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Assay Detail

CHEMBL828581

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

Binding
Inhibition of VLA-4 receptor of Jurkat cells in BURJ assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Jurkat
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Integrin alpha-4/beta-1 (CHEMBL1907599)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Influence of acid surrogates toward potency of VLA-4 antagonist.
Venkatraman S, Lim J, Cramer M, Gardner MF, James J, Alves K, Lingham RB, Mumford RA, Munoz B.
Bioorg Med Chem Lett (2005) 15 : 4053 -4056
PubMed 16039122 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.99 10.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL296804 1 10.52
CHEMBL373343 1 8.22
CHEMBL263565 1 8.00
CHEMBL190640 1 7.96
CHEMBL365145 1 7.92
CHEMBL366117 1 7.89
CHEMBL366338 1 7.70
CHEMBL190761 1 7.22
CHEMBL370943 1 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL296804 IC50 = 0.03 nM 10.52
CHEMBL373343 IC50 = 6.0 nM 8.22
CHEMBL263565 IC50 = 10.0 nM 8.00
CHEMBL190640 IC50 = 11.0 nM 7.96
CHEMBL365145 IC50 = 12.0 nM 7.92
CHEMBL366117 IC50 = 13.0 nM 7.89
CHEMBL366338 IC50 = 20.0 nM 7.70
CHEMBL190761 IC50 = 60.0 nM 7.22
CHEMBL370943 IC50 = 300.0 nM 6.52