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Assay Detail

CHEMBL4154033

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Binding
Binding affinity to p53 Y220C mutant (unknown origin)
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Cellular tumor antigen p53 (CHEMBL4096)
Type SINGLE PROTEIN
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
Kd 5 4.84 5.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4170894 1 5.00
CHEMBL4165245 1 4.68
CHEMBL1235116 1 -
CHEMBL4173155 1 -
CHEMBL1232243 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4170894 Kd = 10000.0 nM 5.00
CHEMBL4165245 Kd = 21000.0 nM 4.68
CHEMBL1235116 Kd = 140000.0 nM -
CHEMBL4173155 Kd - -
CHEMBL1232243 Kd = 820000.0 nM -