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Assay Detail

CHEMBL4775527

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

Binding
Inhibition of TYK2 JH2 domain (unknown origin) by HTRF assay
28
Total Activities
28
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

Discovery of BMS-986202: A Clinical Tyk2 Inhibitor that Binds to Tyk2 JH2.
Liu C,Lin J,Langevine C,Smith D,Li J,Tokarski JS,Khan J,Ruzanov M,Strnad J,Zupa-Fernandez A,Cheng L,Gillooly KM,Shuster D,Zhang Y,Thankappan A,McIntyre KW,Chaudhry C,Elzinga PA,Chiney M,Chimalakonda A,Lombardo LJ,Macor JE,Carter PH,Burke JR,Weinstein DS
J Med Chem (2021) 64 : 677 -694
PubMed 33370104 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 9.21 9.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4789639 BMS-986202 1.0 1 9.72
CHEMBL4435170 DEUCRAVACITINIB 4.0 1 9.70
CHEMBL4793760 1 9.60
CHEMBL4799019 1 9.60
CHEMBL4780233 1 9.57
CHEMBL4799559 1 9.52
CHEMBL4777175 1 9.36
CHEMBL4796821 1 9.32
CHEMBL4799031 1 9.32
CHEMBL4782449 1 9.30
CHEMBL4784838 1 9.29
CHEMBL4792780 1 9.28
CHEMBL4780315 1 9.27
CHEMBL4797596 1 9.15
CHEMBL4785957 1 8.92
CHEMBL4777648 1 8.89
CHEMBL4776752 1 8.85
CHEMBL4788122 1 8.85
CHEMBL4799830 1 8.80
CHEMBL4784391 1 8.72
CHEMBL4780057 1 8.35
CHEMBL4777528 1 -
CHEMBL4785512 1 -
CHEMBL4800399 1 -
CHEMBL4792694 1 -
CHEMBL4789015 1 -
CHEMBL4795231 1 -
CHEMBL4792231 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4789639 BMS-986202 IC50 = 0.19 nM 9.72
CHEMBL4435170 DEUCRAVACITINIB IC50 = 0.2 nM 9.70
CHEMBL4793760 IC50 = 0.25 nM 9.60
CHEMBL4799019 IC50 = 0.25 nM 9.60
CHEMBL4780233 IC50 = 0.27 nM 9.57
CHEMBL4799559 IC50 = 0.3 nM 9.52
CHEMBL4777175 IC50 = 0.44 nM 9.36
CHEMBL4796821 IC50 = 0.48 nM 9.32
CHEMBL4799031 IC50 = 0.48 nM 9.32
CHEMBL4782449 IC50 = 0.5 nM 9.30
CHEMBL4784838 IC50 = 0.51 nM 9.29
CHEMBL4792780 IC50 = 0.52 nM 9.28
CHEMBL4780315 IC50 = 0.54 nM 9.27
CHEMBL4797596 IC50 = 0.71 nM 9.15
CHEMBL4785957 IC50 = 1.2 nM 8.92
CHEMBL4777648 IC50 = 1.3 nM 8.89
CHEMBL4776752 IC50 = 1.4 nM 8.85
CHEMBL4788122 IC50 = 1.4 nM 8.85
CHEMBL4799830 IC50 = 1.6 nM 8.80
CHEMBL4784391 IC50 = 1.9 nM 8.72
CHEMBL4780057 IC50 = 4.5 nM 8.35
CHEMBL4777528 IC50 < 0.25 nM -
CHEMBL4785512 IC50 < 0.25 nM -
CHEMBL4800399 IC50 < 0.25 nM -
CHEMBL4792694 IC50 < 0.25 nM -
CHEMBL4789015 IC50 < 0.25 nM -
CHEMBL4795231 IC50 < 0.25 nM -
CHEMBL4792231 IC50 < 0.25 nM -