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Assay Detail

CHEMBL3375810

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

Binding
Inhibition of Tyk2 (unknown origin)
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

Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation.
Hanan EJ, Eigenbrot C, Bryan MC, Burdick DJ, Chan BK, Chen Y, Dotson J, Heald RA, Jackson PS, La H, Lainchbury MD, Malek S, Purkey HE, Schaefer G, Schmidt S, Seward EM, Sideris S, Tam C, Wang S, Yeap SK, Yen I, Yin J, Yu C, Zilberleyb I, Heffron TP.
J Med Chem (2014) 57 : 10176 -10191
PubMed 25383627 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.92 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3352835 1 7.80
CHEMBL3354186 1 7.44
CHEMBL3354185 1 5.51
CHEMBL3354190 1 -
CHEMBL3354191 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3352835 Ki = 16.0 nM 7.80
CHEMBL3354186 Ki = 36.0 nM 7.44
CHEMBL3354185 Ki = 3100.0 nM 5.51
CHEMBL3354190 Ki > 1000.0 nM -
CHEMBL3354191 Ki > 1000.0 nM -