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Assay Detail

CHEMBL5384075

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

Binding
Agonist activity at alpha1beta2 integrin receptor in human Jurkat E6.1 cells assessed as inhibition of ICAM-1-induced cell adhesion pre-incubated for 30 mins followed by 30 mins incubation in ICAM-1 coated wells by fluorescence plate reader assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Jurkat E6.1
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Integrin alpha1/beta2 complex (CHEMBL5465394)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Design and Pharmacological Characterization of α<sub>4</sub>β<sub>1</sub> Integrin Cyclopeptide Agonists: Computational Investigation of Ligand Determinants for Agonism versus Antagonism.
Anselmi M, Baiula M, Spampinato S, Artali R, He T, Gentilucci L.
J Med Chem (2023) 66 : 5021 -5040
PubMed 36976921 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 7.01 7.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5410616 1 7.01
CHEMBL4586928 1 -
CHEMBL4589062 1 -
CHEMBL5417237 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5410616 EC50 = 98.2 nM 7.01
CHEMBL4586928 EC50 > 5000.0 nM -
CHEMBL4589062 EC50 > 5000.0 nM -
CHEMBL5417237 EC50 > 5000.0 nM -