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Assay Detail

CHEMBL3363505

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

Binding
Inhibition of human MDM2 (1-188 aa) -p53 (1-83 aa) interaction expressed in Escherichia coli after 18 hrs by HTRF assay
23
Total Activities
23
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

Discovery of Potent and Simplified Piperidinone-Based Inhibitors of the MDM2-p53 Interaction.
Yu M, Wang Y, Zhu J, Bartberger MD, Canon J, Chen A, Chow D, Eksterowicz J, Fox B, Fu J, Gribble M, Huang X, Li Z, Liu JJ, Lo MC, McMinn D, Oliner JD, Osgood T, Rew Y, Saiki AY, Shaffer P, Yan X, Ye Q, Yu D, Zhao X, Zhou J, Olson SH, Medina JC, Sun D.
ACS Med Chem Lett (2014) 5 : 894 -899
PubMed 25147610 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 8.44 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3329613 1 9.15
CHEMBL2059435 1 9.00
CHEMBL3329602 1 9.00
CHEMBL3329608 1 8.82
CHEMBL3329611 1 8.70
CHEMBL3329601 1 8.70
CHEMBL3329610 1 8.70
CHEMBL3329224 1 8.70
CHEMBL3329616 1 8.52
CHEMBL3329605 1 8.52
CHEMBL2177190 1 8.52
CHEMBL3329619 1 8.40
CHEMBL3329614 1 8.30
CHEMBL3329617 1 8.30
CHEMBL3329612 1 8.22
CHEMBL3329604 1 8.22
CHEMBL3329615 1 8.15
CHEMBL3329606 1 8.15
CHEMBL3329603 1 8.10
CHEMBL3329620 1 8.05
CHEMBL3329607 1 8.05
CHEMBL3329609 1 8.00
CHEMBL3329618 1 7.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3329613 IC50 = 0.7 nM 9.15
CHEMBL2059435 IC50 = 1.0 nM 9.00
CHEMBL3329602 IC50 = 1.0 nM 9.00
CHEMBL3329608 IC50 = 1.5 nM 8.82
CHEMBL3329611 IC50 = 2.0 nM 8.70
CHEMBL3329601 IC50 = 2.0 nM 8.70
CHEMBL3329610 IC50 = 2.0 nM 8.70
CHEMBL3329224 IC50 = 2.0 nM 8.70
CHEMBL3329616 IC50 = 3.0 nM 8.52
CHEMBL3329605 IC50 = 3.0 nM 8.52
CHEMBL2177190 IC50 = 3.0 nM 8.52
CHEMBL3329619 IC50 = 4.0 nM 8.40
CHEMBL3329614 IC50 = 5.0 nM 8.30
CHEMBL3329617 IC50 = 5.0 nM 8.30
CHEMBL3329612 IC50 = 6.0 nM 8.22
CHEMBL3329604 IC50 = 6.0 nM 8.22
CHEMBL3329615 IC50 = 7.0 nM 8.15
CHEMBL3329606 IC50 = 7.0 nM 8.15
CHEMBL3329603 IC50 = 8.0 nM 8.10
CHEMBL3329620 IC50 = 9.0 nM 8.05
CHEMBL3329607 IC50 = 9.0 nM 8.05
CHEMBL3329609 IC50 = 10.0 nM 8.00
CHEMBL3329618 IC50 = 13.0 nM 7.89