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Assay Detail

CHEMBL4377380

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

Binding
Inhibition of JAK1/TYK2 in human Kit225 T cells assessed as inhibition of STAT phosphorylation by luciferase reporter assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

JAK1/TYK2 (CHEMBL3301391)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165.
Wrobleski ST, Moslin R, Lin S, Zhang Y, Spergel S, Kempson J, Tokarski JS, Strnad J, Zupa-Fernandez A, Cheng L, Shuster D, Gillooly K, Yang X, Heimrich E, McIntyre KW, Chaudhry C, Khan J, Ruzanov M, Tredup J, Mulligan D, Xie D, Sun H, Huang C, D'Arienzo C, Aranibar N, Chiney M, Chimalakonda A, Pitts WJ, Lombardo L, Carter PH, Burke JR, Weinstein DS.
J Med Chem (2019) 62 : 8973 -8995
PubMed 31318208 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 7.48 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4557190 1 8.40
CHEMBL4435170 DEUCRAVACITINIB 4.0 1 8.30
CHEMBL4469750 1 8.22
CHEMBL4457060 1 8.15
CHEMBL4571117 1 8.10
CHEMBL4572855 1 8.10
CHEMBL4566158 1 8.05
CHEMBL4580625 1 7.92
CHEMBL4559585 1 7.92
CHEMBL4443834 1 7.92
CHEMBL4476261 1 7.85
CHEMBL4565054 1 7.82
CHEMBL4543984 1 7.82
CHEMBL4435079 1 7.80
CHEMBL4474729 1 7.66
CHEMBL4441840 1 7.55
CHEMBL4537259 1 7.52
CHEMBL4587924 1 7.47
CHEMBL4468025 1 7.33
CHEMBL4578980 1 7.29
CHEMBL4582205 1 7.20
CHEMBL4527672 1 7.19
CHEMBL4572426 1 7.16
CHEMBL4524832 1 7.11
CHEMBL4577224 1 6.89
CHEMBL4439617 1 6.66
CHEMBL4534832 1 6.31
CHEMBL4581296 1 6.03
CHEMBL4543090 1 5.12
CHEMBL4530035 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4557190 IC50 = 4.0 nM 8.40
CHEMBL4435170 DEUCRAVACITINIB IC50 = 5.0 nM 8.30
CHEMBL4469750 IC50 = 6.0 nM 8.22
CHEMBL4457060 IC50 = 7.0 nM 8.15
CHEMBL4571117 IC50 = 8.0 nM 8.10
CHEMBL4572855 IC50 = 8.0 nM 8.10
CHEMBL4566158 IC50 = 9.0 nM 8.05
CHEMBL4580625 IC50 = 12.0 nM 7.92
CHEMBL4559585 IC50 = 12.0 nM 7.92
CHEMBL4443834 IC50 = 12.0 nM 7.92
CHEMBL4476261 IC50 = 14.0 nM 7.85
CHEMBL4565054 IC50 = 15.0 nM 7.82
CHEMBL4543984 IC50 = 15.0 nM 7.82
CHEMBL4435079 IC50 = 16.0 nM 7.80
CHEMBL4474729 IC50 = 22.0 nM 7.66
CHEMBL4441840 IC50 = 28.0 nM 7.55
CHEMBL4537259 IC50 = 30.0 nM 7.52
CHEMBL4587924 IC50 = 34.0 nM 7.47
CHEMBL4468025 IC50 = 47.0 nM 7.33
CHEMBL4578980 IC50 = 51.0 nM 7.29
CHEMBL4582205 IC50 = 63.0 nM 7.20
CHEMBL4527672 IC50 = 64.0 nM 7.19
CHEMBL4572426 IC50 = 70.0 nM 7.16
CHEMBL4524832 IC50 = 78.0 nM 7.11
CHEMBL4577224 IC50 = 130.0 nM 6.89
CHEMBL4439617 IC50 = 220.0 nM 6.66
CHEMBL4534832 IC50 = 490.0 nM 6.31
CHEMBL4581296 IC50 = 930.0 nM 6.03
CHEMBL4543090 IC50 = 7500.0 nM 5.12
CHEMBL4530035 IC50 > 10000.0 nM -