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Assay Detail

CHEMBL5058466

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

Binding
Inhibition of IL-2 in CD3/CD28 activated human CD4+ve Th cells preincubated for 15 mins followed by addition of immuno-cult and measured after 24 hrs by HTRF assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CD4+ve Th
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Interleukin-2 (CHEMBL5880)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Dual Inhibition of IL-2-Inducible T-Cell Kinase (ITK) and Tropomyosin Receptor Kinase A (TRKA) as Potential Treatment for Atopic Dermatitis and Other Inflammatory and Autoimmune Diseases.
Abdel-Magid AF.
ACS Med Chem Lett (2021) 12 : 1889 -1891
PubMed 34917248 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.27 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5087453 1 8.00
CHEMBL5090091 1 7.89
CHEMBL5088468 1 7.47
CHEMBL5084598 1 7.41
CHEMBL5074957 1 7.33
CHEMBL5079033 1 7.09
CHEMBL5082562 1 7.04
CHEMBL5086824 1 7.02
CHEMBL5080834 1 6.95
CHEMBL5083169 1 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5087453 IC50 = 10.0 nM 8.00
CHEMBL5090091 IC50 = 13.0 nM 7.89
CHEMBL5088468 IC50 = 34.0 nM 7.47
CHEMBL5084598 IC50 = 39.0 nM 7.41
CHEMBL5074957 IC50 = 47.0 nM 7.33
CHEMBL5079033 IC50 = 82.0 nM 7.09
CHEMBL5082562 IC50 = 91.0 nM 7.04
CHEMBL5086824 IC50 = 96.0 nM 7.02
CHEMBL5080834 IC50 = 113.0 nM 6.95
CHEMBL5083169 IC50 = 304.0 nM 6.52