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Assay Detail

CHEMBL4257007

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

Binding
Inhibition of His-tagged wild type IDH1 (unknown origin)/FLAG-tagged IDH1 R132H mutant heterodimer expressed in Sf9 cells pre-incubated for 1 hr before addition of alpha-KG followed by diaphorase and resazurin addition and measured after 5 mins in presence of NADPH and 30 uM NADP ny fluorescence spectrometry
ChEMBL ↗
258
Total Activities
258
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 258 7.08 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4280113 — — 1 7.30
CHEMBL4291028 — — 1 7.30
CHEMBL4280042 — — 1 7.30
CHEMBL4293552 — — 1 7.30
CHEMBL4287992 — — 1 7.30
CHEMBL4294983 — — 1 7.30
CHEMBL4290554 — — 1 7.30
CHEMBL4291587 — — 1 7.30
CHEMBL4294615 — — 1 7.30
CHEMBL4279333 — — 1 7.30
CHEMBL4281221 — — 1 7.30
CHEMBL4281594 — — 1 7.30
CHEMBL4282632 — — 1 7.30
CHEMBL4285688 — — 1 7.30
CHEMBL4282686 — — 1 7.30
CHEMBL4292856 — — 1 7.30
CHEMBL4280488 — — 1 7.30
CHEMBL4282969 — — 1 7.30
CHEMBL4277498 — — 1 7.30
CHEMBL4283985 — — 1 7.00
CHEMBL4278807 — — 1 7.00
CHEMBL4279855 — — 1 7.00
CHEMBL4285080 — — 1 7.00
CHEMBL4281357 — — 1 7.00
CHEMBL4289397 — — 1 7.00
CHEMBL4288364 — — 1 7.00
CHEMBL4293462 — — 1 7.00
CHEMBL4292464 — — 1 7.00
CHEMBL4287154 — — 1 7.00
CHEMBL4284019 — — 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4279333 — IC50 = 50.0 nM 7.30
CHEMBL4277498 — IC50 = 50.0 nM 7.30
CHEMBL4285688 — IC50 = 50.0 nM 7.30
CHEMBL4282632 — IC50 = 50.0 nM 7.30
CHEMBL4281594 — IC50 = 50.0 nM 7.30
CHEMBL4281221 — IC50 = 50.0 nM 7.30
CHEMBL4282686 — IC50 = 50.0 nM 7.30
CHEMBL4292856 — IC50 = 50.0 nM 7.30
CHEMBL4280488 — IC50 = 50.0 nM 7.30
CHEMBL4280042 — IC50 = 50.0 nM 7.30
CHEMBL4287992 — IC50 = 50.0 nM 7.30
CHEMBL4294983 — IC50 = 50.0 nM 7.30
CHEMBL4280113 — IC50 = 50.0 nM 7.30
CHEMBL4290554 — IC50 = 50.0 nM 7.30
CHEMBL4291587 — IC50 = 50.0 nM 7.30
CHEMBL4294615 — IC50 = 50.0 nM 7.30
CHEMBL4282969 — IC50 = 50.0 nM 7.30
CHEMBL4291028 — IC50 = 50.0 nM 7.30
CHEMBL4293552 — IC50 = 50.0 nM 7.30
CHEMBL4282936 — IC50 = 100.0 nM 7.00
CHEMBL4292464 — IC50 = 100.0 nM 7.00
CHEMBL4293462 — IC50 = 100.0 nM 7.00
CHEMBL4288364 — IC50 = 100.0 nM 7.00
CHEMBL4289397 — IC50 = 100.0 nM 7.00
CHEMBL4281357 — IC50 = 100.0 nM 7.00
CHEMBL4285080 — IC50 = 100.0 nM 7.00
CHEMBL4279855 — IC50 = 100.0 nM 7.00
CHEMBL4278807 — IC50 = 100.0 nM 7.00
CHEMBL4283985 — IC50 = 100.0 nM 7.00
CHEMBL4291957 — IC50 = 100.0 nM 7.00
CHEMBL4294396 — IC50 = 100.0 nM 7.00
CHEMBL4288016 — IC50 = 100.0 nM 7.00
CHEMBL4276904 — IC50 = 100.0 nM 7.00
CHEMBL4292328 — IC50 = 100.0 nM 7.00
CHEMBL4277835 — IC50 = 100.0 nM 7.00
CHEMBL4278869 — IC50 = 100.0 nM 7.00
CHEMBL4289797 — IC50 = 100.0 nM 7.00
CHEMBL4290818 — IC50 = 100.0 nM 7.00
CHEMBL4293859 — IC50 = 100.0 nM 7.00
CHEMBL4294899 — IC50 = 100.0 nM 7.00
CHEMBL4279934 — IC50 = 100.0 nM 7.00
CHEMBL4294774 — IC50 = 100.0 nM 7.00
CHEMBL4294387 — IC50 = 100.0 nM 7.00
CHEMBL4293353 — IC50 = 100.0 nM 7.00
CHEMBL4293274 — IC50 = 100.0 nM 7.00
CHEMBL4292259 — IC50 = 100.0 nM 7.00
CHEMBL4281385 — IC50 = 100.0 nM 7.00
CHEMBL4280325 — IC50 = 100.0 nM 7.00
CHEMBL4284594 — IC50 = 100.0 nM 7.00
CHEMBL4282925 — IC50 = 100.0 nM 7.00