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Assay Detail

CHEMBL5375114

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

Binding
Inhibition of GST-fused TYK2 (888 to 1187 residues)(unknown origin) using FITC-Ahr-KKSRGDYMTMQIG-NH2 peptide as substrate incubated for 30 mins in presence of ATP by caliper microfluidic mobility shift assay
17
Total Activities
17
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

Design of a Supersoft Topical JAK Inhibitor, Which Is Effective in Human Skin but Rapidly Deactivated in Blood.
Thoma G, Decoret O, Vangrevelinghe E, Trunzer M, Decker A, Orjuela Leon A, Beerli C, Bruno S, Hauchard A, Paulat G, Zerwes HG, Hacini-Rachinel F.
J Med Chem (2023) 66 : 15042 -15053
PubMed 37906573 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.80 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5412967 1 9.00
CHEMBL5396554 1 8.70
CHEMBL5407260 1 8.70
CHEMBL5404574 1 8.70
CHEMBL5422886 1 8.70
CHEMBL5407329 1 8.15
CHEMBL5431257 1 8.00
CHEMBL5409953 1 8.00
CHEMBL5403897 1 7.77
CHEMBL5420083 1 7.68
CHEMBL5424439 1 7.54
CHEMBL5417474 1 7.43
CHEMBL5270549 1 7.30
CHEMBL5395839 1 7.27
CHEMBL5279787 1 7.23
CHEMBL5420971 1 6.77
CHEMBL5271559 1 5.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5412967 IC50 = 1.0 nM 9.00
CHEMBL5396554 IC50 = 2.0 nM 8.70
CHEMBL5407260 IC50 = 2.0 nM 8.70
CHEMBL5404574 IC50 = 2.0 nM 8.70
CHEMBL5422886 IC50 = 2.0 nM 8.70
CHEMBL5407329 IC50 = 7.0 nM 8.15
CHEMBL5431257 IC50 = 10.0 nM 8.00
CHEMBL5409953 IC50 = 10.0 nM 8.00
CHEMBL5403897 IC50 = 17.0 nM 7.77
CHEMBL5420083 IC50 = 21.0 nM 7.68
CHEMBL5424439 IC50 = 29.0 nM 7.54
CHEMBL5417474 IC50 = 37.0 nM 7.43
CHEMBL5270549 IC50 = 50.0 nM 7.30
CHEMBL5395839 IC50 = 54.0 nM 7.27
CHEMBL5279787 IC50 = 59.0 nM 7.23
CHEMBL5420971 IC50 = 170.0 nM 6.77
CHEMBL5271559 IC50 = 2094.0 nM 5.68