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Assay Detail

CHEMBL4257009

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

Binding
Inhibition of DH1 R132H mutant homodimer (unknown origin) expressed in Sf9 cells pre-incubated for 1 hr before addition of alpha-KG followed by 90 mins incubation in presence of NADPH, NADP, diaphorase and resazurin by fluorescence spectrometry
ChEMBL ↗
59
Total Activities
59
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 59 7.17 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4287525 — — 1 7.30
CHEMBL4282861 — — 1 7.30
CHEMBL4284907 — — 1 7.30
CHEMBL4282086 — — 1 7.30
CHEMBL4283130 — — 1 7.30
CHEMBL4281163 — — 1 7.30
CHEMBL4277726 — — 1 7.30
CHEMBL4291180 — — 1 7.30
CHEMBL4288840 — — 1 7.30
CHEMBL4289876 — — 1 7.30
CHEMBL4288448 — — 1 7.30
CHEMBL4283396 — — 1 7.30
CHEMBL4292196 — — 1 7.30
CHEMBL4291634 — — 1 7.30
CHEMBL4287161 — — 1 7.30
CHEMBL4293942 — — 1 7.30
CHEMBL4292892 — — 1 7.00
CHEMBL4287094 — — 1 7.00
CHEMBL4293316 — — 1 7.00
CHEMBL4281641 — — 1 7.00
CHEMBL4287998 — — 1 7.00
CHEMBL4286947 — — 1 7.00
CHEMBL4286585 — — 1 7.00
CHEMBL4282906 — — 1 7.00
CHEMBL4279452 — — 1 7.00
CHEMBL4289215 — — 1 7.00
CHEMBL4295139 — — 1 7.00
CHEMBL4281837 — — 1 7.00
CHEMBL4279901 — — 1 -
CHEMBL4290152 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4287525 — IC50 = 50.0 nM 7.30
CHEMBL4287161 — IC50 = 50.0 nM 7.30
CHEMBL4282861 — IC50 = 50.0 nM 7.30
CHEMBL4284907 — IC50 = 50.0 nM 7.30
CHEMBL4282086 — IC50 = 50.0 nM 7.30
CHEMBL4283130 — IC50 = 50.0 nM 7.30
CHEMBL4281163 — IC50 = 50.0 nM 7.30
CHEMBL4277726 — IC50 = 50.0 nM 7.30
CHEMBL4291180 — IC50 = 50.0 nM 7.30
CHEMBL4293942 — IC50 = 50.0 nM 7.30
CHEMBL4288840 — IC50 = 50.0 nM 7.30
CHEMBL4289876 — IC50 = 50.0 nM 7.30
CHEMBL4288448 — IC50 = 50.0 nM 7.30
CHEMBL4283396 — IC50 = 50.0 nM 7.30
CHEMBL4292196 — IC50 = 50.0 nM 7.30
CHEMBL4291634 — IC50 = 50.0 nM 7.30
CHEMBL4287094 — IC50 = 100.0 nM 7.00
CHEMBL4293316 — IC50 = 100.0 nM 7.00
CHEMBL4281641 — IC50 = 100.0 nM 7.00
CHEMBL4287998 — IC50 = 100.0 nM 7.00
CHEMBL4286947 — IC50 = 100.0 nM 7.00
CHEMBL4286585 — IC50 = 100.0 nM 7.00
CHEMBL4279452 — IC50 = 100.0 nM 7.00
CHEMBL4292892 — IC50 = 100.0 nM 7.00
CHEMBL4289215 — IC50 = 100.0 nM 7.00
CHEMBL4295139 — IC50 = 100.0 nM 7.00
CHEMBL4281837 — IC50 = 100.0 nM 7.00
CHEMBL4282906 — IC50 = 100.0 nM 7.00
CHEMBL4283896 — IC50 >= 1000.0 nM -
CHEMBL4284394 — IC50 < 50.0 nM -
CHEMBL4278828 — IC50 < 50.0 nM -
CHEMBL4292065 — IC50 >= 1000.0 nM -
CHEMBL4292293 — IC50 >= 1000.0 nM -
CHEMBL4294559 — IC50 >= 1000.0 nM -
CHEMBL4282029 — IC50 >= 1000.0 nM -
CHEMBL4285713 — IC50 < 50.0 nM -
CHEMBL4295085 — IC50 < 50.0 nM -
CHEMBL4295153 — IC50 >= 1000.0 nM -
CHEMBL4290056 — IC50 >= 1000.0 nM -
CHEMBL4286059 — IC50 >= 1000.0 nM -
CHEMBL4282686 — IC50 >= 1000.0 nM -
CHEMBL4280581 — IC50 >= 1000.0 nM -
CHEMBL4278831 — IC50 < 50.0 nM -
CHEMBL4287607 — IC50 >= 1000.0 nM -
CHEMBL4293309 — IC50 >= 1000.0 nM -
CHEMBL4292928 — IC50 >= 1000.0 nM -
CHEMBL4294956 — IC50 >= 1000.0 nM -
CHEMBL4278420 — IC50 < 50.0 nM -
CHEMBL4290152 — IC50 - — -
CHEMBL4279901 — IC50 >= 1000.0 nM -