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Assay Detail

CHEMBL5628152

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

Binding
Inhibition of PARP1 (unknown origin) incubated for 1 hr by ELISA analysis
39
Total Activities
39
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

Identification of [1,2,4]Triazolo[4,3-a]pyrazine PARP1 inhibitors with overcome acquired resistance activities.
Wang P, Zhu WT, Wang Y, Song SS, Xi Y, Yang XY, Shen YY, Su Y, Sun YM, Gao YL, Chen Y, Ding J, Miao ZH, Zhang A, He JX.
Eur J Med Chem (2023) 259 : 115709 -115709
PubMed 37567056 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 39 8.02 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5631710 1 9.22
CHEMBL5632420 1 9.15
CHEMBL5632796 1 8.77
CHEMBL5632854 1 8.70
CHEMBL5633982 1 8.70
CHEMBL5632428 1 8.55
CHEMBL5632340 1 8.49
CHEMBL5631531 1 8.49
CHEMBL5633486 1 8.47
CHEMBL3907010 1 8.40
CHEMBL5632118 1 8.40
CHEMBL521686 OLAPARIB 4.0 1 8.39
CHEMBL5631466 1 8.39
CHEMBL5631857 1 8.39
CHEMBL3903910 1 8.37
CHEMBL5631243 1 8.34
CHEMBL5632074 1 8.24
CHEMBL5633663 1 8.11
CHEMBL5632868 1 8.04
CHEMBL5632742 1 8.03
CHEMBL3936349 1 7.92
CHEMBL5631862 1 7.88
CHEMBL5633084 1 7.75
CHEMBL5632703 1 7.68
CHEMBL5633542 1 7.60
CHEMBL5632172 1 7.37
CHEMBL5631371 1 7.21
CHEMBL5634039 1 7.15
CHEMBL5631781 1 6.97
CHEMBL5633569 1 6.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5631710 IC50 = 0.6 nM 9.22
CHEMBL5632420 IC50 = 0.7 nM 9.15
CHEMBL5632796 IC50 = 1.7 nM 8.77
CHEMBL5632854 IC50 = 2.0 nM 8.70
CHEMBL5633982 IC50 = 2.0 nM 8.70
CHEMBL5632428 IC50 = 2.8 nM 8.55
CHEMBL5632340 IC50 = 3.2 nM 8.49
CHEMBL5631531 IC50 = 3.2 nM 8.49
CHEMBL5633486 IC50 = 3.4 nM 8.47
CHEMBL3907010 IC50 = 4.0 nM 8.40
CHEMBL5632118 IC50 = 4.0 nM 8.40
CHEMBL521686 OLAPARIB IC50 = 4.1 nM 8.39
CHEMBL5631857 IC50 = 4.1 nM 8.39
CHEMBL5631466 IC50 = 4.1 nM 8.39
CHEMBL3903910 IC50 = 4.3 nM 8.37
CHEMBL5631243 IC50 = 4.6 nM 8.34
CHEMBL5632074 IC50 = 5.8 nM 8.24
CHEMBL5633663 IC50 = 7.7 nM 8.11
CHEMBL5632868 IC50 = 9.2 nM 8.04
CHEMBL5632742 IC50 = 9.4 nM 8.03
CHEMBL3936349 IC50 = 11.9 nM 7.92
CHEMBL5631862 IC50 = 13.1 nM 7.88
CHEMBL5633084 IC50 = 17.6 nM 7.75
CHEMBL5632703 IC50 = 21.0 nM 7.68
CHEMBL5633542 IC50 = 25.0 nM 7.60
CHEMBL5632172 IC50 = 42.8 nM 7.37
CHEMBL5631371 IC50 = 61.3 nM 7.21
CHEMBL5634039 IC50 = 70.7 nM 7.15
CHEMBL5631781 IC50 = 108.0 nM 6.97
CHEMBL5633569 IC50 = 182.0 nM 6.74
CHEMBL5632685 IC50 = 230.0 nM 6.64
CHEMBL5633556 IC50 = 947.0 nM 6.02
CHEMBL5632530 IC50 < 0.3 nM -
CHEMBL5633862 IC50 - -
CHEMBL5631422 IC50 > 1000.0 nM -
CHEMBL5633842 IC50 > 1000.0 nM -
CHEMBL5633704 IC50 > 1000.0 nM -
CHEMBL5631418 IC50 > 1000.0 nM -
CHEMBL5633159 IC50 > 1000.0 nM -