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Assay Detail

CHEMBL2330634

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

Binding
Inhibition of recombinant mTOR (unknown origin)
6
Total Activities
6
Compounds Tested
1
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

Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity.
Foote KM, Blades K, Cronin A, Fillery S, Guichard SS, Hassall L, Hickson I, Jacq X, Jewsbury PJ, McGuire TM, Nissink JW, Odedra R, Page K, Perkins P, Suleman A, Tam K, Thommes P, Broadhurst R, Wood C.
J Med Chem (2013) 56 : 2125 -2138
PubMed 23394205 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.80 7.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2325697 1 7.42
CHEMBL2325704 1 6.75
CHEMBL2325703 1 6.72
CHEMBL2325706 1 6.64
CHEMBL2030442 1 6.48
CHEMBL2325705 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2325697 IC50 = 38.0 nM 7.42
CHEMBL2325704 IC50 = 180.0 nM 6.75
CHEMBL2325703 IC50 = 190.0 nM 6.72
CHEMBL2325706 IC50 = 230.0 nM 6.64
CHEMBL2030442 IC50 = 330.0 nM 6.48
CHEMBL2325705 IC50 - -