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Assay Detail

CHEMBL2169664

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

Binding
Inhibition of recombinant GST-tagged mTOR-mediated 4EBP1 phosphorylation after 90 mins by FRET assay
57
Total Activities
57
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Serine/threonine-protein kinase mTOR (CHEMBL2842)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-based design of a novel series of potent, selective inhibitors of the class I phosphatidylinositol 3-kinases.
Smith AL, D'Angelo ND, Bo YY, Booker SK, Cee VJ, Herberich B, Hong FT, Jackson CL, Lanman BA, Liu L, Nishimura N, Pettus LH, Reed AB, Tadesse S, Tamayo NA, Wurz RP, Yang K, Andrews KL, Whittington DA, McCarter JD, Miguel TS, Zalameda L, Jiang J, Subramanian R, Mullady EL, Caenepeel S, Freeman DJ, Wang L, Zhang N, Wu T, Hughes PE, Norman MH.
J Med Chem (2012) 55 : 5188 -5219
PubMed 22548365 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 57 6.15 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2165051 1 8.15
CHEMBL1762782 1 8.10
CHEMBL1615182 1 7.03
CHEMBL2165052 1 6.70
CHEMBL2165039 1 6.54
CHEMBL2165270 1 6.44
CHEMBL2165037 1 6.28
CHEMBL2165038 1 6.25
CHEMBL2165016 1 5.85
CHEMBL2165031 1 5.85
CHEMBL2165026 1 5.60
CHEMBL2165004 1 5.44
CHEMBL2165015 1 5.43
CHEMBL2165017 1 5.32
CHEMBL2165041 1 5.29
CHEMBL2165268 1 5.14
CHEMBL2165269 1 5.11
CHEMBL2165044 1 -
CHEMBL2165050 1 -
CHEMBL2165045 1 -
CHEMBL2165046 1 -
CHEMBL2165047 1 -
CHEMBL2165048 1 -
CHEMBL2165049 1 -
CHEMBL2165043 1 -
CHEMBL2165042 1 -
CHEMBL2165040 1 -
CHEMBL2165024 1 -
CHEMBL2165036 1 -
CHEMBL2165035 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2165051 IC50 = 7.0 nM 8.15
CHEMBL1762782 IC50 = 8.0 nM 8.10
CHEMBL1615182 IC50 = 93.0 nM 7.03
CHEMBL2165052 IC50 = 200.0 nM 6.70
CHEMBL2165039 IC50 = 290.0 nM 6.54
CHEMBL2165270 IC50 = 360.0 nM 6.44
CHEMBL2165037 IC50 = 530.0 nM 6.28
CHEMBL2165038 IC50 = 560.0 nM 6.25
CHEMBL2165016 IC50 = 1400.0 nM 5.85
CHEMBL2165031 IC50 = 1400.0 nM 5.85
CHEMBL2165026 IC50 = 2500.0 nM 5.60
CHEMBL2165004 IC50 = 3600.0 nM 5.44
CHEMBL2165015 IC50 = 3700.0 nM 5.43
CHEMBL2165017 IC50 = 4800.0 nM 5.32
CHEMBL2165041 IC50 = 5100.0 nM 5.29
CHEMBL2165268 IC50 = 7200.0 nM 5.14
CHEMBL2165269 IC50 = 7800.0 nM 5.11
CHEMBL2165030 IC50 > 10000.0 nM -
CHEMBL2165032 IC50 > 10000.0 nM -
CHEMBL2165033 IC50 > 10000.0 nM -
CHEMBL2165034 IC50 > 10000.0 nM -
CHEMBL2165021 IC50 > 10000.0 nM -
CHEMBL2165009 IC50 > 10000.0 nM -
CHEMBL2165010 IC50 > 10000.0 nM -
CHEMBL2165011 IC50 > 10000.0 nM -
CHEMBL2165012 IC50 > 10000.0 nM -
CHEMBL2165013 IC50 > 10000.0 nM -
CHEMBL2165014 IC50 > 10000.0 nM -
CHEMBL2165018 IC50 > 10000.0 nM -
CHEMBL2165019 IC50 > 10000.0 nM -
CHEMBL2165020 IC50 > 10000.0 nM -
CHEMBL2165003 IC50 > 10000.0 nM -
CHEMBL2165005 IC50 > 10000.0 nM -
CHEMBL2165042 IC50 > 10000.0 nM -
CHEMBL2165044 IC50 > 10000.0 nM -
CHEMBL2165050 IC50 > 10000.0 nM -
CHEMBL2165045 IC50 > 10000.0 nM -
CHEMBL2165046 IC50 > 10000.0 nM -
CHEMBL2165047 IC50 > 10000.0 nM -
CHEMBL2165048 IC50 > 10000.0 nM -
CHEMBL2165049 IC50 > 10000.0 nM -
CHEMBL2165043 IC50 > 10000.0 nM -
CHEMBL2165006 IC50 > 10000.0 nM -
CHEMBL2165040 IC50 > 10000.0 nM -
CHEMBL2165024 IC50 > 10000.0 nM -
CHEMBL2165036 IC50 > 10000.0 nM -
CHEMBL2165035 IC50 > 10000.0 nM -
CHEMBL2165271 IC50 > 10000.0 nM -
CHEMBL2165053 IC50 > 10000.0 nM -
CHEMBL2165008 IC50 > 10000.0 nM -