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Assay Detail

CHEMBL980899

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

Binding
Inhibition of AKT
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

RAC-alpha serine/threonine-protein kinase (CHEMBL4282)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinase with broad spectrum in vivo antitumor activity.
Velaparthi U, Wittman M, Liu P, Carboni JM, Lee FY, Attar R, Balimane P, Clarke W, Sinz MW, Hurlburt W, Patel K, Discenza L, Kim S, Gottardis M, Greer A, Li A, Saulnier M, Yang Z, Zimmermann K, Trainor G, Vyas D.
J Med Chem (2008) 51 : 5897 -5900
PubMed 18763755 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 4.32 4.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL459729 1 4.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL459729 IC50 = 48390.0 nM 4.32