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Assay Detail

CHEMBL759581

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

Binding
In vitro inhibition against human full length PARP protein
34
Total Activities
34
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

Resistance-modifying agents. 9. Synthesis and biological properties of benzimidazole inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase.
White AW, Almassy R, Calvert AH, Curtin NJ, Griffin RJ, Hostomsky Z, Maegley K, Newell DR, Srinivasan S, Golding BT.
J Med Chem (2000) 43 : 4084 -4097
PubMed 11063605 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 34 7.69 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL334734 1 8.92
CHEMBL133241 1 8.80
CHEMBL338923 1 8.70
CHEMBL131891 1 8.52
CHEMBL335993 1 8.40
CHEMBL133343 1 8.27
CHEMBL334357 1 8.24
CHEMBL337386 1 8.23
CHEMBL134022 1 8.22
CHEMBL131719 1 8.22
CHEMBL336070 1 8.20
CHEMBL337254 1 8.17
CHEMBL131820 1 8.17
CHEMBL335516 1 8.10
CHEMBL133855 1 8.09
CHEMBL132947 1 8.08
CHEMBL133353 1 8.05
CHEMBL335226 1 8.03
CHEMBL134116 1 8.03
CHEMBL133275 1 7.97
CHEMBL134197 1 7.96
CHEMBL133976 1 7.89
CHEMBL81723 1 7.82
CHEMBL131737 1 7.50
CHEMBL341427 1 7.07
CHEMBL133694 1 7.02
CHEMBL121765 1 7.00
CHEMBL423343 1 6.90
CHEMBL132834 1 6.87
CHEMBL334603 1 6.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL334734 Ki = 1.2 nM 8.92
CHEMBL133241 Ki = 1.6 nM 8.80
CHEMBL338923 Ki = 2.0 nM 8.70
CHEMBL131891 Ki = 3.0 nM 8.52
CHEMBL335993 Ki = 4.0 nM 8.40
CHEMBL133343 Ki = 5.4 nM 8.27
CHEMBL334357 Ki = 5.8 nM 8.24
CHEMBL337386 Ki = 5.9 nM 8.23
CHEMBL134022 Ki = 6.0 nM 8.22
CHEMBL131719 Ki = 6.0 nM 8.22
CHEMBL336070 Ki = 6.3 nM 8.20
CHEMBL337254 Ki = 6.8 nM 8.17
CHEMBL131820 Ki = 6.8 nM 8.17
CHEMBL335516 Ki = 8.0 nM 8.10
CHEMBL133855 Ki = 8.1 nM 8.09
CHEMBL132947 Ki = 8.4 nM 8.08
CHEMBL133353 Ki = 9.0 nM 8.05
CHEMBL335226 Ki = 9.4 nM 8.03
CHEMBL134116 Ki = 9.4 nM 8.03
CHEMBL133275 Ki = 10.6 nM 7.97
CHEMBL134197 Ki = 11.0 nM 7.96
CHEMBL133976 Ki = 13.0 nM 7.89
CHEMBL81723 Ki = 15.0 nM 7.82
CHEMBL131737 Ki = 32.0 nM 7.50
CHEMBL341427 Ki = 85.0 nM 7.07
CHEMBL133694 Ki = 95.0 nM 7.02
CHEMBL121765 Ki = 99.0 nM 7.00
CHEMBL423343 Ki = 126.0 nM 6.90
CHEMBL132834 Ki = 136.0 nM 6.87
CHEMBL334603 Ki = 190.0 nM 6.72
CHEMBL335198 Ki = 290.0 nM 6.54
CHEMBL133096 Ki = 350.0 nM 6.46
CHEMBL338955 Ki = 530.0 nM 6.28
CHEMBL336859 Ki = 100000.0 nM 4.00