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Assay Detail

CHEMBL4154044

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Functional
Antiproliferative activity against human BxPC3 cells harboring p53 Y220C mutant after 72 hrs by CellTiter-Glo assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type BXPC-3
Confidence 1 — Organism
Curated By Intermediate

Target

BXPC-3 (CHEMBL614530)
Type CELL-LINE
Organism Homo sapiens

Publication

Aminobenzothiazole derivatives stabilize the thermolabile p53 cancer mutant Y220C and show anticancer activity in p53-Y220C cell lines.
Baud MGJ, Bauer MR, Verduci L, Dingler FA, Patel KJ, Horil Roy D, Joerger AC, Fersht AR.
Eur J Med Chem (2018) 152 : 101 -114
PubMed 29702446 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 4.58 4.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4170894 1 4.96
CHEMBL4166006 1 4.75
CHEMBL1235116 1 4.37
CHEMBL4163657 1 4.24
CHEMBL4168439 1 -
CHEMBL4162051 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4170894 IC50 = 11000.0 nM 4.96
CHEMBL4166006 IC50 = 18000.0 nM 4.75
CHEMBL1235116 IC50 = 43000.0 nM 4.37
CHEMBL4163657 IC50 = 57000.0 nM 4.24
CHEMBL4168439 IC50 - -
CHEMBL4162051 IC50 - -