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Assay Detail

CHEMBL821412

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

Functional
Antagonistic activity against VLA-4 integrin of human jurkat cells using [125I]VCAM-Ig as radioligand
ChEMBL ↗
51
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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

The discovery of sulfonylated dipeptides as potent VLA-4 antagonists.
Hagmann WK, Durette PL, Lanza T, Kevin NJ, de Laszlo SE, Kopka IE, Young D, Magriotis PA, Li B, Lin LS, Yang G, Kamenecka T, Chang LL, Wilson J, MacCoss M, Mills SG, Van Riper G, McCauley E, Egger LA, Kidambi U, Lyons K, Vincent S, Stearns R, Colletti A, Teffera J, Tong S, Fenyk-Melody J, Owens K, Levorse D, Kim P, Schmidt JA, Mumford RA.
Bioorg Med Chem Lett (2001) 11 : 2709 -2713
PubMed 11591507 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 51 9.26 10.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL309823 — — 1 10.15
CHEMBL56511 — — 1 10.10
CHEMBL76119 — — 1 10.10
CHEMBL91402 — — 1 10.05
CHEMBL91737 — — 1 10.05
CHEMBL330687 — — 1 10.00
CHEMBL423683 — — 1 10.00
CHEMBL91877 — — 1 9.96
CHEMBL424616 — — 1 9.89
CHEMBL91485 — — 1 9.89
CHEMBL88478 — — 1 9.89
CHEMBL90637 — — 1 9.85
CHEMBL330525 — — 1 9.85
CHEMBL91061 — — 1 9.82
CHEMBL90198 — — 1 9.82
CHEMBL88608 — — 1 9.80
CHEMBL90315 — — 1 9.66
CHEMBL90580 — — 1 9.66
CHEMBL91775 — — 1 9.64
CHEMBL328973 — — 1 9.62
CHEMBL313632 — — 1 9.55
CHEMBL94107 — — 1 9.46
CHEMBL329900 — — 1 9.44
CHEMBL328890 — — 1 9.42
CHEMBL90844 — — 1 9.41
CHEMBL91572 — — 1 9.40
CHEMBL30192 — — 1 9.34
CHEMBL91031 — — 1 9.30
CHEMBL330006 — — 1 9.30
CHEMBL330340 — — 1 9.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL309823 — IC50 = 0.07 nM 10.15
CHEMBL56511 — IC50 = 0.08 nM 10.10
CHEMBL76119 — IC50 = 0.08 nM 10.10
CHEMBL91402 — IC50 = 0.09 nM 10.05
CHEMBL91737 — IC50 = 0.09 nM 10.05
CHEMBL330687 — IC50 = 0.1 nM 10.00
CHEMBL423683 — IC50 = 0.1 nM 10.00
CHEMBL91877 — IC50 = 0.11 nM 9.96
CHEMBL424616 — IC50 = 0.13 nM 9.89
CHEMBL91485 — IC50 = 0.13 nM 9.89
CHEMBL88478 — IC50 = 0.13 nM 9.89
CHEMBL90637 — IC50 = 0.14 nM 9.85
CHEMBL330525 — IC50 = 0.14 nM 9.85
CHEMBL90198 — IC50 = 0.15 nM 9.82
CHEMBL91061 — IC50 = 0.15 nM 9.82
CHEMBL88608 — IC50 = 0.16 nM 9.80
CHEMBL90315 — IC50 = 0.22 nM 9.66
CHEMBL90580 — IC50 = 0.22 nM 9.66
CHEMBL91775 — IC50 = 0.23 nM 9.64
CHEMBL328973 — IC50 = 0.24 nM 9.62
CHEMBL313632 — IC50 = 0.28 nM 9.55
CHEMBL94107 — IC50 = 0.35 nM 9.46
CHEMBL329900 — IC50 = 0.36 nM 9.44
CHEMBL328890 — IC50 = 0.38 nM 9.42
CHEMBL90844 — IC50 = 0.39 nM 9.41
CHEMBL91572 — IC50 = 0.4 nM 9.40
CHEMBL30192 — IC50 = 0.46 nM 9.34
CHEMBL91031 — IC50 = 0.5 nM 9.30
CHEMBL330006 — IC50 = 0.5 nM 9.30
CHEMBL330340 — IC50 = 0.52 nM 9.28
CHEMBL93638 — IC50 = 0.52 nM 9.28
CHEMBL431283 — IC50 = 0.54 nM 9.27
CHEMBL432215 — IC50 = 0.63 nM 9.20
CHEMBL29359 — IC50 = 0.64 nM 9.19
CHEMBL91109 — IC50 = 0.65 nM 9.19
CHEMBL91319 — IC50 = 0.9 nM 9.05
CHEMBL93790 — IC50 = 0.92 nM 9.04
CHEMBL90669 — IC50 = 0.95 nM 9.02
CHEMBL91136 — IC50 = 1.01 nM 9.00
CHEMBL92106 — IC50 = 1.02 nM 8.99
CHEMBL92200 — IC50 = 1.12 nM 8.95
CHEMBL91030 — IC50 = 1.33 nM 8.88
CHEMBL327701 — IC50 = 1.43 nM 8.85
CHEMBL329356 — IC50 = 1.53 nM 8.81
CHEMBL93700 — IC50 = 2.4 nM 8.62
CHEMBL278045 — IC50 = 4.5 nM 8.35
CHEMBL91053 — IC50 = 7.0 nM 8.15
CHEMBL91172 — IC50 = 10.0 nM 8.00
CHEMBL93912 — IC50 = 45.0 nM 7.35
CHEMBL90995 — IC50 = 192.0 nM 6.72