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Assay Detail

CHEMBL5538583

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

Binding
Inhibition of PARP7 (unknown origin) measured after 1 hr incubation by microplate reader assay
19
Total Activities
19
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

Protein mono-ADP-ribosyltransferase TIPARP (CHEMBL2380188)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Highly Selective PARP7 Inhibitors with a Novel Scaffold for Cancer Immunotherapy.
Gu H, Yan W, Yang J, Liu B, Zhao X, Wang H, Xu W, Wang C, Chen Y, Dong Q, Zhu Q, Xu Y, Zou Y.
J Med Chem (2024) 67 : 1932 -1948
PubMed 38059836 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.58 8.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5571636 1 8.35
CHEMBL5095043 ATAMPARIB 1.0 1 8.25
CHEMBL5573525 1 8.07
CHEMBL5570155 1 7.70
CHEMBL5563046 1 7.65
CHEMBL5571907 1 7.34
CHEMBL5566904 1 7.21
CHEMBL5572349 1 6.91
CHEMBL5591356 1 6.77
CHEMBL5569932 1 -
CHEMBL5566250 1 -
CHEMBL5564068 1 -
CHEMBL5590832 1 -
CHEMBL5562672 1 -
CHEMBL5575757 1 -
CHEMBL5572531 1 -
CHEMBL5592601 1 -
CHEMBL5567004 1 -
CHEMBL5592002 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5571636 IC50 = 4.5 nM 8.35
CHEMBL5095043 ATAMPARIB IC50 = 5.6 nM 8.25
CHEMBL5573525 IC50 = 8.5 nM 8.07
CHEMBL5570155 IC50 = 20.0 nM 7.70
CHEMBL5563046 IC50 = 22.3 nM 7.65
CHEMBL5571907 IC50 = 46.0 nM 7.34
CHEMBL5566904 IC50 = 62.0 nM 7.21
CHEMBL5572349 IC50 = 122.0 nM 6.91
CHEMBL5591356 IC50 = 171.3 nM 6.77
CHEMBL5569932 IC50 - -
CHEMBL5566250 IC50 - -
CHEMBL5564068 IC50 - -
CHEMBL5590832 IC50 - -
CHEMBL5562672 IC50 - -
CHEMBL5575757 IC50 - -
CHEMBL5572531 IC50 - -
CHEMBL5592601 IC50 - -
CHEMBL5567004 IC50 - -
CHEMBL5592002 IC50 - -