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Assay Detail

CHEMBL4723752

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

Binding
Binding affinity to N-terminal His-tagged STK17B kinase domain (25 to 329 residues) (unknown origin) expressed in Escherichia coli by KINOMEscan scanMAX assay
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

Serine/threonine-protein kinase 17B (CHEMBL3980)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A Chemical Probe for Dark Kinase STK17B Derives Its Potency and High Selectivity through a Unique P-Loop Conformation.
Picado A,Chaikuad A,Wells CI,Shrestha S,Zuercher WJ,Pickett JE,Kwarcinski FE,Sinha P,de Silva CS,Zutshi R,Liu S,Kannan N,Knapp S,Drewry DH,Willson TM
J Med Chem (2020) 63 : 14626 -14646
PubMed 33215924 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 5 7.64 8.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1836719 1 8.42
CHEMBL4752776 1 8.25
CHEMBL1836721 1 7.96
CHEMBL1836641 1 7.52
CHEMBL4763392 1 6.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1836719 Kd = 3.8 nM 8.42
CHEMBL4752776 Kd = 5.6 nM 8.25
CHEMBL1836721 Kd = 11.0 nM 7.96
CHEMBL1836641 Kd = 30.0 nM 7.52
CHEMBL4763392 Kd = 910.0 nM 6.04