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Assay Detail

CHEMBL4257017

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

Binding
Inhibition of IDH1 R132C mutant (unknown origin) expressed in human U87MG cells assessed as reduction in 2-HG formation incubated for 48 hrs by LC-MS method
ChEMBL ↗
246
Total Activities
246
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

Therapeutically active compounds and their methods of use
(2016)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 246 7.15 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4293509 — — 1 7.30
CHEMBL4295139 — — 1 7.30
CHEMBL4281482 — — 1 7.30
CHEMBL4281625 — — 1 7.30
CHEMBL4289800 — — 1 7.30
CHEMBL4282694 — — 1 7.30
CHEMBL4288632 — — 1 7.30
CHEMBL4289797 — — 1 7.30
CHEMBL4285495 — — 1 7.30
CHEMBL4284814 — — 1 7.30
CHEMBL4288431 — — 1 7.30
CHEMBL4281900 — — 1 7.30
CHEMBL4279394 — — 1 7.30
CHEMBL4276680 — — 1 7.30
CHEMBL4294177 — — 1 7.30
CHEMBL4292494 — — 1 7.30
CHEMBL4277498 — — 1 7.30
CHEMBL4280325 — — 1 7.00
CHEMBL4281385 — — 1 7.00
CHEMBL4294387 — — 1 7.00
CHEMBL4293859 — — 1 7.00
CHEMBL4291957 — — 1 7.00
CHEMBL4294396 — — 1 7.00
CHEMBL4294983 — — 1 7.00
CHEMBL4291587 — — 1 7.00
CHEMBL4282071 — — 1 7.00
CHEMBL4289977 — — 1 7.00
CHEMBL4286718 — — 1 7.00
CHEMBL4284624 — — 1 7.00
CHEMBL4279012 — — 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4279394 — IC50 = 50.0 nM 7.30
CHEMBL4284814 — IC50 = 50.0 nM 7.30
CHEMBL4293509 — IC50 = 50.0 nM 7.30
CHEMBL4294177 — IC50 = 50.0 nM 7.30
CHEMBL4276680 — IC50 = 50.0 nM 7.30
CHEMBL4292494 — IC50 = 50.0 nM 7.30
CHEMBL4281900 — IC50 = 50.0 nM 7.30
CHEMBL4288431 — IC50 = 50.0 nM 7.30
CHEMBL4277498 — IC50 = 50.0 nM 7.30
CHEMBL4289797 — IC50 = 50.0 nM 7.30
CHEMBL4295139 — IC50 = 50.0 nM 7.30
CHEMBL4281482 — IC50 = 50.0 nM 7.30
CHEMBL4281625 — IC50 = 50.0 nM 7.30
CHEMBL4289800 — IC50 = 50.0 nM 7.30
CHEMBL4282694 — IC50 = 50.0 nM 7.30
CHEMBL4288632 — IC50 = 50.0 nM 7.30
CHEMBL4285495 — IC50 = 50.0 nM 7.30
CHEMBL4285024 — IC50 = 100.0 nM 7.00
CHEMBL4289977 — IC50 = 100.0 nM 7.00
CHEMBL4283760 — IC50 = 100.0 nM 7.00
CHEMBL4279012 — IC50 = 100.0 nM 7.00
CHEMBL4282071 — IC50 = 100.0 nM 7.00
CHEMBL4292065 — IC50 = 100.0 nM 7.00
CHEMBL4291587 — IC50 = 100.0 nM 7.00
CHEMBL4284624 — IC50 = 100.0 nM 7.00
CHEMBL4294544 — IC50 = 100.0 nM 7.00
CHEMBL4291957 — IC50 = 100.0 nM 7.00
CHEMBL4286718 — IC50 = 100.0 nM 7.00
CHEMBL4280325 — IC50 = 100.0 nM 7.00
CHEMBL4293859 — IC50 = 100.0 nM 7.00
CHEMBL4294387 — IC50 = 100.0 nM 7.00
CHEMBL4281385 — IC50 = 100.0 nM 7.00
CHEMBL4294983 — IC50 = 100.0 nM 7.00
CHEMBL4294396 — IC50 = 100.0 nM 7.00
CHEMBL4277108 — IC50 < 50.0 nM -
CHEMBL4277173 — IC50 < 50.0 nM -
CHEMBL4282325 — IC50 < 50.0 nM -
CHEMBL4277087 — IC50 < 50.0 nM -
CHEMBL4278576 — IC50 < 50.0 nM -
CHEMBL4287227 — IC50 < 50.0 nM -
CHEMBL4286181 — IC50 < 50.0 nM -
CHEMBL4281016 — IC50 < 50.0 nM -
CHEMBL4294595 — IC50 < 50.0 nM -
CHEMBL4280159 — IC50 < 50.0 nM -
CHEMBL4282925 — IC50 < 50.0 nM -
CHEMBL4278189 — IC50 < 50.0 nM -
CHEMBL4289705 — IC50 < 50.0 nM -
CHEMBL4286920 — IC50 < 50.0 nM -
CHEMBL4294406 — IC50 < 50.0 nM -
CHEMBL4284203 — IC50 < 50.0 nM -