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Assay Detail

CHEMBL2352065

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

Functional
Cytotoxicity against human PC3 cells assessed as growth inhibition after 3 days by WST1 assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type PC-3
Confidence 1 — Organism
Curated By Autocuration

Target

PC-3 (CHEMBL390)
Type CELL-LINE
Organism Homo sapiens

Publication

Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
Mortensen DS, Sapienza J, Lee BG, Perrin-Ninkovic SM, Harris R, Shevlin G, Parnes JS, Whitefield B, Hickman M, Khambatta G, Bisonette RR, Peng S, Gamez JC, Leisten J, Narla RK, Fultz KE, Sankar S.
Bioorg Med Chem Lett (2013) 23 : 1588 -1591
PubMed 23414803 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.17 6.83

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2348864 1 6.83
CHEMBL2348865 1 6.65
CHEMBL2348862 1 5.81
CHEMBL2348863 1 5.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2348864 IC50 = 148.0 nM 6.83
CHEMBL2348865 IC50 = 224.0 nM 6.65
CHEMBL2348862 IC50 = 1550.0 nM 5.81
CHEMBL2348863 IC50 = 4180.0 nM 5.38