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Assay Detail

CHEMBL4678539

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Binding
Inhibition of PARP-1 in human HeLa cells incubated for 18 hrs in presence of H2O2
ChEMBL ↗
58
Total Activities
58
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HeLa
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 Pamiparib (BGB-290), a Potent and Selective Poly (ADP-ribose) Polymerase (PARP) Inhibitor in Clinical Development.
Wang H,Ren B,Liu Y,Jiang B,Guo Y,Wei M,Luo L,Kuang X,Qiu M,Lv L,Xu H,Qi R,Yan H,Xu D,Wang Z,Huo CX,Zhu Y,Zhao Y,Wu Y,Qin Z,Su D,Tang T,Wang F,Sun X,Feng Y,Peng H,Wang X,Gao Y,Liu Y,Gong W,Yu F,Liu X,Wang L,Zhou C
J Med Chem (2020) 63 : 15541 -15563
PubMed 33264017 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 58 8.02 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4112930 PAMIPARIB 3.0 1 9.70
CHEMBL521686 OLAPARIB 4.0 1 9.40
CHEMBL4776661 — — 1 9.30
CHEMBL4107982 — — 1 9.22
CHEMBL3931972 — — 1 8.89
CHEMBL3983859 — — 1 8.89
CHEMBL3908123 — — 1 8.85
CHEMBL3911687 — — 1 8.77
CHEMBL3905389 — — 1 8.72
CHEMBL3940569 — — 1 8.64
CHEMBL3929889 — — 1 8.62
CHEMBL3925115 — — 1 8.62
CHEMBL3910080 — — 1 8.57
CHEMBL3972156 — — 1 8.54
CHEMBL3905040 — — 1 8.54
CHEMBL3969742 — — 1 8.51
CHEMBL3984980 — — 1 8.49
CHEMBL3917078 — — 1 8.47
CHEMBL4784831 — — 1 8.46
CHEMBL3962648 — — 1 8.46
CHEMBL3891329 — — 1 8.44
CHEMBL3970252 — — 1 8.40
CHEMBL3908092 — — 1 8.37
CHEMBL3901638 — — 1 8.36
CHEMBL3901034 — — 1 8.32
CHEMBL3975917 — — 1 8.31
CHEMBL3907535 — — 1 8.30
CHEMBL3929705 — — 1 8.26
CHEMBL3922789 — — 1 8.17
CHEMBL3970120 — — 1 8.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4112930 PAMIPARIB EC50 = 0.2 nM 9.70
CHEMBL521686 OLAPARIB EC50 = 0.4 nM 9.40
CHEMBL4776661 — EC50 = 0.5 nM 9.30
CHEMBL4107982 — EC50 = 0.6 nM 9.22
CHEMBL3931972 — EC50 = 1.3 nM 8.89
CHEMBL3983859 — EC50 = 1.3 nM 8.89
CHEMBL3908123 — EC50 = 1.4 nM 8.85
CHEMBL3911687 — EC50 = 1.7 nM 8.77
CHEMBL3905389 — EC50 = 1.9 nM 8.72
CHEMBL3940569 — EC50 = 2.3 nM 8.64
CHEMBL3929889 — EC50 = 2.4 nM 8.62
CHEMBL3925115 — EC50 = 2.4 nM 8.62
CHEMBL3910080 — EC50 = 2.7 nM 8.57
CHEMBL3905040 — EC50 = 2.9 nM 8.54
CHEMBL3972156 — EC50 = 2.9 nM 8.54
CHEMBL3969742 — EC50 = 3.1 nM 8.51
CHEMBL3984980 — EC50 = 3.2 nM 8.49
CHEMBL3917078 — EC50 = 3.4 nM 8.47
CHEMBL4784831 — EC50 = 3.5 nM 8.46
CHEMBL3962648 — EC50 = 3.5 nM 8.46
CHEMBL3891329 — EC50 = 3.6 nM 8.44
CHEMBL3970252 — EC50 = 4.0 nM 8.40
CHEMBL3908092 — EC50 = 4.3 nM 8.37
CHEMBL3901638 — EC50 = 4.4 nM 8.36
CHEMBL3901034 — EC50 = 4.8 nM 8.32
CHEMBL3975917 — EC50 = 4.9 nM 8.31
CHEMBL3907535 — EC50 = 5.0 nM 8.30
CHEMBL3929705 — EC50 = 5.5 nM 8.26
CHEMBL3922789 — EC50 = 6.8 nM 8.17
CHEMBL3970120 — EC50 = 6.9 nM 8.16
CHEMBL3961684 — EC50 = 7.6 nM 8.12
CHEMBL3931542 — EC50 = 8.0 nM 8.10
CHEMBL3947623 — EC50 = 8.1 nM 8.09
CHEMBL4749300 — EC50 = 9.3 nM 8.03
CHEMBL4749094 — EC50 = 11.7 nM 7.93
CHEMBL3926240 — EC50 = 12.0 nM 7.92
CHEMBL3900548 — EC50 = 12.4 nM 7.91
CHEMBL3906623 — EC50 = 13.0 nM 7.89
CHEMBL3954603 — EC50 = 13.9 nM 7.86
CHEMBL3983342 — EC50 = 15.0 nM 7.82
CHEMBL4784468 — EC50 = 15.4 nM 7.81
CHEMBL4788782 — EC50 = 16.6 nM 7.78
CHEMBL4748572 — EC50 = 22.0 nM 7.66
CHEMBL3969049 — EC50 = 23.0 nM 7.64
CHEMBL4753364 — EC50 = 24.1 nM 7.62
CHEMBL3916191 — EC50 = 26.6 nM 7.58
CHEMBL3983247 — EC50 = 30.0 nM 7.52
CHEMBL3898162 — EC50 = 33.0 nM 7.48
CHEMBL3914932 — EC50 = 45.5 nM 7.34
CHEMBL4747486 — EC50 = 54.7 nM 7.26