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Assay Detail

CHEMBL4261269

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

Binding
Inhibition of TYK2 (unknown origin) preincubated for 20 mins followed by [33P]-ATP addition measured after 2 hrs by filter-binding method
23
Total Activities
23
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

Application of Sequential Palladium Catalysis for the Discovery of Janus Kinase Inhibitors in the Benzo[ c]pyrrolo[2,3- h][1,6]naphthyridin-5-one (BPN) Series.
Elsayed MSA, Nielsen JJ, Park S, Park J, Liu Q, Kim CH, Pommier Y, Agama K, Low PS, Cushman M.
J Med Chem (2018) 61 : 10440 -10462
PubMed 30460842 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 7.03 8.71

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4295151 1 8.71
CHEMBL4291720 1 8.65
CHEMBL4290597 1 8.36
CHEMBL4281080 1 8.08
CHEMBL221959 TOFACITINIB 4.0 1 7.98
CHEMBL4286762 1 7.76
CHEMBL4278842 1 7.74
CHEMBL4291298 1 7.49
CHEMBL4284499 1 7.40
CHEMBL4287893 1 7.35
CHEMBL4286103 1 7.13
CHEMBL4283458 1 6.78
CHEMBL4279991 1 6.75
CHEMBL4281492 1 6.59
CHEMBL4289532 1 6.56
CHEMBL4278853 1 6.47
CHEMBL4280783 1 6.37
CHEMBL4288673 1 6.15
CHEMBL4294002 1 5.93
CHEMBL4289375 1 5.82
CHEMBL4277379 1 5.32
CHEMBL4282720 1 5.24
CHEMBL4285332 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4295151 IC50 = 1.93 nM 8.71
CHEMBL4291720 IC50 = 2.24 nM 8.65
CHEMBL4290597 IC50 = 4.35 nM 8.36
CHEMBL4281080 IC50 = 8.38 nM 8.08
CHEMBL221959 TOFACITINIB IC50 = 10.38 nM 7.98
CHEMBL4286762 IC50 = 17.4 nM 7.76
CHEMBL4278842 IC50 = 18.42 nM 7.74
CHEMBL4291298 IC50 = 32.39 nM 7.49
CHEMBL4284499 IC50 = 39.43 nM 7.40
CHEMBL4287893 IC50 = 45.1 nM 7.35
CHEMBL4286103 IC50 = 73.66 nM 7.13
CHEMBL4283458 IC50 = 166.85 nM 6.78
CHEMBL4279991 IC50 = 176.3 nM 6.75
CHEMBL4281492 IC50 = 256.5 nM 6.59
CHEMBL4289532 IC50 = 273.4 nM 6.56
CHEMBL4278853 IC50 = 336.3 nM 6.47
CHEMBL4280783 IC50 = 427.45 nM 6.37
CHEMBL4288673 IC50 = 708.65 nM 6.15
CHEMBL4294002 IC50 = 1163.5 nM 5.93
CHEMBL4289375 IC50 = 1502.0 nM 5.82
CHEMBL4277379 IC50 = 4766.0 nM 5.32
CHEMBL4282720 IC50 = 5730.0 nM 5.24
CHEMBL4285332 IC50 > 1000.0 nM -