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Assay Detail

CHEMBL818048

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

Binding
Inhibition of [125I]VCAM-Ig binding to VLA-4 of Jurkat cells in the presence of Mn2+
14
Total Activities
14
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

N-isonicotinoyl-(L)-4-aminophenylalanine derivatives as tight binding VLA-4 antagonists.
Doherty GA, Yang GX, Borges E, Tong S, McCauley ED, Treonz KM, Van Riper G, Pacholok S, Si Q, Koo GC, Shah K, Mumford RA, Hagmann WK.
Bioorg Med Chem Lett (2003) 13 : 1891 -1895
PubMed 12749892 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 9.85 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL56511 1 10.10
CHEMBL298835 1 10.05
CHEMBL56822 1 10.00
CHEMBL292619 1 10.00
CHEMBL296804 1 10.00
CHEMBL294708 1 9.96
CHEMBL293807 1 9.89
CHEMBL293756 1 9.85
CHEMBL59531 1 9.82
CHEMBL55900 1 9.80
CHEMBL56520 1 9.72
CHEMBL440481 1 9.68
CHEMBL53733 1 9.57
CHEMBL1160252 1 9.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL56511 IC50 = 0.08 nM 10.10
CHEMBL298835 IC50 = 0.09 nM 10.05
CHEMBL56822 IC50 = 0.1 nM 10.00
CHEMBL292619 IC50 = 0.1 nM 10.00
CHEMBL296804 IC50 = 0.1 nM 10.00
CHEMBL294708 IC50 = 0.11 nM 9.96
CHEMBL293807 IC50 = 0.13 nM 9.89
CHEMBL293756 IC50 = 0.14 nM 9.85
CHEMBL59531 IC50 = 0.15 nM 9.82
CHEMBL55900 IC50 = 0.16 nM 9.80
CHEMBL56520 IC50 = 0.19 nM 9.72
CHEMBL440481 IC50 = 0.21 nM 9.68
CHEMBL53733 IC50 = 0.27 nM 9.57
CHEMBL1160252 IC50 = 0.36 nM 9.44