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Assay Detail

CHEMBL868168

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Binding
Displacement of p53 mimicking fluorescent peptide from Hdm2 by FP assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

E3 ubiquitin-protein ligase Mdm2 (CHEMBL5023)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Enantiomerically pure 1,4-benzodiazepine-2,5-diones as Hdm2 antagonists.
Marugan JJ, Leonard K, Raboisson P, Gushue JM, Calvo R, Koblish HK, Lattanze J, Zhao S, Cummings MD, Player MR, Schubert C, Maroney AC, Lu T.
Bioorg Med Chem Lett (2006) 16 : 3115 -3120
PubMed 16630722 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.85 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL377614 1 6.60
CHEMBL377203 1 6.43
CHEMBL210545 1 6.41
CHEMBL208562 1 6.26
CHEMBL207364 1 6.10
CHEMBL210151 1 6.07
CHEMBL378662 1 5.81
CHEMBL207202 1 5.62
CHEMBL209201 1 5.57
CHEMBL207541 1 5.27
CHEMBL378851 1 5.20
CHEMBL377639 1 4.88
CHEMBL207013 1 -
CHEMBL425780 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL377614 IC50 = 250.0 nM 6.60
CHEMBL377203 IC50 = 367.0 nM 6.43
CHEMBL210545 IC50 = 394.0 nM 6.41
CHEMBL208562 IC50 = 546.0 nM 6.26
CHEMBL207364 IC50 = 787.0 nM 6.10
CHEMBL210151 IC50 = 856.0 nM 6.07
CHEMBL378662 IC50 = 1550.0 nM 5.81
CHEMBL207202 IC50 = 2390.0 nM 5.62
CHEMBL209201 IC50 = 2700.0 nM 5.57
CHEMBL207541 IC50 = 5400.0 nM 5.27
CHEMBL378851 IC50 = 6250.0 nM 5.20
CHEMBL377639 IC50 = 13100.0 nM 4.88
CHEMBL207013 IC50 > 12500.0 nM -
CHEMBL425780 IC50 - -