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Assay Detail

CHEMBL5515136

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

Binding
Inhibition of MDM2/p53 (unknown origin) interaction by fluorescence polarization assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Tumour suppressor p53/oncoprotein Mdm2 (CHEMBL1907611)
Type PROTEIN-PROTEIN INTERACTION
Organism Homo sapiens

Publication

Synthesis and biological evaluation of 4-imidazolidinone-containing compounds as potent inhibitors of the MDM2/p53 interaction.
Lin Z, Liu C, Yan Z, Cheng J, Wang X, Zhou F, Lyu X, Zhang S, Zhang D, Meng X, Zhao Y.
Eur J Med Chem (2024) 270 : 116366 -116366
PubMed 38581730 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 28 8.27 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5560431 1 9.40
CHEMBL5560586 1 9.22
CHEMBL5425989 1 9.15
CHEMBL5558118 1 9.00
CHEMBL5542912 1 9.00
CHEMBL5549791 1 8.92
CHEMBL5532484 1 8.92
CHEMBL5561895 1 8.92
CHEMBL5565747 1 8.89
CHEMBL2381408 SAR-405838 1.0 1 8.89
CHEMBL2402734 1 8.74
CHEMBL5560521 1 8.57
CHEMBL5556588 1 8.57
CHEMBL5568457 1 8.51
CHEMBL5542517 1 8.51
CHEMBL5532632 1 8.28
CHEMBL5564909 1 8.28
CHEMBL5523604 1 8.12
CHEMBL5542298 1 8.02
CHEMBL5561291 1 7.83
CHEMBL5557103 1 7.55
CHEMBL5560797 1 7.48
CHEMBL191334 NUTLIN-3 1 7.37
CHEMBL5555581 1 7.30
CHEMBL5558411 1 7.17
CHEMBL5558286 1 6.82
CHEMBL5560663 1 5.96
CHEMBL5558590 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5560431 Ki = 0.4 nM 9.40
CHEMBL5560586 Ki = 0.6 nM 9.22
CHEMBL5425989 Ki = 0.7 nM 9.15
CHEMBL5558118 Ki = 1.0 nM 9.00
CHEMBL5542912 Ki = 1.0 nM 9.00
CHEMBL5549791 Ki = 1.2 nM 8.92
CHEMBL5532484 Ki = 1.2 nM 8.92
CHEMBL5561895 Ki = 1.2 nM 8.92
CHEMBL5565747 Ki = 1.3 nM 8.89
CHEMBL2381408 SAR-405838 Ki = 1.3 nM 8.89
CHEMBL2402734 Ki = 1.8 nM 8.74
CHEMBL5560521 Ki = 2.7 nM 8.57
CHEMBL5556588 Ki = 2.7 nM 8.57
CHEMBL5568457 Ki = 3.1 nM 8.51
CHEMBL5542517 Ki = 3.1 nM 8.51
CHEMBL5532632 Ki = 5.2 nM 8.28
CHEMBL5564909 Ki = 5.3 nM 8.28
CHEMBL5523604 Ki = 7.6 nM 8.12
CHEMBL5542298 Ki = 9.6 nM 8.02
CHEMBL5561291 Ki = 14.8 nM 7.83
CHEMBL5557103 Ki = 27.9 nM 7.55
CHEMBL5560797 Ki = 32.8 nM 7.48
CHEMBL191334 NUTLIN-3 Ki = 42.6 nM 7.37
CHEMBL5555581 Ki = 50.5 nM 7.30
CHEMBL5558411 Ki = 67.4 nM 7.17
CHEMBL5558286 Ki = 151.6 nM 6.82
CHEMBL5560663 Ki = 1088.0 nM 5.96
CHEMBL5558590 Ki > 27000.0 nM -