Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL2182644

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

Binding
Activity at p53 in human SJSA1 cells assessed as induction of p21 mRNA expression after 7 hrs by qRT-PCR analysis in presence of 10% human serum
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type SJSA-1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Structure-based design of novel inhibitors of the MDM2-p53 interaction.
Rew Y, Sun D, Gonzalez-Lopez De Turiso F, Bartberger MD, Beck HP, Canon J, Chen A, Chow D, Deignan J, Fox BM, Gustin D, Huang X, Jiang M, Jiao X, Jin L, Kayser F, Kopecky DJ, Li Y, Lo MC, Long AM, Michelsen K, Oliner JD, Osgood T, Ragains M, Saiki AY, Schneider S, Toteva M, Yakowec P, Yan X, Ye Q, Yu D, Zhao X, Zhou J, Medina JC, Olson SH.
J Med Chem (2012) 55 : 4936 -4954
PubMed 22524527 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.42 6.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2059435 1 6.12
CHEMBL2177191 1 5.82
CHEMBL2177189 1 5.80
CHEMBL2059300 1 5.72
CHEMBL2177188 1 5.51
CHEMBL2177187 1 5.37
CHEMBL2177190 1 5.26
CHEMBL191334 NUTLIN-3 1 5.15
CHEMBL2177186 1 4.97
CHEMBL2177813 1 4.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2059435 IC50 = 760.0 nM 6.12
CHEMBL2177191 IC50 = 1500.0 nM 5.82
CHEMBL2177189 IC50 = 1600.0 nM 5.80
CHEMBL2059300 IC50 = 1900.0 nM 5.72
CHEMBL2177188 IC50 = 3100.0 nM 5.51
CHEMBL2177187 IC50 = 4300.0 nM 5.37
CHEMBL2177190 IC50 = 5500.0 nM 5.26
CHEMBL191334 NUTLIN-3 IC50 = 7100.0 nM 5.15
CHEMBL2177186 IC50 = 10700.0 nM 4.97
CHEMBL2177813 IC50 = 34400.0 nM 4.46