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Assay Detail

CHEMBL4257014

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 1 hr before addition of alpha-KG followed by 16 hrs incubation in presence of NADPH, NADP, diaphorase and resazurin by fluorescence spectrometry based cofactor depletion assay
ChEMBL ↗
256
Total Activities
256
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 256 7.17 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4280581 — — 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
CHEMBL4277498 — — 1 7.30
CHEMBL4284814 — — 1 7.30
CHEMBL4288431 — — 1 7.30
CHEMBL4284624 — — 1 7.30
CHEMBL4281900 — — 1 7.30
CHEMBL4280463 — — 1 7.30
CHEMBL4292196 — — 1 7.30
CHEMBL4282029 — — 1 7.30
CHEMBL4290152 — — 1 7.30
CHEMBL4286718 — — 1 7.30
CHEMBL4283760 — — 1 7.00
CHEMBL4294544 — — 1 7.00
CHEMBL4285024 — — 1 7.00
CHEMBL4280325 — — 1 7.00
CHEMBL4281385 — — 1 7.00
CHEMBL4294387 — — 1 7.00
CHEMBL4293859 — — 1 7.00
CHEMBL4291957 — — 1 7.00
CHEMBL4294396 — — 1 7.00
CHEMBL4290554 — — 1 7.00
CHEMBL4294615 — — 1 7.00
CHEMBL4282071 — — 1 7.00
CHEMBL4289977 — — 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4282694 — IC50 = 50.0 nM 7.30
CHEMBL4281625 — IC50 = 50.0 nM 7.30
CHEMBL4277498 — IC50 = 50.0 nM 7.30
CHEMBL4288431 — IC50 = 50.0 nM 7.30
CHEMBL4286718 — IC50 = 50.0 nM 7.30
CHEMBL4284624 — IC50 = 50.0 nM 7.30
CHEMBL4285495 — IC50 = 50.0 nM 7.30
CHEMBL4280463 — IC50 = 50.0 nM 7.30
CHEMBL4289797 — IC50 = 50.0 nM 7.30
CHEMBL4292196 — IC50 = 50.0 nM 7.30
CHEMBL4289800 — IC50 = 50.0 nM 7.30
CHEMBL4288632 — IC50 = 50.0 nM 7.30
CHEMBL4284814 — IC50 = 50.0 nM 7.30
CHEMBL4282029 — IC50 = 50.0 nM 7.30
CHEMBL4280581 — IC50 = 50.0 nM 7.30
CHEMBL4290152 — IC50 = 50.0 nM 7.30
CHEMBL4281900 — IC50 = 50.0 nM 7.30
CHEMBL4282071 — IC50 = 100.0 nM 7.00
CHEMBL4289977 — IC50 = 100.0 nM 7.00
CHEMBL4294615 — IC50 = 100.0 nM 7.00
CHEMBL4290554 — IC50 = 100.0 nM 7.00
CHEMBL4294396 — IC50 = 100.0 nM 7.00
CHEMBL4291957 — IC50 = 100.0 nM 7.00
CHEMBL4294387 — IC50 = 100.0 nM 7.00
CHEMBL4281385 — IC50 = 100.0 nM 7.00
CHEMBL4280325 — IC50 = 100.0 nM 7.00
CHEMBL4285024 — IC50 = 100.0 nM 7.00
CHEMBL4294544 — IC50 = 100.0 nM 7.00
CHEMBL4283760 — IC50 = 100.0 nM 7.00
CHEMBL4293859 — IC50 = 100.0 nM 7.00
CHEMBL4289777 — IC50 < 50.0 nM -
CHEMBL4287992 — IC50 < 50.0 nM -
CHEMBL4290807 — IC50 < 50.0 nM -
CHEMBL4284203 — IC50 < 50.0 nM -
CHEMBL4290997 — IC50 < 50.0 nM -
CHEMBL4282925 — IC50 < 50.0 nM -
CHEMBL4295099 — IC50 < 50.0 nM -
CHEMBL4291368 — IC50 < 50.0 nM -
CHEMBL4293274 — IC50 >= 1000.0 nM -
CHEMBL4276898 — IC50 < 50.0 nM -
CHEMBL4294886 — IC50 < 50.0 nM -
CHEMBL4277108 — IC50 < 50.0 nM -
CHEMBL4280159 — IC50 < 50.0 nM -
CHEMBL4287227 — IC50 < 50.0 nM -
CHEMBL4286181 — IC50 < 50.0 nM -
CHEMBL4294595 — IC50 < 50.0 nM -
CHEMBL4277087 — IC50 < 50.0 nM -
CHEMBL4291112 — IC50 < 50.0 nM -
CHEMBL4289616 — IC50 < 50.0 nM -
CHEMBL4290818 — IC50 >= 1000.0 nM -