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Assay Detail

CHEMBL1109709

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

Functional
Antiproliferative activity against human MCF7.1 cells after 3 days by celltiter-glo luminescence assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MCF7.1
Confidence 1 — Organism
Curated By Autocuration

Publication

Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor.
Heffron TP, Berry M, Castanedo G, Chang C, Chuckowree I, Dotson J, Folkes A, Gunzner J, Lesnick JD, Lewis C, Mathieu S, Nonomiya J, Olivero A, Pang J, Peterson D, Salphati L, Sampath D, Sideris S, Sutherlin DP, Tsui V, Wan NC, Wang S, Wong S, Zhu BY.
Bioorg Med Chem Lett (2010) 20 : 2408 -2411
PubMed 20346656 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 8.08 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1090601 1 10.40
CHEMBL1090598 1 9.77
CHEMBL1090599 1 9.72
CHEMBL1090600 1 9.54
CHEMBL594844 1 9.37
CHEMBL1093267 1 7.19
CHEMBL1091977 1 7.17
CHEMBL1090239 1 7.11
CHEMBL1083192 1 6.89
CHEMBL1091978 1 6.84
CHEMBL1091979 1 6.79
CHEMBL521851 PICTILISIB 2.0 1 6.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1090601 EC50 = 0.04 nM 10.40
CHEMBL1090598 EC50 = 0.17 nM 9.77
CHEMBL1090599 EC50 = 0.19 nM 9.72
CHEMBL1090600 EC50 = 0.29 nM 9.54
CHEMBL594844 EC50 = 0.43 nM 9.37
CHEMBL1093267 EC50 = 65.0 nM 7.19
CHEMBL1091977 EC50 = 68.0 nM 7.17
CHEMBL1090239 EC50 = 78.0 nM 7.11
CHEMBL1083192 EC50 = 130.0 nM 6.89
CHEMBL1091978 EC50 = 143.0 nM 6.84
CHEMBL1091979 EC50 = 164.0 nM 6.79
CHEMBL521851 PICTILISIB EC50 = 720.0 nM 6.14