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Assay Detail

CHEMBL3223610

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

Binding
Inhibition of mTOR (unknown origin)
12
Total Activities
12
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Small molecules targeting phosphoinositide 3-kinases
Wu P, Hu Y
Medchemcomm (2012) 3 : 1337 -1355
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.61 8.80
Ki 2 7.79 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL592445 GEDATOLISIB 3.0 1 8.80
CHEMBL1081312 1 8.00
CHEMBL3218579 1 7.80
CHEMBL1922094 APITOLISIB 2.0 1 7.77
CHEMBL1879463 DACTOLISIB 3.0 1 7.68
CHEMBL1233882 1 6.85
CHEMBL3349370 1 6.72
CHEMBL3218580 1 5.97
CHEMBL1233881 1 5.77
CHEMBL1230790 1 5.68
CHEMBL1234815 1 4.00
CHEMBL2216870 IDELALISIB 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL592445 GEDATOLISIB IC50 = 1.6 nM 8.80
CHEMBL1081312 IC50 = 10.0 nM 8.00
CHEMBL3218579 Ki = 16.0 nM 7.80
CHEMBL1922094 APITOLISIB Ki = 17.0 nM 7.77
CHEMBL1879463 DACTOLISIB IC50 = 21.0 nM 7.68
CHEMBL1233882 IC50 = 140.0 nM 6.85
CHEMBL3349370 IC50 = 190.0 nM 6.72
CHEMBL3218580 IC50 = 1060.0 nM 5.97
CHEMBL1233881 IC50 = 1700.0 nM 5.77
CHEMBL1230790 IC50 = 2100.0 nM 5.68
CHEMBL1234815 IC50 = 100000.0 nM 4.00
CHEMBL2216870 IDELALISIB IC50 > 10000.0 nM -