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Assay Detail

CHEMBL1058638

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

Binding
Inhibition of flag-tagged truncated human mTOR (1360-2549) expressed in HEK293 cells by DELFIA assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

ATP-competitive inhibitors of the mammalian target of rapamycin: design and synthesis of highly potent and selective pyrazolopyrimidines.
Zask A, Verheijen JC, Curran K, Kaplan J, Richard DJ, Nowak P, Malwitz DJ, Brooijmans N, Bard J, Svenson K, Lucas J, Toral-Barza L, Zhang WG, Hollander I, Gibbons JJ, Abraham RT, Ayral-Kaloustian S, Mansour TS, Yu K.
J Med Chem (2009) 52 : 5013 -5016
PubMed 19645448 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 8.77 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL558955 1 10.10
CHEMBL538378 1 9.70
CHEMBL557963 1 9.52
CHEMBL558486 1 9.49
CHEMBL556947 1 9.47
CHEMBL551440 1 9.42
CHEMBL562999 1 9.35
CHEMBL563985 1 9.34
CHEMBL550972 1 9.28
CHEMBL561907 1 9.21
CHEMBL540695 1 9.08
CHEMBL564404 1 9.00
CHEMBL562439 1 8.96
CHEMBL551442 1 8.85
CHEMBL552532 1 8.82
CHEMBL558288 1 8.70
CHEMBL562365 1 8.68
CHEMBL561708 1 8.37
CHEMBL561103 1 8.34
CHEMBL561844 1 8.15
CHEMBL550286 1 8.02
CHEMBL564099 1 7.66
CHEMBL562165 1 7.34
CHEMBL557895 1 5.61

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL558955 IC50 = 0.08 nM 10.10
CHEMBL538378 IC50 = 0.2 nM 9.70
CHEMBL557963 IC50 = 0.3 nM 9.52
CHEMBL558486 IC50 = 0.32 nM 9.49
CHEMBL556947 IC50 = 0.34 nM 9.47
CHEMBL551440 IC50 = 0.38 nM 9.42
CHEMBL562999 IC50 = 0.45 nM 9.35
CHEMBL563985 IC50 = 0.46 nM 9.34
CHEMBL550972 IC50 = 0.52 nM 9.28
CHEMBL561907 IC50 = 0.61 nM 9.21
CHEMBL540695 IC50 = 0.83 nM 9.08
CHEMBL564404 IC50 = 1.0 nM 9.00
CHEMBL562439 IC50 = 1.1 nM 8.96
CHEMBL551442 IC50 = 1.4 nM 8.85
CHEMBL552532 IC50 = 1.5 nM 8.82
CHEMBL558288 IC50 = 2.0 nM 8.70
CHEMBL562365 IC50 = 2.1 nM 8.68
CHEMBL561708 IC50 = 4.3 nM 8.37
CHEMBL561103 IC50 = 4.6 nM 8.34
CHEMBL561844 IC50 = 7.0 nM 8.15
CHEMBL550286 IC50 = 9.6 nM 8.02
CHEMBL564099 IC50 = 22.0 nM 7.66
CHEMBL562165 IC50 = 46.0 nM 7.34
CHEMBL557895 IC50 = 2450.0 nM 5.61