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Assay Detail

CHEMBL1925476

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

Functional
Antiproliferative activity against human PC3 cells after overnight incubation by CellTiter-Glo luminescence assay
10
Total Activities
10
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

Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer.
Sutherlin DP, Bao L, Berry M, Castanedo G, Chuckowree I, Dotson J, Folks A, Friedman L, Goldsmith R, Gunzner J, Heffron T, Lesnick J, Lewis C, Mathieu S, Murray J, Nonomiya J, Pang J, Pegg N, Prior WW, Rouge L, Salphati L, Sampath D, Tian Q, Tsui V, Wan NC, Wang S, Wei B, Wiesmann C, Wu P, Zhu BY, Olivero A.
J Med Chem (2011) 54 : 7579 -7587
PubMed 21981714 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.54 6.94

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1922095 1 6.94
CHEMBL1091978 1 6.66
CHEMBL1922090 1 6.64
CHEMBL521851 PICTILISIB 2.0 1 6.55
CHEMBL1921986 1 6.53
CHEMBL1083192 1 6.51
CHEMBL1922094 APITOLISIB 2.0 1 6.51
CHEMBL1922092 1 6.43
CHEMBL1922093 1 6.34
CHEMBL1922091 1 6.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1922095 IC50 = 116.0 nM 6.94
CHEMBL1091978 IC50 = 220.0 nM 6.66
CHEMBL1922090 IC50 = 228.0 nM 6.64
CHEMBL521851 PICTILISIB IC50 = 280.0 nM 6.55
CHEMBL1921986 IC50 = 295.0 nM 6.53
CHEMBL1083192 IC50 = 310.0 nM 6.51
CHEMBL1922094 APITOLISIB IC50 = 307.0 nM 6.51
CHEMBL1922092 IC50 = 367.0 nM 6.43
CHEMBL1922093 IC50 = 457.0 nM 6.34
CHEMBL1922091 IC50 = 556.0 nM 6.25