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Assay Detail

CHEMBL5544196

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Functional
Antiproliferative activity against human NCI-H1373 cells incubated for 4 days by luminescence cell viability assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type NCI-H1373
Confidence 1 — Organism
Curated By Autocuration

Target

NCI-H1373 (CHEMBL4296389)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of tricyclic PARP7 inhibitors with high potency, selectivity, and oral bioavailability.
Xu J, Zhao A, Chen D, Wang J, Ma J, Qing L, Li Y, Fang H, He H, Pan W, Zhang S.
Eur J Med Chem (2024) 266 : 116160 -116160
PubMed 38277917 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.55 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5568745 1 8.60
CHEMBL5568973 1 8.29
CHEMBL5572156 1 8.19
CHEMBL5569182 1 7.80
CHEMBL5565268 1 7.71
CHEMBL5564709 1 7.70
CHEMBL5575932 1 7.68
CHEMBL5572774 1 7.35
CHEMBL5095043 ATAMPARIB 1.0 1 7.34
CHEMBL5575060 1 7.22
CHEMBL5574187 1 6.46
CHEMBL5565931 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5568745 IC50 = 2.5 nM 8.60
CHEMBL5568973 IC50 = 5.1 nM 8.29
CHEMBL5572156 IC50 = 6.4 nM 8.19
CHEMBL5569182 IC50 = 16.0 nM 7.80
CHEMBL5565268 IC50 = 19.7 nM 7.71
CHEMBL5564709 IC50 = 20.0 nM 7.70
CHEMBL5575932 IC50 = 21.0 nM 7.68
CHEMBL5572774 IC50 = 44.7 nM 7.35
CHEMBL5095043 ATAMPARIB IC50 = 45.3 nM 7.34
CHEMBL5575060 IC50 = 60.5 nM 7.22
CHEMBL5574187 IC50 = 344.0 nM 6.46
CHEMBL5565931 IC50 = 499.0 nM 6.30