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Assay Detail

CHEMBL5046580

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

Binding
Inhibition of recombinant human DRAK1 using KKLNRTLSFAEPG as substrate after 40 mins in presence of [gamma-33ATP] by scintillation counting based radiometry assay
7
Total Activities
7
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

Serine/threonine-protein kinase 17A (CHEMBL4525)
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
Inhibition 5 - -
IC50 2 6.60 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5079601 1 6.70
CHEMBL5075360 1 6.49
CHEMBL5079920 1 -
CHEMBL5088930 1 -
CHEMBL5085430 1 -
CHEMBL5090046 1 -
CHEMBL3605057 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5079601 IC50 = 202.0 nM 6.70
CHEMBL5075360 IC50 = 325.0 nM 6.49
CHEMBL5079920 Inhibition - % -
CHEMBL5088930 Inhibition - % -
CHEMBL5085430 Inhibition - % -
CHEMBL5090046 Inhibition - % -
CHEMBL3605057 Inhibition - % -