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Assay Detail

CHEMBL4359664

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

Binding
Binding affinity to human C-terminal thrombin cleavage site-fused/6xHis-tagged JAK2 JH2 pseudokinase domain W777A/F974AH/V617F triple mutant (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 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 6.38 6.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4525245 1 6.64
CHEMBL4476380 1 6.40
CHEMBL4449644 1 6.37
CHEMBL191003 JNJ-7706621 1 6.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4525245 Kd = 230.0 nM 6.64
CHEMBL4476380 Kd = 400.0 nM 6.40
CHEMBL4449644 Kd = 430.0 nM 6.37
CHEMBL191003 JNJ-7706621 Kd = 820.0 nM 6.09