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Assay Detail

CHEMBL4844059

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Binding
Inhibition of PARP-2 (unknown origin)
4
Total Activities
4
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 2 (CHEMBL5366)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Novel Apigenin-Piperazine Hybrids as Potent and Selective Poly (ADP-Ribose) Polymerase-1 (PARP-1) Inhibitors for the Treatment of Cancer.
Long H, Hu X, Wang B, Wang Q, Wang R, Liu S, Xiong F, Jiang Z, Zhang XQ, Ye WC, Wang H.
J Med Chem (2021) 64 : 12089 -12108
PubMed 34404206 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 4.70 4.99
Kd 1 5.85 5.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3606021 1 5.85
CHEMBL63354 AMENTOFLAVONE 1 4.99
CHEMBL4303397 1 4.40
CHEMBL4799284 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3606021 Kd = 1400.0 nM 5.85
CHEMBL63354 AMENTOFLAVONE IC50 = 10300.0 nM 4.99
CHEMBL4303397 IC50 = 40000.0 nM 4.40
CHEMBL4799284 IC50 > 1000.0 nM -