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Assay Detail

CHEMBL4325713

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
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 high-throughput mass spectrometric 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 Autocuration

Target

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

Publication

Structure-Based Design and Identification of FT-2102 (Olutasidenib), a Potent Mutant-Selective IDH1 Inhibitor.
Caravella JA, Lin J, Diebold RB, Campbell AM, Ericsson A, Gustafson G, Wang Z, Castro J, Clarke A, Gotur D, Josephine HR, Katz M, Kershaw M, Yao L, Toms AV, Barr KJ, Dinsmore CJ, Walker D, Ashwell S, Lu W.
J Med Chem (2020) 63 : 1612 -1623
PubMed 31971798 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.22 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4297610 OLUTASIDENIB 4.0 1 8.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4297610 OLUTASIDENIB IC50 = 6.0 nM 8.22