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Assay Detail

CHEMBL1942065

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

Binding
Inhibition of His-tagged AKT1 using 5FAM-GRPRTSSFAEGCONH2 as substrate by fluorescence based assay
8
Total Activities
8
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 of novel, potent, and selective inhibitors of 3-phosphoinositide-dependent kinase (PDK1).
Murphy ST, Alton G, Bailey S, Baxi SM, Burke BJ, Chappie TA, Ermolieff J, Ferre R, Greasley S, Hickey M, Humphrey J, Kablaoui N, Kath J, Kazmirski S, Kraus M, Kupchinsky S, Li J, Lingardo L, Marx MA, Richter D, Tanis SP, Tran K, Vernier W, Xie Z, Yin MJ, Yu XH.
J Med Chem (2011) 54 : 8490 -8500
PubMed 22040023 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 6.76 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1940249 1 8.00
CHEMBL1940250 1 7.00
CHEMBL1940251 1 6.77
CHEMBL1940246 1 6.68
CHEMBL1940248 1 6.64
CHEMBL1938415 1 6.58
CHEMBL1940252 1 6.44
CHEMBL1940253 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1940249 Ki = 10.0 nM 8.00
CHEMBL1940250 Ki = 100.0 nM 7.00
CHEMBL1940251 Ki = 170.0 nM 6.77
CHEMBL1940246 Ki = 210.0 nM 6.68
CHEMBL1940248 Ki = 230.0 nM 6.64
CHEMBL1938415 Ki = 260.0 nM 6.58
CHEMBL1940252 Ki = 360.0 nM 6.44
CHEMBL1940253 Ki = 1100.0 nM 5.96