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Assay Detail

CHEMBL4482015

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

Functional
Antiproliferative activity against rat T cells cultured with Concanavalin A for 24 hrs assessed inhibition of IL-2-stimulated cell proliferation after 72 hrs by MTS assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type T-cell
Confidence 1 — Organism
Curated By Autocuration

Target

T-cell (CHEMBL614309)
Type CELL-LINE

Publication

Structure-based design and synthesis of pyrimidine-4,6-diamine derivatives as Janus kinase 3 inhibitors.
Yu RN, Chen CJ, Shu L, Yin Y, Wang ZJ, Zhang TT, Zhang DY.
Bioorg Med Chem (2019) 27 : 1646 -1657
PubMed 30853331 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.72 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL221959 TOFACITINIB 4.0 1 8.70
CHEMBL3601722 1 7.92
CHEMBL4573218 1 7.82
CHEMBL4574614 1 7.39
CHEMBL4546009 1 7.30
CHEMBL4518786 1 7.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL221959 TOFACITINIB IC50 = 2.0 nM 8.70
CHEMBL3601722 IC50 = 12.0 nM 7.92
CHEMBL4573218 IC50 = 15.0 nM 7.82
CHEMBL4574614 IC50 = 41.0 nM 7.39
CHEMBL4546009 IC50 = 50.0 nM 7.30
CHEMBL4518786 IC50 = 64.0 nM 7.19