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Assay Detail

CHEMBL5245512

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

Binding
Inhibition of JAK2 (unknown origin)
8
Total Activities
8
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

Janus kinases (JAKs): The efficient therapeutic targets for autoimmune diseases and myeloproliferative disorders.
Xu P, Shen P, Yu B, Xu X, Ge R, Cheng X, Chen Q, Bian J, Li Z, Wang J.
Eur J Med Chem (2020) 192 : 112155 -112155
PubMed 32120325 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.94 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL21156 1 9.00
CHEMBL495727 AT-9283 2.0 1 8.92
CHEMBL1287853 FEDRATINIB 4.0 1 8.52
CHEMBL4116008 CERDULATINIB 2.0 1 8.22
CHEMBL1995703 1 8.22
CHEMBL3622820 ITACITINIB 3.0 1 7.20
CHEMBL3301606 SOLCITINIB 2.0 1 6.97
CHEMBL4564280 1 6.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL21156 IC50 = 1.0 nM 9.00
CHEMBL495727 AT-9283 IC50 = 1.2 nM 8.92
CHEMBL1287853 FEDRATINIB IC50 = 3.0 nM 8.52
CHEMBL4116008 CERDULATINIB IC50 = 6.0 nM 8.22
CHEMBL1995703 IC50 = 6.0 nM 8.22
CHEMBL3622820 ITACITINIB IC50 = 63.0 nM 7.20
CHEMBL3301606 SOLCITINIB IC50 = 107.8 nM 6.97
CHEMBL4564280 IC50 = 343.0 nM 6.46