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Assay Detail

CHEMBL4257015

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

Binding
Inhibition of IDH2 R140Q mutant homodimer (unknown origin) expressed in Sf9 cells pre-incubated for 6 hrs before addition of alpha-KG followed by 60 mins incubation in presence of NADPH, NADP, diaphorase and resazurin by fluorescence spectrometry based cofactor depletion assay
32
Total Activities
32
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], mitochondrial (CHEMBL3991501)
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 32 7.13 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4278435 1 7.30
CHEMBL4277108 1 7.30
CHEMBL4284203 1 7.30
CHEMBL4282925 1 7.30
CHEMBL4286667 1 7.30
CHEMBL4281594 1 7.30
CHEMBL4290554 1 7.30
CHEMBL4285495 1 7.30
CHEMBL4278414 1 7.00
CHEMBL4286947 1 7.00
CHEMBL4294899 1 7.00
CHEMBL4288016 1 7.00
CHEMBL4292464 1 7.00
CHEMBL4283985 1 7.00
CHEMBL4285110 1 7.00
CHEMBL4284068 1 7.00
CHEMBL4277506 1 7.00
CHEMBL4278807 1 7.00
CHEMBL4287037 1 -
CHEMBL4290450 1 -
CHEMBL4288655 1 -
CHEMBL4289486 1 -
CHEMBL4280213 1 -
CHEMBL4281221 1 -
CHEMBL4277498 1 -
CHEMBL4294615 1 -
CHEMBL4282989 1 -
CHEMBL4282906 1 -
CHEMBL4291028 1 -
CHEMBL4292328 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4278435 IC50 = 50.0 nM 7.30
CHEMBL4277108 IC50 = 50.0 nM 7.30
CHEMBL4284203 IC50 = 50.0 nM 7.30
CHEMBL4282925 IC50 = 50.0 nM 7.30
CHEMBL4286667 IC50 = 50.0 nM 7.30
CHEMBL4281594 IC50 = 50.0 nM 7.30
CHEMBL4290554 IC50 = 50.0 nM 7.30
CHEMBL4285495 IC50 = 50.0 nM 7.30
CHEMBL4294899 IC50 = 100.0 nM 7.00
CHEMBL4286947 IC50 = 100.0 nM 7.00
CHEMBL4278414 IC50 = 100.0 nM 7.00
CHEMBL4288016 IC50 = 100.0 nM 7.00
CHEMBL4292464 IC50 = 100.0 nM 7.00
CHEMBL4283985 IC50 = 100.0 nM 7.00
CHEMBL4285110 IC50 = 100.0 nM 7.00
CHEMBL4284068 IC50 = 100.0 nM 7.00
CHEMBL4277506 IC50 = 100.0 nM 7.00
CHEMBL4278807 IC50 = 100.0 nM 7.00
CHEMBL4280132 IC50 < 50.0 nM -
CHEMBL4283138 IC50 < 50.0 nM -
CHEMBL4287037 IC50 < 50.0 nM -
CHEMBL4290450 IC50 < 50.0 nM -
CHEMBL4288655 IC50 < 50.0 nM -
CHEMBL4289486 IC50 < 50.0 nM -
CHEMBL4280213 IC50 < 50.0 nM -
CHEMBL4281221 IC50 < 50.0 nM -
CHEMBL4277498 IC50 < 50.0 nM -
CHEMBL4294615 IC50 < 50.0 nM -
CHEMBL4282989 IC50 < 50.0 nM -
CHEMBL4282906 IC50 < 50.0 nM -
CHEMBL4291028 IC50 < 50.0 nM -
CHEMBL4292328 IC50 >= 1000.0 nM -