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Assay Detail

CHEMBL2406000

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

Functional
Cytotoxicity against human MDA-MB-435 cells expressing p53 mutant assessed as growth inhibition by MTT assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MDA-MB-435
Confidence 1 — Organism
Curated By Autocuration

Target

MDA-MB-435 (CHEMBL614697)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.
Ding Q, Zhang Z, Liu JJ, Jiang N, Zhang J, Ross TM, Chu XJ, Bartkovitz D, Podlaski F, Janson C, Tovar C, Filipovic ZM, Higgins B, Glenn K, Packman K, Vassilev LT, Graves B.
J Med Chem (2013) 56 : 5979 -5983
PubMed 23808545 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.00 5.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2402734 1 5.21
CHEMBL2402729 1 5.07
CHEMBL2402737 IDASANUTLIN 3.0 1 5.04
CHEMBL2402733 1 5.04
CHEMBL2402730 1 5.01
CHEMBL2402731 1 4.96
CHEMBL2402735 1 4.95
CHEMBL2402732 1 4.95
CHEMBL2402736 1 4.93
CHEMBL2402573 1 4.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2402734 IC50 = 6200.0 nM 5.21
CHEMBL2402729 IC50 = 8560.0 nM 5.07
CHEMBL2402737 IDASANUTLIN IC50 = 9100.0 nM 5.04
CHEMBL2402733 IC50 = 9200.0 nM 5.04
CHEMBL2402730 IC50 = 9700.0 nM 5.01
CHEMBL2402731 IC50 = 11100.0 nM 4.96
CHEMBL2402735 IC50 = 11300.0 nM 4.95
CHEMBL2402732 IC50 = 11200.0 nM 4.95
CHEMBL2402736 IC50 = 11700.0 nM 4.93
CHEMBL2402573 IC50 = 14400.0 nM 4.84