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Assay Detail

CHEMBL3118991

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

Binding
Inhibition of TYK2 (unknown origin)
26
Total Activities
26
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

Anilino-monoindolylmaleimides as potent and selective JAK3 inhibitors.
McDonnell ME, Bian H, Wrobel J, Smith GR, Liang S, Ma H, Reitz AB.
Bioorg Med Chem Lett (2014) 24 : 1116 -1121
PubMed 24461299 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 6.00 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1789941 RUXOLITINIB 4.0 1 9.40
CHEMBL221959 TOFACITINIB 4.0 1 7.62
CHEMBL3114776 1 6.00
CHEMBL1650951 1 5.77
CHEMBL366266 1 5.64
CHEMBL3114775 1 5.29
CHEMBL3114761 1 5.24
CHEMBL3114768 1 5.13
CHEMBL3114772 1 5.01
CHEMBL3114786 1 4.92
CHEMBL3114764 1 -
CHEMBL3114763 1 -
CHEMBL3114762 1 -
CHEMBL3114785 1 -
CHEMBL3114784 1 -
CHEMBL3114783 1 -
CHEMBL3114782 1 -
CHEMBL3114781 1 -
CHEMBL3114765 1 -
CHEMBL3114773 1 -
CHEMBL3114771 1 -
CHEMBL3114770 1 -
CHEMBL3114769 1 -
CHEMBL3114767 1 -
CHEMBL3114766 1 -
CHEMBL3114774 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1789941 RUXOLITINIB IC50 = 0.4 nM 9.40
CHEMBL221959 TOFACITINIB IC50 = 24.0 nM 7.62
CHEMBL3114776 IC50 = 995.0 nM 6.00
CHEMBL1650951 IC50 = 1691.0 nM 5.77
CHEMBL366266 IC50 = 2310.0 nM 5.64
CHEMBL3114775 IC50 = 5104.0 nM 5.29
CHEMBL3114761 IC50 = 5827.0 nM 5.24
CHEMBL3114768 IC50 = 7368.0 nM 5.13
CHEMBL3114772 IC50 = 9844.0 nM 5.01
CHEMBL3114786 IC50 = 11927.0 nM 4.92
CHEMBL3114764 IC50 > 10000.0 nM -
CHEMBL3114763 IC50 > 10000.0 nM -
CHEMBL3114762 IC50 > 10000.0 nM -
CHEMBL3114785 IC50 > 10000.0 nM -
CHEMBL3114784 IC50 > 10000.0 nM -
CHEMBL3114783 IC50 > 10000.0 nM -
CHEMBL3114782 IC50 > 10000.0 nM -
CHEMBL3114781 IC50 > 10000.0 nM -
CHEMBL3114765 IC50 > 10000.0 nM -
CHEMBL3114773 IC50 > 10000.0 nM -
CHEMBL3114771 IC50 > 10000.0 nM -
CHEMBL3114770 IC50 > 10000.0 nM -
CHEMBL3114769 IC50 > 10000.0 nM -
CHEMBL3114767 IC50 > 10000.0 nM -
CHEMBL3114766 IC50 > 10000.0 nM -
CHEMBL3114774 IC50 > 10000.0 nM -