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Assay Detail

CHEMBL2390489

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Binding
Inhibition of wild type IDH1 (unknown origin) expressed in Escherichia coli BL21 using alpha-ketoglutarate as substrate incubated for 5 mins prior to substrate addition measured every 30 secs
6
Total Activities
6
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

Crystallographic Investigation and Selective Inhibition of Mutant Isocitrate Dehydrogenase.
Zheng B, Yao Y, Liu Z, Deng L, Anglin JL, Jiang H, Prasad BV, Song Y.
ACS Med Chem Lett (2013) 4 : 542 -546
PubMed 23795241 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 4.85 4.91

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2386126 1 4.91
CHEMBL2386127 1 4.78
CHEMBL2386130 1 -
CHEMBL2386129 1 -
CHEMBL2386128 1 -
CHEMBL2386125 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2386126 Ki = 12300.0 nM 4.91
CHEMBL2386127 Ki = 16800.0 nM 4.78
CHEMBL2386130 Ki > 50000.0 nM -
CHEMBL2386129 Ki > 50000.0 nM -
CHEMBL2386128 Ki > 50000.0 nM -
CHEMBL2386125 Ki > 50000.0 nM -