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Assay Detail

CHEMBL4432791

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

Binding
Inhibition of PARP-2 (unknown origin) after 1 hr in presence of NAD+/biotinylated NAD+/slDNA by ELISA
23
Total Activities
23
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 2 (CHEMBL5366)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel tricyclic poly (ADP-ribose) polymerase-1/2 inhibitors with potent anticancer chemopotentiating activity: Design, synthesis and biological evaluation.
Li H, Hu Y, Wang X, He G, Xu Y, Zhu Q.
Bioorg Med Chem (2016) 24 : 4731 -4740
PubMed 27561983 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 8.28 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL506871 VELIPARIB 3.0 1 8.89
CHEMBL4522170 1 8.26
CHEMBL4458889 1 8.14
CHEMBL4435879 1 8.11
CHEMBL4460350 1 8.00
CHEMBL4592544 1 -
CHEMBL4570886 1 -
CHEMBL4458372 1 -
CHEMBL4468323 1 -
CHEMBL4436157 1 -
CHEMBL4532640 1 -
CHEMBL4578024 1 -
CHEMBL4586369 1 -
CHEMBL4515565 1 -
CHEMBL4454541 1 -
CHEMBL4463611 1 -
CHEMBL4590570 1 -
CHEMBL4447860 1 -
CHEMBL4454690 1 -
CHEMBL4459573 1 -
CHEMBL4545981 1 -
CHEMBL4563153 1 -
CHEMBL4579910 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL506871 VELIPARIB IC50 = 1.3 nM 8.89
CHEMBL4522170 IC50 = 5.5 nM 8.26
CHEMBL4458889 IC50 = 7.2 nM 8.14
CHEMBL4435879 IC50 = 7.7 nM 8.11
CHEMBL4460350 IC50 = 9.9 nM 8.00
CHEMBL4592544 IC50 - -
CHEMBL4570886 IC50 - -
CHEMBL4458372 IC50 - -
CHEMBL4468323 IC50 - -
CHEMBL4436157 IC50 - -
CHEMBL4532640 IC50 - -
CHEMBL4578024 IC50 - -
CHEMBL4586369 IC50 - -
CHEMBL4515565 IC50 - -
CHEMBL4454541 IC50 - -
CHEMBL4463611 IC50 - -
CHEMBL4590570 IC50 - -
CHEMBL4447860 IC50 - -
CHEMBL4454690 IC50 - -
CHEMBL4459573 IC50 - -
CHEMBL4545981 IC50 - -
CHEMBL4563153 IC50 - -
CHEMBL4579910 IC50 - -