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Assay Detail

CHEMBL4251841

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

Binding
Inhibition of TYK2 JH2 domain in IL23-stimulated human Kit225 T cells by luciferase reporter assay
24
Total Activities
24
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 imidazo[1,2-<i>b</i>]pyridazine TYK2 pseudokinase ligands as potent and selective allosteric inhibitors of TYK2 signalling.
Moslin R, Gardner D, Santella J, Zhang Y, Duncia JV, Liu C, Lin J, Tokarski JS, Strnad J, Pedicord D, Chen J, Blat Y, Zupa-Fernandez A, Cheng L, Sun H, Chaudhry C, Huang C, D'Arienzo C, Sack JS, Muckelbauer JK, Chang C, Tredup J, Xie D, Aranibar N, Burke JR, Carter PH, Weinstein DS.
Medchemcomm (2017) 8 : 700 -712
PubMed 30108788 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 6.22 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4285841 1 7.70
CHEMBL4287761 1 7.16
CHEMBL4279157 1 7.00
CHEMBL4293907 1 6.96
CHEMBL4295039 1 6.82
CHEMBL4279883 1 6.62
CHEMBL4291200 1 6.52
CHEMBL4289426 1 6.52
CHEMBL4291611 1 6.48
CHEMBL4293510 1 6.39
CHEMBL4278757 1 6.32
CHEMBL4283351 1 6.29
CHEMBL4287081 1 6.22
CHEMBL4285755 1 6.16
CHEMBL4290130 1 6.11
CHEMBL4287153 1 6.00
CHEMBL4293619 1 5.96
CHEMBL4281304 1 5.92
CHEMBL4289875 1 5.85
CHEMBL4283724 1 5.47
CHEMBL4286006 1 5.31
CHEMBL4282627 1 5.21
CHEMBL4285530 1 5.14
CHEMBL4289149 1 5.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4285841 IC50 = 20.0 nM 7.70
CHEMBL4287761 IC50 = 70.0 nM 7.16
CHEMBL4279157 IC50 = 100.0 nM 7.00
CHEMBL4293907 IC50 = 110.0 nM 6.96
CHEMBL4295039 IC50 = 150.0 nM 6.82
CHEMBL4279883 IC50 = 240.0 nM 6.62
CHEMBL4291200 IC50 = 300.0 nM 6.52
CHEMBL4289426 IC50 = 300.0 nM 6.52
CHEMBL4291611 IC50 = 330.0 nM 6.48
CHEMBL4293510 IC50 = 410.0 nM 6.39
CHEMBL4278757 IC50 = 480.0 nM 6.32
CHEMBL4283351 IC50 = 510.0 nM 6.29
CHEMBL4287081 IC50 = 600.0 nM 6.22
CHEMBL4285755 IC50 = 700.0 nM 6.16
CHEMBL4290130 IC50 = 780.0 nM 6.11
CHEMBL4287153 IC50 = 1000.0 nM 6.00
CHEMBL4293619 IC50 = 1100.0 nM 5.96
CHEMBL4281304 IC50 = 1200.0 nM 5.92
CHEMBL4289875 IC50 = 1400.0 nM 5.85
CHEMBL4283724 IC50 = 3400.0 nM 5.47
CHEMBL4286006 IC50 = 4900.0 nM 5.31
CHEMBL4282627 IC50 = 6200.0 nM 5.21
CHEMBL4285530 IC50 = 7300.0 nM 5.14
CHEMBL4289149 IC50 = 8200.0 nM 5.09