olaharski A, Silverman L, Biller S, Su SM, Yen K.
ACS Med Chem Lett (2018) 9 : 300 -305
PubMed 29670690 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.30 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4282663 1 8.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4282663 IC50 = 5.0 nM 8.30