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Assay Detail

CHEMBL4031308

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ADMET
Inhibition of human JAK3 using GEEEEYFELVKKKK as substrate in presence of [gamma-33P]-ATP
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Tyrosine-protein kinase JAK3 (CHEMBL2148)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat.
Yao L, Mustafa N, Tan EC, Poulsen A, Singh P, Duong-Thi MD, Lee JXT, Ramanujulu PM, Chng WJ, Yen JJY, Ohlson S, Dymock BW.
J Med Chem (2017) 60 : 8336 -8357
PubMed 28953386 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.31 6.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4095596 1 6.36
CHEMBL4060201 1 6.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4095596 IC50 = 436.0 nM 6.36
CHEMBL4060201 IC50 = 569.0 nM 6.25