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Assay Detail

CHEMBL4481500

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

Binding
Binding affinity to biotinylated full length human ADCK3 expressed in Escherichia coli incubated for 1.5 hrs by fluorescent tracer dependent TR-FRET based competitive ligand binding displacement assay
11
Total Activities
11
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

Atypical kinase COQ8A, mitochondrial (CHEMBL5550)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

SGC-GAK-1: A Chemical Probe for Cyclin G Associated Kinase (GAK).
Asquith CRM, Berger BT, Wan J, Bennett JM, Capuzzi SJ, Crona DJ, Drewry DH, East MP, Elkins JM, Fedorov O, Godoi PH, Hunter DM, Knapp S, Müller S, Torrice CD, Wells CI, Earp HS, Willson TM, Zuercher WJ.
J Med Chem (2019) 62 : 2830 -2836
PubMed 30768268 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 11 6.41 7.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4575895 1 7.18
CHEMBL4556662 1 6.77
CHEMBL4585158 1 6.77
CHEMBL4517424 1 6.72
CHEMBL4443342 1 6.72
CHEMBL535429 1 6.66
CHEMBL311959 1 6.60
CHEMBL530635 1 6.13
CHEMBL4586530 1 5.92
CHEMBL4592501 1 5.70
CHEMBL4586588 1 5.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4575895 Kd = 66.0 nM 7.18
CHEMBL4556662 Kd = 170.0 nM 6.77
CHEMBL4585158 Kd = 170.0 nM 6.77
CHEMBL4517424 Kd = 190.0 nM 6.72
CHEMBL4443342 Kd = 190.0 nM 6.72
CHEMBL535429 Kd = 220.0 nM 6.66
CHEMBL311959 Kd = 250.0 nM 6.60
CHEMBL530635 Kd = 740.0 nM 6.13
CHEMBL4586530 Kd = 1200.0 nM 5.92
CHEMBL4592501 Kd = 2000.0 nM 5.70
CHEMBL4586588 Kd = 4100.0 nM 5.39