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Assay Detail

CHEMBL5521717

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

Binding
Inhibition of PARP1 (unknown origin) using histone as substrate incubated for 45 mins by absorbance based analysis
16
Total Activities
16
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

Rational Design of PARP1/c-Met Dual Inhibitors for Overcoming PARP1 Inhibitor Resistance Induced by c-Met Overexpression.
Sun Z, Li L, Zhai B, Hu M, Huang L, Huang S, Ye L, Kong X, Xu J, Bai J, Yan J, Zhou Q, Hu Z, Zhang Y, Jiang Y, Zhang Y, Qiao Z, Zou Y, Xu Y, Zhu Q.
J Med Chem (2024) 67 : 4916 -4935
PubMed 38477575 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 8.37 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5562332 1 9.92
CHEMBL5566491 1 9.05
CHEMBL5550003 1 8.96
CHEMBL5567666 1 8.96
CHEMBL5542393 1 8.68
CHEMBL5567210 1 8.48
CHEMBL5561784 1 8.43
CHEMBL521686 OLAPARIB 4.0 1 8.37
CHEMBL5560815 1 8.33
CHEMBL5560235 1 8.24
CHEMBL5555264 1 8.15
CHEMBL5566081 1 8.14
CHEMBL5556439 1 7.49
CHEMBL5559117 1 7.38
CHEMBL5568564 1 7.04
CHEMBL5560130 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5562332 IC50 = 0.12 nM 9.92
CHEMBL5566491 IC50 = 0.9 nM 9.05
CHEMBL5550003 IC50 = 1.1 nM 8.96
CHEMBL5567666 IC50 = 1.1 nM 8.96
CHEMBL5542393 IC50 = 2.1 nM 8.68
CHEMBL5567210 IC50 = 3.3 nM 8.48
CHEMBL5561784 IC50 = 3.7 nM 8.43
CHEMBL521686 OLAPARIB IC50 = 4.3 nM 8.37
CHEMBL5560815 IC50 = 4.7 nM 8.33
CHEMBL5560235 IC50 = 5.8 nM 8.24
CHEMBL5555264 IC50 = 7.1 nM 8.15
CHEMBL5566081 IC50 = 7.3 nM 8.14
CHEMBL5556439 IC50 = 32.2 nM 7.49
CHEMBL5559117 IC50 = 42.0 nM 7.38
CHEMBL5568564 IC50 = 91.7 nM 7.04
CHEMBL5560130 IC50 > 1000.0 nM -