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Assay Detail

CHEMBL4323767

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

Binding
Antagonist activity at alpha5beta1 integrin receptor in human K562 cells assessed as reduction in fibronectin-induced cell adhesion pre-incubated for 30 mins
6
Total Activities
6
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

Could Dissecting the Molecular Framework of β-Lactam Integrin Ligands Enhance Selectivity?
Martelli G, Baiula M, Caligiana A, Galletti P, Gentilucci L, Artali R, Spampinato S, Giacomini D.
J Med Chem (2019) 62 : 10156 -10166
PubMed 31670514 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.50 7.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4575577 1 7.38
CHEMBL4593469 1 7.01
CHEMBL4461668 1 6.80
CHEMBL4534088 1 6.38
CHEMBL4585226 1 5.96
CHEMBL4454796 1 5.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4575577 IC50 = 41.5 nM 7.38
CHEMBL4593469 IC50 = 96.9 nM 7.01
CHEMBL4461668 IC50 = 158.0 nM 6.80
CHEMBL4534088 IC50 = 419.0 nM 6.38
CHEMBL4585226 IC50 = 1110.0 nM 5.96
CHEMBL4454796 IC50 = 3512.0 nM 5.45