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Assay Detail

CHEMBL5046593

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

Binding
Inhibition of human AAK1 using peptide as substrate incubated for 120 mins in presence of [gamma-33ATP] by scintillation counting based radiometry assay
5
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

AP2-associated protein kinase 1 (CHEMBL3830)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of Pyrimidine-Based Lead Compounds for Understudied Kinases Implicated in Driving Neurodegeneration.
Drewry DH, Annor-Gyamfi JK, Wells CI, Pickett JE, Dederer V, Preuss F, Mathea S, Axtman AD.
J Med Chem (2022) 65 : 1313 -1328
PubMed 34333981 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.88 7.13
Inhibition 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5079149 2 7.13
CHEMBL5083125 1 7.10
CHEMBL5075360 1 6.41
CHEMBL5079920 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5079149 IC50 = 74.0 nM 7.13
CHEMBL5083125 IC50 = 80.0 nM 7.10
CHEMBL5075360 IC50 = 390.0 nM 6.41
CHEMBL5079920 Inhibition - % -
CHEMBL5079149 Inhibition - % -