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Assay Detail

CHEMBL4380268

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

Binding
Inhibition of recombinant human PARP1 using histone as substrate after 1 hr in presence of biotinylated NAD+ by ELISA
19
Total Activities
19
Compounds Tested
1
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

Discovery of Novel Dual Poly(ADP-ribose)polymerase and Phosphoinositide 3-Kinase Inhibitors as a Promising Strategy for Cancer Therapy.
Wang J, Li H, He G, Chu Z, Peng K, Ge Y, Zhu Q, Xu Y.
J Med Chem (2020) 63 : 122 -139
PubMed 31846325 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 8.71 9.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4461392 1 9.36
CHEMBL4437593 1 9.19
CHEMBL4549595 1 9.17
CHEMBL4525998 1 9.16
CHEMBL4436980 1 9.14
CHEMBL4461382 1 9.08
CHEMBL4571423 1 9.08
CHEMBL4551779 1 8.97
CHEMBL4436366 1 8.96
CHEMBL4446789 1 8.95
CHEMBL4438927 1 8.93
CHEMBL4438741 1 8.59
CHEMBL4593274 1 8.31
CHEMBL521686 OLAPARIB 4.0 1 8.30
CHEMBL4470724 1 8.22
CHEMBL4531016 1 8.21
CHEMBL4551630 1 8.10
CHEMBL4541731 1 8.02
CHEMBL4465869 1 7.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4461392 IC50 = 0.4365 nM 9.36
CHEMBL4437593 IC50 = 0.6457 nM 9.19
CHEMBL4549595 IC50 = 0.6761 nM 9.17
CHEMBL4525998 IC50 = 0.6918 nM 9.16
CHEMBL4436980 IC50 = 0.7244 nM 9.14
CHEMBL4461382 IC50 = 0.8318 nM 9.08
CHEMBL4571423 IC50 = 0.8318 nM 9.08
CHEMBL4551779 IC50 = 1.072 nM 8.97
CHEMBL4436366 IC50 = 1.096 nM 8.96
CHEMBL4446789 IC50 = 1.122 nM 8.95
CHEMBL4438927 IC50 = 1.175 nM 8.93
CHEMBL4438741 IC50 = 2.57 nM 8.59
CHEMBL4593274 IC50 = 4.898 nM 8.31
CHEMBL521686 OLAPARIB IC50 = 5.012 nM 8.30
CHEMBL4470724 IC50 = 6.026 nM 8.22
CHEMBL4531016 IC50 = 6.166 nM 8.21
CHEMBL4551630 IC50 = 7.943 nM 8.10
CHEMBL4541731 IC50 = 9.55 nM 8.02
CHEMBL4465869 IC50 = 15.49 nM 7.81