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Assay Detail

CHEMBL5369331

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

Binding
Inhibition of N-terminal GST-tagged human recombinant JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 peptide as substrate incubated for 10 mins measured after 90 mins in presence of ATP by caliper mobility shift assay
6
Total Activities
6
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

Discovery of the Potent and Selective Inhaled Janus Kinase 1 Inhibitor AZD4604 and Its Preclinical Characterization.
Nilsson M, Berggren K, Berglund S, Cerboni S, Collins M, Dahl G, Elmqvist D, Grimster NP, Hendrickx R, Johansson JR, Kettle JG, Lepistö M, Rhedin M, Smailagic A, Su Q, Wennberg T, Wu A, Österlund T, Naessens T, Mitra S.
J Med Chem (2023) 66 : 13400 -13415
PubMed 37738648 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.45 6.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5397400 1 6.14
CHEMBL4447181 LONDAMOCITINIB 2.0 1 5.91
CHEMBL5409783 1 5.61
CHEMBL5405817 1 5.17
CHEMBL5410836 1 5.13
CHEMBL5420468 1 4.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5397400 IC50 = 728.0 nM 6.14
CHEMBL4447181 LONDAMOCITINIB IC50 = 1221.0 nM 5.91
CHEMBL5409783 IC50 = 2431.0 nM 5.61
CHEMBL5405817 IC50 = 6838.0 nM 5.17
CHEMBL5410836 IC50 = 7419.0 nM 5.13
CHEMBL5420468 IC50 = 17544.0 nM 4.76