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Assay Detail

CHEMBL4235136

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

Binding
Induction of p53 transcriptional activity (unknown origin) expressed in HEK293 cells coexpressing TK-driven Rluc after 20 to 22 hrs by luciferase reporter gene assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cellular tumor antigen p53 (CHEMBL4096)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel tertiary sulfonamides as potent anti-cancer agents.
Okolotowicz KJ, Dwyer M, Ryan D, Cheng J, Cashman EA, Moore S, Mercola M, Cashman JR.
Bioorg Med Chem (2018) 26 : 4441 -4451
PubMed 30075999 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 7.71 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4248974 1 8.70
CHEMBL4246320 1 8.40
CHEMBL4238053 1 8.40
CHEMBL4243509 1 8.05
CHEMBL4240212 1 7.92
CHEMBL4244338 1 7.19
CHEMBL4240141 1 7.13
CHEMBL4240977 1 6.82
CHEMBL4243377 1 6.80
CHEMBL4243580 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4248974 EC50 = 2.0 nM 8.70
CHEMBL4246320 EC50 = 4.0 nM 8.40
CHEMBL4238053 EC50 = 4.0 nM 8.40
CHEMBL4243509 EC50 = 9.0 nM 8.05
CHEMBL4240212 EC50 = 12.0 nM 7.92
CHEMBL4244338 EC50 = 65.0 nM 7.19
CHEMBL4240141 EC50 = 74.0 nM 7.13
CHEMBL4240977 EC50 = 152.0 nM 6.82
CHEMBL4243377 EC50 = 158.0 nM 6.80
CHEMBL4243580 EC50 > 5000.0 nM -