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Assay Detail

CHEMBL4359666

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

Binding
Inhibition of wild type full length human JAK2 (1 to 1132 residues) autophosphorylation expressed in HEK293T cells incubated in buffer with compound for 1 hr followed by treatment with enzyme and [gamma32P]-ATP for 15 mins by immunoprecipitation assay based autoradiography
3
Total Activities
2
Compounds Tested
2
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

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
IC50 2 4.93 5.53
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL191003 JNJ-7706621 2 5.53
CHEMBL4476380 1 4.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL191003 JNJ-7706621 IC50 = 2960.0 nM 5.53
CHEMBL4476380 IC50 = 46530.0 nM 4.33
CHEMBL191003 JNJ-7706621 Inhibition - % -