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Assay Detail

CHEMBL4359663

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

Binding
Binding affinity to wild type human C-terminal thrombin cleavage site-fused/ 6xHis-tagged JAK2 JH2 pseudokinase domain (536 to 812 residues) expressed in baculovirus infected sf9 insect cells by microscale thermophoresis assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Tyrosine-protein kinase JAK2 (CHEMBL2971)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective Janus Kinase 2 (JAK2) Pseudokinase Ligands with a Diaminotriazole Core.
Liosi ME, Krimmer SG, Newton AS, Dawson TK, Puleo DE, Cutrona KJ, Suzuki Y, Schlessinger J, Jorgensen WL.
J Med Chem (2020) 63 : 5324 -5340
PubMed 32329617 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 4 6.52 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4525245 1 6.70
CHEMBL4449644 1 6.54
CHEMBL4476380 1 6.51
CHEMBL191003 JNJ-7706621 1 6.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4525245 Kd = 200.0 nM 6.70
CHEMBL4449644 Kd = 290.0 nM 6.54
CHEMBL4476380 Kd = 310.0 nM 6.51
CHEMBL191003 JNJ-7706621 Kd = 490.0 nM 6.31