Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5366416

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

Binding
Inhibition of PARP1 (unknown origin) using histone as substrate by ELISA
34
Total Activities
34
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

YCH1899, a Highly Effective Phthalazin-1(2<i>H</i>)-one Derivative That Overcomes Resistance to Prior PARP Inhibitors.
Sun Y, Yang H, Yuan J, Wang L, Song S, Chen R, Bao X, Jia L, Yang T, Zhang X, He Q, Gan Y, Miao Z, He J, Yang C.
J Med Chem (2023) 66 : 12284 -12303
PubMed 37605459 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 8.68 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5401127 1 10.70
CHEMBL5425729 1 9.77
CHEMBL5404605 1 9.64
CHEMBL5428376 1 9.62
CHEMBL5425393 1 9.59
CHEMBL5395197 1 9.36
CHEMBL5408163 1 9.13
CHEMBL5419303 1 9.07
CHEMBL5425070 1 9.02
CHEMBL5410501 1 9.02
CHEMBL5421957 1 9.01
CHEMBL5432616 1 8.90
CHEMBL5429957 1 8.89
CHEMBL5435418 1 8.87
CHEMBL3930624 FLUZOPARIB 3.0 1 8.84
CHEMBL5397203 1 8.72
CHEMBL5427132 1 8.67
CHEMBL5412306 1 8.63
CHEMBL5417924 1 8.25
CHEMBL5423216 1 8.21
CHEMBL5436154 1 8.20
CHEMBL521686 OLAPARIB 4.0 1 8.18
CHEMBL5436989 1 8.13
CHEMBL5433982 1 8.09
CHEMBL5427638 1 8.07
CHEMBL5422190 1 7.89
CHEMBL5438131 1 7.87
CHEMBL5436743 1 7.64
CHEMBL5416682 1 7.33
CHEMBL5437055 1 7.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5401127 IC50 = 0.02 nM 10.70
CHEMBL5425729 IC50 = 0.17 nM 9.77
CHEMBL5404605 IC50 = 0.23 nM 9.64
CHEMBL5428376 IC50 = 0.24 nM 9.62
CHEMBL5425393 IC50 = 0.26 nM 9.59
CHEMBL5395197 IC50 = 0.44 nM 9.36
CHEMBL5408163 IC50 = 0.74 nM 9.13
CHEMBL5419303 IC50 = 0.86 nM 9.07
CHEMBL5425070 IC50 = 0.96 nM 9.02
CHEMBL5410501 IC50 = 0.96 nM 9.02
CHEMBL5421957 IC50 = 0.97 nM 9.01
CHEMBL5432616 IC50 = 1.26 nM 8.90
CHEMBL5429957 IC50 = 1.28 nM 8.89
CHEMBL5435418 IC50 = 1.35 nM 8.87
CHEMBL3930624 FLUZOPARIB IC50 = 1.46 nM 8.84
CHEMBL5397203 IC50 = 1.91 nM 8.72
CHEMBL5427132 IC50 = 2.14 nM 8.67
CHEMBL5412306 IC50 = 2.33 nM 8.63
CHEMBL5417924 IC50 = 5.67 nM 8.25
CHEMBL5423216 IC50 = 6.19 nM 8.21
CHEMBL5436154 IC50 = 6.34 nM 8.20
CHEMBL521686 OLAPARIB IC50 = 6.65 nM 8.18
CHEMBL5436989 IC50 = 7.32 nM 8.13
CHEMBL5433982 IC50 = 8.15 nM 8.09
CHEMBL5427638 IC50 = 8.49 nM 8.07
CHEMBL5422190 IC50 = 12.92 nM 7.89
CHEMBL5438131 IC50 = 13.45 nM 7.87
CHEMBL5436743 IC50 = 23.05 nM 7.64
CHEMBL5416682 IC50 = 47.35 nM 7.33
CHEMBL5437055 IC50 = 61.66 nM 7.21
CHEMBL5402698 IC50 < 0.001 nM -
CHEMBL5437176 IC50 < 0.001 nM -
CHEMBL5425913 IC50 < 0.1 nM -
CHEMBL3137320 TALAZOPARIB IC50 - -