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Assay Detail

CHEMBL2389361

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

Functional
Cytotoxicity against human RKO cells expressing wild type p53 assessed as cell viability after 5 days by MTT assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type RKO
Confidence 1 — Organism
Curated By Autocuration

Target

RKO (CHEMBL614879)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development.
Vu B, Wovkulich P, Pizzolato G, Lovey A, Ding Q, Jiang N, Liu JJ, Zhao C, Glenn K, Wen Y, Tovar C, Packman K, Vassilev L, Graves B.
ACS Med Chem Lett (2013) 4 : 466 -469
PubMed 24900694 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.00 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2386348 1 6.52
CHEMBL2386347 1 6.52
CHEMBL2386345 1 6.52
CHEMBL2386346 RO-5045337 1.0 1 6.40
CHEMBL2386344 1 6.40
CHEMBL2386349 1 6.30
CHEMBL2386343 1 6.30
CHEMBL2386169 1 6.30
CHEMBL2386350 1 6.22
CHEMBL191334 NUTLIN-3 1 5.82
CHEMBL2386170 1 5.17
CHEMBL2386351 1 4.90
CHEMBL2386168 1 4.62
CHEMBL2386167 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2386348 IC50 = 300.0 nM 6.52
CHEMBL2386347 IC50 = 300.0 nM 6.52
CHEMBL2386345 IC50 = 300.0 nM 6.52
CHEMBL2386346 RO-5045337 IC50 = 400.0 nM 6.40
CHEMBL2386344 IC50 = 400.0 nM 6.40
CHEMBL2386349 IC50 = 500.0 nM 6.30
CHEMBL2386343 IC50 = 500.0 nM 6.30
CHEMBL2386169 IC50 = 500.0 nM 6.30
CHEMBL2386350 IC50 = 600.0 nM 6.22
CHEMBL191334 NUTLIN-3 IC50 = 1500.0 nM 5.82
CHEMBL2386170 IC50 = 6800.0 nM 5.17
CHEMBL2386351 IC50 = 12500.0 nM 4.90
CHEMBL2386168 IC50 = 23700.0 nM 4.62
CHEMBL2386167 IC50 > 30000.0 nM -