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Assay Detail

CHEMBL5055384

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

Binding
Binding affinity to wild-type human partial length AKT3 expressed in bacterial expression system assessed as residual binding level by Kinomescan method
5
Total Activities
5
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

RAC-gamma serine/threonine-protein kinase (CHEMBL4816)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, Synthesis, and Evaluation of Potent, Selective, and Bioavailable AKT Kinase Degraders.
Yu X, Xu J, Xie L, Wang L, Shen Y, Cahuzac KM, Chen X, Liu J, Parsons RE, Jin J.
J Med Chem (2021) 64 : 18054 -18081
PubMed 34855399 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 5 8.24 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2177390 IPATASERTIB 3.0 1 8.60
CHEMBL5073195 1 8.38
CHEMBL5091595 1 8.19
CHEMBL5078362 1 8.09
CHEMBL5082198 1 7.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2177390 IPATASERTIB Kd = 2.5 nM 8.60
CHEMBL5073195 Kd = 4.2 nM 8.38
CHEMBL5091595 Kd = 6.5 nM 8.19
CHEMBL5078362 Kd = 8.1 nM 8.09
CHEMBL5082198 Kd = 12.0 nM 7.92