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Assay Detail

CHEMBL4031306

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Binding
Binding affinity to N-terminal His tagged human recombinant JAK2 (1014 to 1132 residues) expressed in Escherichia coli after 60 to 90 mins by LC/MS analysis
10
Total Activities
10
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

Tyrosine-protein kinase JAK2 (CHEMBL2971)
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
Kd 10 5.35 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4098975 1 6.00
CHEMBL4084049 1 5.70
CHEMBL4091233 1 5.70
CHEMBL4069283 1 5.70
CHEMBL4060201 1 5.30
CHEMBL4089113 1 5.30
CHEMBL4060602 1 5.22
CHEMBL4088824 1 5.00
CHEMBL1630770 1 4.26
CHEMBL4070306 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4098975 Kd = 1000.0 nM 6.00
CHEMBL4084049 Kd = 2000.0 nM 5.70
CHEMBL4091233 Kd = 2000.0 nM 5.70
CHEMBL4069283 Kd = 2000.0 nM 5.70
CHEMBL4060201 Kd = 5000.0 nM 5.30
CHEMBL4089113 Kd = 5000.0 nM 5.30
CHEMBL4060602 Kd = 6000.0 nM 5.22
CHEMBL4088824 Kd = 10000.0 nM 5.00
CHEMBL1630770 Kd = 55000.0 nM 4.26
CHEMBL4070306 Kd < 1000.0 nM -