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Assay Detail

CHEMBL3803215

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

Binding
Inhibition of JAK1 (unknown origin)
3
Total Activities
3
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

Design, synthesis and preliminary biological evaluation of 4-aminopyrazole derivatives as novel and potent JAKs inhibitors.
Liang X, Huang Y, Zang J, Gao Q, Wang B, Xu W, Zhang Y.
Bioorg Med Chem (2016) 24 : 2660 -2672
PubMed 27137359 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.12 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2105759 BARICITINIB 4.0 1 8.40
CHEMBL1789941 RUXOLITINIB 4.0 1 8.15
CHEMBL221959 TOFACITINIB 4.0 1 7.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2105759 BARICITINIB IC50 = 4.0 nM 8.40
CHEMBL1789941 RUXOLITINIB IC50 = 7.0 nM 8.15
CHEMBL221959 TOFACITINIB IC50 = 15.0 nM 7.82