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Assay Detail

CHEMBL4377385

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Binding
Inhibition of human ERG by in vitro patch clamp method
7
Total Activities
7
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

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 7 4.80 5.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4469750 1 5.17
CHEMBL4559585 1 4.80
CHEMBL4557190 1 4.42
CHEMBL4435170 DEUCRAVACITINIB 4.0 1 -
CHEMBL4580625 1 -
CHEMBL4476261 1 -
CHEMBL4571117 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4469750 IC50 = 6700.0 nM 5.17
CHEMBL4559585 IC50 = 16000.0 nM 4.80
CHEMBL4557190 IC50 = 38000.0 nM 4.42
CHEMBL4435170 DEUCRAVACITINIB IC50 > 80000.0 nM -
CHEMBL4580625 IC50 > 80000.0 nM -
CHEMBL4476261 IC50 > 80000.0 nM -
CHEMBL4571117 IC50 > 80000.0 nM -