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Assay Detail

CHEMBL4685307

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

Binding
Inhibition of JAK3 in mouse T cells assessed as reduction in IL2-stimulated cell proliferation measured after 72 hrs by MTS assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type T cell
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Tyrosine-protein kinase JAK3 (CHEMBL5250)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Design, synthesis, and pharmacological evaluation of 4- or 6-phenyl-pyrimidine derivatives as novel and selective Janus kinase 3 inhibitors.
Shu L,Chen C,Huan X,Huang H,Wang M,Zhang J,Yan Y,Liu J,Zhang T,Zhang D
Eur J Med Chem (2020) 191 : 112148 -112148
PubMed 32097841 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.68 6.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4746272 1 6.11
CHEMBL221959 TOFACITINIB 4.0 1 5.82
CHEMBL4750184 1 5.68
CHEMBL4780984 1 5.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4746272 IC50 = 770.0 nM 6.11
CHEMBL221959 TOFACITINIB IC50 = 1500.0 nM 5.82
CHEMBL4750184 IC50 = 2110.0 nM 5.68
CHEMBL4780984 IC50 = 7500.0 nM 5.12