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Assay Detail

CHEMBL4481506

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

Binding
Binding affinity to C-terminal AVI-tagged GAK (unknown origin) (12 to 347 residues) expressed in Escherichia coli after 1.5 hrs by TR-FRET assay
7
Total Activities
7
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

Cyclin-G-associated kinase (CHEMBL4355)
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
Ki 7 6.62 8.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4443342 1 8.51
CHEMBL4531690 1 8.42
CHEMBL4535001 1 7.31
CHEMBL3823499 1 6.66
CHEMBL4462395 1 5.60
CHEMBL4514780 1 5.09
CHEMBL4518437 1 4.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4443342 Ki = 3.1 nM 8.51
CHEMBL4531690 Ki = 3.8 nM 8.42
CHEMBL4535001 Ki = 49.0 nM 7.31
CHEMBL3823499 Ki = 220.0 nM 6.66
CHEMBL4462395 Ki = 2500.0 nM 5.60
CHEMBL4514780 Ki = 8200.0 nM 5.09
CHEMBL4518437 Ki = 19000.0 nM 4.72