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Assay Detail

CHEMBL5384077

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

Binding
Agonist activity at alpha5beta1 integrin receptor in human K562 cells assessed as inhibition of fibronectin-induced cell adhesion pre-incubated for 30 mins followed by 1 hr incubation in fibronectin coated wells by fluorescence plate reader assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type K562
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Integrin alpha-5/beta-1 (CHEMBL2095226)
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 8 6.83 8.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4586928 1 8.01
CHEMBL5417237 1 6.78
CHEMBL5395825 1 5.71
CHEMBL5408335 1 -
CHEMBL88478 1 -
CHEMBL4589062 1 -
CHEMBL5410616 1 -
CHEMBL5419935 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4586928 EC50 = 9.7 nM 8.01
CHEMBL5417237 EC50 = 168.0 nM 6.78
CHEMBL5395825 EC50 = 1950.0 nM 5.71
CHEMBL5408335 EC50 > 5000.0 nM -
CHEMBL88478 EC50 > 5000.0 nM -
CHEMBL4589062 EC50 > 5000.0 nM -
CHEMBL5410616 EC50 > 5000.0 nM -
CHEMBL5419935 EC50 > 5000.0 nM -