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Assay Detail

CHEMBL1120950

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

Binding
Inhibition of LFA1-mediated IL2 mRNA level in SEB-stimulated human whole blood measured after 6 hrs post stimulation by RT-PCR analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Blood
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Integrin alpha-L (CHEMBL1803)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Small molecule antagonist of leukocyte function associated antigen-1 (LFA-1): structure-activity relationships leading to the identification of 6-((5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]nonan-7-yl)nicotinic acid (BMS-688521).
Watterson SH, Xiao Z, Dodd DS, Tortolani DR, Vaccaro W, Potin D, Launay M, Stetsko DK, Skala S, Davis PM, Lee D, Yang X, McIntyre KW, Balimane P, Patel K, Yang Z, Marathe P, Kadiyala P, Tebben AJ, Sheriff S, Chang CY, Ziemba T, Zhang H, Chen BC, DelMonte AJ, Aranibar N, McKinnon M, Barrish JC, Suchard SJ, Murali Dhar TG.
J Med Chem (2010) 53 : 3814 -3830
PubMed 20405922 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.56 6.56

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL214529 1 6.56
CHEMBL1098726 1 6.56

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL214529 IC50 = 276.0 nM 6.56
CHEMBL1098726 IC50 = 276.0 nM 6.56