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Assay Detail

CHEMBL5136187

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

Binding
Binding affinity to JAK2 JH2 V617F mutant (unknown origin) expressed in baculovirus infected Sf9 cells assessed as dissociation constant measured upto 30 mins in presence of tracer by competitive fluorescence polarization assay
6
Total Activities
6
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

Insights on JAK2 Modulation by Potent, Selective, and Cell-Permeable Pseudokinase-Domain Ligands.
Liosi ME, Ippolito JA, Henry SP, Krimmer SG, Newton AS, Cutrona KJ, Olivarez RA, Mohanty J, Schlessinger J, Jorgensen WL.
J Med Chem (2022) 65 : 8380 -8400
PubMed 35653642 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 6 7.09 7.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5191140 1 7.48
CHEMBL5192135 1 7.37
CHEMBL5184259 1 7.30
CHEMBL5196073 1 7.21
CHEMBL5176386 1 6.88
CHEMBL4449644 1 6.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5191140 Kd = 33.0 nM 7.48
CHEMBL5192135 Kd = 43.0 nM 7.37
CHEMBL5184259 Kd = 50.0 nM 7.30
CHEMBL5196073 Kd = 62.0 nM 7.21
CHEMBL5176386 Kd = 131.0 nM 6.88
CHEMBL4449644 Kd = 478.0 nM 6.32