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Assay Detail

CHEMBL5362137

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

Binding
Binding affinity to MDMX (1 to 118 residues) (unknown origin) assessed as inhibition constant incubated for 1 hr measured by fluorescence polarization assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Protein Mdm4 (CHEMBL1255126)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-based discovery of novel α-aminoketone derivatives as dual p53-MDM2/MDMX inhibitors for the treatment of cancer.
Luo HJ, Si DJ, Sun XJ, Wang MY, Yang YB, Wang B, Wen HM, Li W, Liu J.
Eur J Med Chem (2023) 252 : 115282 -115282
PubMed 36989812 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 5.10 6.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3347643 1 6.11
CHEMBL5418298 1 5.61
CHEMBL5426939 1 5.46
CHEMBL5416654 1 5.38
CHEMBL5430787 1 5.13
CHEMBL5437839 1 5.03
CHEMBL5422731 1 4.94
CHEMBL5400761 1 4.89
CHEMBL5417713 1 4.88
CHEMBL5433819 1 4.81
CHEMBL5396791 1 4.54
CHEMBL5400500 1 4.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3347643 Ki = 780.0 nM 6.11
CHEMBL5418298 Ki = 2450.0 nM 5.61
CHEMBL5426939 Ki = 3460.0 nM 5.46
CHEMBL5416654 Ki = 4220.0 nM 5.38
CHEMBL5430787 Ki = 7430.0 nM 5.13
CHEMBL5437839 Ki = 9370.0 nM 5.03
CHEMBL5422731 Ki = 11590.0 nM 4.94
CHEMBL5400761 Ki = 12930.0 nM 4.89
CHEMBL5417713 Ki = 13040.0 nM 4.88
CHEMBL5433819 Ki = 15570.0 nM 4.81
CHEMBL5396791 Ki = 29100.0 nM 4.54
CHEMBL5400500 Ki = 36820.0 nM 4.43