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Assay Detail

CHEMBL3587522

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

Binding
Inhibition of mTORC1 in human PC3 cells assessed as inhibition of p70S6K phosphorylation after 1 hr
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type PC-3
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

mTORC1 (CHEMBL4296661)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115.
Mortensen DS, Perrin-Ninkovic SM, Shevlin G, Elsner J, Zhao J, Whitefield B, Tehrani L, Sapienza J, Riggs JR, Parnes JS, Papa P, Packard G, Lee BG, Harris R, Correa M, Bahmanyar S, Richardson SJ, Peng SX, Leisten J, Khambatta G, Hickman M, Gamez JC, Bisonette RR, Apuy J, Cathers BE, Canan SS, Moghaddam MF, Raymon HK, Worland P, Narla RK, Fultz KE, Sankar S.
J Med Chem (2015) 58 : 5599 -5608
PubMed 26102506 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.79 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3586561 1 8.40
CHEMBL3586566 1 8.22
CHEMBL3586387 1 8.10
CHEMBL3586568 1 8.00
CHEMBL3586571 1 8.00
CHEMBL3586567 1 7.92
CHEMBL3586562 1 7.57
CHEMBL3586572 1 7.28
CHEMBL3586559 1 7.27
CHEMBL3586570 1 7.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3586561 IC50 = 4.0 nM 8.40
CHEMBL3586566 IC50 = 6.0 nM 8.22
CHEMBL3586387 IC50 = 8.0 nM 8.10
CHEMBL3586568 IC50 = 10.0 nM 8.00
CHEMBL3586571 IC50 = 10.0 nM 8.00
CHEMBL3586567 IC50 = 12.0 nM 7.92
CHEMBL3586562 IC50 = 27.0 nM 7.57
CHEMBL3586572 IC50 = 53.0 nM 7.28
CHEMBL3586559 IC50 = 54.0 nM 7.27
CHEMBL3586570 IC50 = 66.0 nM 7.18