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Assay Detail

CHEMBL4481004

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

Binding
Inhibition of PARP1 (unknown origin)
7
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Medicinal chemistry approaches of poly ADP-Ribose polymerase 1 (PARP1) inhibitors as anticancer agents - A recent update.
Jain PG, Patel BD.
Eur J Med Chem (2019) 165 : 198 -215
PubMed 30684797 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.48 8.42
Ki 3 7.04 8.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1094636 NIRAPARIB 4.0 2 8.49
CHEMBL4569989 1 8.00
CHEMBL123904 1 7.32
CHEMBL4521985 1 7.10
CHEMBL125200 1 6.38
CHEMBL81977 3-AMINOBENZAMIDE 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1094636 NIRAPARIB Ki = 3.2 nM 8.49
CHEMBL1094636 NIRAPARIB IC50 = 3.8 nM 8.42
CHEMBL4569989 IC50 = 10.0 nM 8.00
CHEMBL123904 Ki = 48.0 nM 7.32
CHEMBL4521985 IC50 = 79.0 nM 7.10
CHEMBL125200 IC50 = 420.0 nM 6.38
CHEMBL81977 3-AMINOBENZAMIDE Ki = 5000.0 nM 5.30