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Assay Detail

CHEMBL4045568

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

Binding
Inhibition of PMDM6-F peptide binding to MDM2 binding domain (1 to 118 residues) (unknown origin) by fluorescence polarization binding assay
19
Total Activities
19
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

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

Publication

Design, synthesis and biological evaluation of novel antitumor spirotetrahydrothiopyran-oxindole derivatives as potent p53-MDM2 inhibitors.
Ji C, Wang S, Chen S, He S, Jiang Y, Miao Z, Li J, Sheng C.
Bioorg Med Chem (2017) 25 : 5268 -5277
PubMed 28797774 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 19 5.44 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2152332 1 6.82
CHEMBL4085100 1 5.71
CHEMBL4082861 1 5.52
CHEMBL4100837 1 5.52
CHEMBL4076023 1 5.47
CHEMBL4079450 1 5.47
CHEMBL4097488 1 5.47
CHEMBL4105189 1 5.40
CHEMBL4098502 1 5.39
CHEMBL4068639 1 5.39
CHEMBL4089755 1 5.38
CHEMBL4103052 1 5.38
CHEMBL4080485 1 5.33
CHEMBL4095014 1 5.32
CHEMBL4095297 1 5.31
CHEMBL4087333 1 5.28
CHEMBL4067591 1 5.19
CHEMBL4074857 1 5.00
CHEMBL4071267 1 4.93

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2152332 Kd = 150.0 nM 6.82
CHEMBL4085100 Kd = 1970.0 nM 5.71
CHEMBL4082861 Kd = 3000.0 nM 5.52
CHEMBL4100837 Kd = 3000.0 nM 5.52
CHEMBL4076023 Kd = 3400.0 nM 5.47
CHEMBL4079450 Kd = 3400.0 nM 5.47
CHEMBL4097488 Kd = 3400.0 nM 5.47
CHEMBL4105189 Kd = 4000.0 nM 5.40
CHEMBL4098502 Kd = 4100.0 nM 5.39
CHEMBL4068639 Kd = 4100.0 nM 5.39
CHEMBL4089755 Kd = 4200.0 nM 5.38
CHEMBL4103052 Kd = 4200.0 nM 5.38
CHEMBL4080485 Kd = 4700.0 nM 5.33
CHEMBL4095014 Kd = 4800.0 nM 5.32
CHEMBL4095297 Kd = 4900.0 nM 5.31
CHEMBL4087333 Kd = 5200.0 nM 5.28
CHEMBL4067591 Kd = 6400.0 nM 5.19
CHEMBL4074857 Kd = 10100.0 nM 5.00
CHEMBL4071267 Kd = 11700.0 nM 4.93