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Assay Detail

CHEMBL5529686

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

Binding
Inhibition of mTOR in human MDA-MB-468 cells incubated for 2.5 hrs by Alexa Fluor 488 staining based fluorescence analysis
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MDA-MB-468
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Identification of Novel, Selective Ataxia-Telangiectasia Mutated Kinase Inhibitors with the Ability to Penetrate the Blood-Brain Barrier: The Discovery of AZD1390.
Pike KG, Hunt TA, Barlaam B, Benstead D, Cadogan E, Chen K, Cook CR, Colclough N, Deng C, Durant ST, Eatherton A, Goldberg K, Johnström P, Liu L, Liu Z, Nissink JWM, Pang C, Pass M, Robb GR, Roberts C, Schou M, Steward O, Sykes A, Yan Y, Zhai B, Zheng L.
J Med Chem (2024) 67 : 3090 -3111
PubMed 38306388 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.90 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5575600 1 6.30
CHEMBL3960662 1 5.90
CHEMBL5555756 1 5.50
CHEMBL5566946 1 -
CHEMBL4594429 AZD-1390 1.0 1 -
CHEMBL5572255 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5575600 IC50 = 501.19 nM 6.30
CHEMBL3960662 IC50 = 1258.93 nM 5.90
CHEMBL5555756 IC50 = 3162.28 nM 5.50
CHEMBL5566946 IC50 > 31622.78 nM -
CHEMBL4594429 AZD-1390 IC50 > 15848.93 nM -
CHEMBL5572255 IC50 > 1258.93 nM -