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Assay Detail

CHEMBL3364003

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

Binding
Inhibition of p53-MDM2 (unknown origin) interaction using 0.02% BSA buffer after 1 hr by HTRF assay
13
Total Activities
13
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 selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy.
Zhang Z, Ding Q, Liu JJ, Zhang J, Jiang N, Chu XJ, Bartkovitz D, Luk KC, Janson C, Tovar C, Filipovic ZM, Higgins B, Glenn K, Packman K, Vassilev LT, Graves B.
Bioorg Med Chem (2014) 22 : 4001 -4009
PubMed 24997575 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 8.01 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3310182 1 8.40
CHEMBL3310321 1 8.30
CHEMBL3310320 1 8.30
CHEMBL3310188 1 8.30
CHEMBL3310186 1 8.30
CHEMBL3310185 1 8.30
CHEMBL3310184 1 8.30
CHEMBL3310322 1 8.22
CHEMBL3310319 1 8.15
CHEMBL3310187 1 8.15
CHEMBL2402737 IDASANUTLIN 3.0 1 8.05
CHEMBL3310323 1 7.82
CHEMBL3310183 1 5.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3310182 IC50 = 4.0 nM 8.40
CHEMBL3310321 IC50 = 5.0 nM 8.30
CHEMBL3310320 IC50 = 5.0 nM 8.30
CHEMBL3310188 IC50 = 5.0 nM 8.30
CHEMBL3310186 IC50 = 5.0 nM 8.30
CHEMBL3310185 IC50 = 5.0 nM 8.30
CHEMBL3310184 IC50 = 5.0 nM 8.30
CHEMBL3310322 IC50 = 6.0 nM 8.22
CHEMBL3310319 IC50 = 7.0 nM 8.15
CHEMBL3310187 IC50 = 7.0 nM 8.15
CHEMBL2402737 IDASANUTLIN IC50 = 9.0 nM 8.05
CHEMBL3310323 IC50 = 15.0 nM 7.82
CHEMBL3310183 IC50 = 3089.0 nM 5.51