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Assay Detail

CHEMBL4131015

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

Functional
Cytotoxicity against BRCA2 deficient Chinese hamster VC8 cells after 3 days by CCK8 or SRB assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cricetulus griseus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery, mechanism and metabolism studies of 2,3-difluorophenyl-linker-containing PARP1 inhibitors with enhanced in vivo efficacy for cancer therapy.
Chen W, Guo N, Qi M, Dai H, Hong M, Guan L, Huan X, Song S, He J, Wang Y, Xi Y, Yang X, Shen Y, Su Y, Sun Y, Gao Y, Chen Y, Ding J, Tang Y, Ren G, Miao Z, Li J.
Eur J Med Chem (2017) 138 : 514 -531
PubMed 28692916 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 6.58 8.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3137320 TALAZOPARIB 4.0 1 8.38
CHEMBL4169012 1 8.06
CHEMBL4175142 1 7.50
CHEMBL4162463 1 7.37
CHEMBL4174278 1 7.17
CHEMBL4169337 1 7.04
CHEMBL4159834 1 6.86
CHEMBL4172321 1 6.83
CHEMBL4171279 1 6.69
CHEMBL4165908 1 6.55
CHEMBL521686 OLAPARIB 4.0 1 6.25
CHEMBL4175790 1 6.21
CHEMBL4167044 1 6.03
CHEMBL4161687 1 6.01
CHEMBL4167934 1 5.80
CHEMBL4161414 1 5.71
CHEMBL4161087 1 5.68
CHEMBL4160023 1 5.48
CHEMBL4167280 1 5.40
CHEMBL4170665 1 -
CHEMBL4174093 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3137320 TALAZOPARIB IC50 = 4.2 nM 8.38
CHEMBL4169012 IC50 = 8.8 nM 8.06
CHEMBL4175142 IC50 = 31.7 nM 7.50
CHEMBL4162463 IC50 = 42.6 nM 7.37
CHEMBL4174278 IC50 = 68.1 nM 7.17
CHEMBL4169337 IC50 = 90.1 nM 7.04
CHEMBL4159834 IC50 = 136.7 nM 6.86
CHEMBL4172321 IC50 = 148.7 nM 6.83
CHEMBL4171279 IC50 = 206.0 nM 6.69
CHEMBL4165908 IC50 = 284.2 nM 6.55
CHEMBL521686 OLAPARIB IC50 = 565.6 nM 6.25
CHEMBL4175790 IC50 = 624.3 nM 6.21
CHEMBL4167044 IC50 = 937.8 nM 6.03
CHEMBL4161687 IC50 = 987.1 nM 6.01
CHEMBL4167934 IC50 = 1599.3 nM 5.80
CHEMBL4161414 IC50 = 1944.6 nM 5.71
CHEMBL4161087 IC50 = 2076.1 nM 5.68
CHEMBL4160023 IC50 = 3287.8 nM 5.48
CHEMBL4167280 IC50 = 3966.3 nM 5.40
CHEMBL4170665 IC50 < 3.2 nM -
CHEMBL4174093 IC50 = 0.003 nM -