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Assay Detail

CHEMBL4714259

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

Binding
Inhibition of recombinant human JAK1 assessed as phosphorylation level in presence of 1 mM ATP
4
Total Activities
4
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 JAK1 (CHEMBL2835)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Small molecule approaches to treat autoimmune and inflammatory diseases (Part I): Kinase inhibitors.
Zheng J,Wu J,Ding X,Shen HC,Zou G
Bioorg Med Chem Lett (2021) 38 : 127862 -127862
PubMed 33609659 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.46 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4782814 1 8.40
CHEMBL4747591 1 7.77
CHEMBL3301607 FILGOTINIB 4.0 1 6.20
CHEMBL4085457 RITLECITINIB 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4782814 IC50 = 4.0 nM 8.40
CHEMBL4747591 IC50 = 17.0 nM 7.77
CHEMBL3301607 FILGOTINIB IC50 = 636.0 nM 6.20
CHEMBL4085457 RITLECITINIB IC50 > 10000.0 nM -