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Assay Detail

CHEMBL5046599

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

Binding
Inhibition of human TYK2 (875 to end residues) using GGMEDIYFEFMGGKKK as substrate measured after 40 mins in presence of [gamma33P]ATP by radiometric scintillation counting method
5
Total Activities
5
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

Non-receptor tyrosine-protein kinase TYK2 (CHEMBL3553)
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 5 6.93 7.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5087006 1 7.48
CHEMBL5079149 1 7.32
CHEMBL5083125 1 7.17
CHEMBL5089987 1 6.56
CHEMBL5075360 1 6.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5087006 IC50 = 33.0 nM 7.48
CHEMBL5079149 IC50 = 48.0 nM 7.32
CHEMBL5083125 IC50 = 67.0 nM 7.17
CHEMBL5089987 IC50 = 276.0 nM 6.56
CHEMBL5075360 IC50 = 720.0 nM 6.14