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Assay Detail

CHEMBL763195

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

Binding
Binding affinity towards human poly(ADP-ribose) polymerase-1 (PARP-1)
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Poly [ADP-ribose] polymerase 1 (CHEMBL3105)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potentiation of cytotoxic drug activity in human tumour cell lines, by amine-substituted 2-arylbenzimidazole-4-carboxamide PARP-1 inhibitors.
White AW, Curtin NJ, Eastman BW, Golding BT, Hostomsky Z, Kyle S, Li J, Maegley KA, Skalitzky DJ, Webber SE, Yu XH, Griffin RJ.
Bioorg Med Chem Lett (2004) 14 : 2433 -2437
PubMed 15109627 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 7.84 8.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL83916 1 8.49
CHEMBL81125 1 8.35
CHEMBL79218 1 8.35
CHEMBL82434 1 8.25
CHEMBL83971 1 8.23
CHEMBL312135 1 8.23
CHEMBL419475 1 8.14
CHEMBL81831 1 8.06
CHEMBL312719 1 8.01
CHEMBL81077 1 7.99
CHEMBL84328 1 7.93
CHEMBL432166 1 7.92
CHEMBL81723 1 7.82
CHEMBL443798 1 7.51
CHEMBL81143 1 6.57
CHEMBL81977 3-AMINOBENZAMIDE 1 5.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL83916 Ki = 3.2 nM 8.49
CHEMBL81125 Ki = 4.5 nM 8.35
CHEMBL79218 Ki = 4.5 nM 8.35
CHEMBL82434 Ki = 5.6 nM 8.25
CHEMBL83971 Ki = 5.9 nM 8.23
CHEMBL312135 Ki = 5.9 nM 8.23
CHEMBL419475 Ki = 7.2 nM 8.14
CHEMBL81831 Ki = 8.7 nM 8.06
CHEMBL312719 Ki = 9.8 nM 8.01
CHEMBL81077 Ki = 10.2 nM 7.99
CHEMBL84328 Ki = 11.7 nM 7.93
CHEMBL432166 Ki = 12.0 nM 7.92
CHEMBL81723 Ki = 15.0 nM 7.82
CHEMBL443798 Ki = 31.0 nM 7.51
CHEMBL81143 Ki = 272.0 nM 6.57
CHEMBL81977 3-AMINOBENZAMIDE Ki = 3100.0 nM 5.51