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Assay Detail

CHEMBL3587380

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

Binding
Inhibition of mTORC2 in human PC3 cells assessed as inhibition of Akt phosphorylation at S473 after 1 hr
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type PC-3
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.
Mortensen DS, Perrin-Ninkovic SM, Shevlin G, Zhao J, Packard G, Bahmanyar S, Correa M, Elsner J, Harris R, Lee BG, Papa P, Parnes JS, Riggs JR, Sapienza J, Tehrani L, Whitefield B, Apuy J, Bisonette RR, Gamez JC, Hickman M, Khambatta G, Leisten J, Peng SX, Richardson SJ, Cathers BE, Canan SS, Moghaddam MF, Raymon HK, Worland P, Narla RK, Fultz KE, Sankar S.
J Med Chem (2015) 58 : 5323 -5333
PubMed 26083478 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.82 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3586404 ONATASERTIB 2.0 1 8.00
CHEMBL3585359 1 7.05
CHEMBL3586381 1 6.96
CHEMBL3586394 1 6.89
CHEMBL3586398 1 6.80
CHEMBL2348862 1 6.50
CHEMBL3586402 1 6.48
CHEMBL3586403 1 6.46
CHEMBL3586391 1 6.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3586404 ONATASERTIB IC50 = 10.0 nM 8.00
CHEMBL3585359 IC50 = 90.0 nM 7.05
CHEMBL3586381 IC50 = 110.0 nM 6.96
CHEMBL3586394 IC50 = 130.0 nM 6.89
CHEMBL3586398 IC50 = 160.0 nM 6.80
CHEMBL2348862 IC50 = 320.0 nM 6.50
CHEMBL3586402 IC50 = 330.0 nM 6.48
CHEMBL3586403 IC50 = 350.0 nM 6.46
CHEMBL3586391 IC50 = 610.0 nM 6.21