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Assay Detail

CHEMBL4145360

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

Binding
Inhibition of wild-type human partial length KIT (I571 to D952 residues) expressed in bacterial expression system by ATP-site competition binding assay based KinomeScan assay relative to control
2
Total Activities
2
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

Mast/stem cell growth factor receptor Kit (CHEMBL1936)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimization of Isothiazolo[4,3- b]pyridine-Based Inhibitors of Cyclin G Associated Kinase (GAK) with Broad-Spectrum Antiviral Activity.
Pu SY, Wouters R, Schor S, Rozenski J, Barouch-Bentov R, Prugar LI, O'Brien CM, Brannan JM, Dye JM, Herdewijn P, De Jonghe S, Einav S.
J Med Chem (2018) 61 : 6178 -6192
PubMed 29953812 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 2 7.12 8.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3425867 1 8.35
CHEMBL4172550 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3425867 Kd = 4.5 nM 8.35
CHEMBL4172550 Kd = 1300.0 nM 5.89