Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1786466

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

Functional
Antagonist activity at alphavbeta3 integrin receptor human VSMC assessed as inhibition of vitronectin-induced cell adhesion
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Integrin alpha-V/beta-3 (CHEMBL1907598)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Improvement in aqueous solubility in small molecule drug discovery programs by disruption of molecular planarity and symmetry.
Ishikawa M, Hashimoto Y.
J Med Chem (2011) 54 : 1539 -1554
PubMed 21344906 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.99 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1782662 1 7.80
CHEMBL599138 1 7.51
CHEMBL599119 1 7.32
CHEMBL1782663 1 7.28
CHEMBL1782660 1 7.28
CHEMBL1782661 1 7.14
CHEMBL1083695 1 6.96
CHEMBL598737 1 6.72
CHEMBL1782659 1 6.41
CHEMBL1782657 1 6.28
CHEMBL1782658 1 6.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1782662 IC50 = 16.0 nM 7.80
CHEMBL599138 IC50 = 31.0 nM 7.51
CHEMBL599119 IC50 = 48.0 nM 7.32
CHEMBL1782663 IC50 = 52.0 nM 7.28
CHEMBL1782660 IC50 = 53.0 nM 7.28
CHEMBL1782661 IC50 = 72.0 nM 7.14
CHEMBL1083695 IC50 = 110.0 nM 6.96
CHEMBL598737 IC50 = 190.0 nM 6.72
CHEMBL1782659 IC50 = 390.0 nM 6.41
CHEMBL1782657 IC50 = 530.0 nM 6.28
CHEMBL1782658 IC50 = 660.0 nM 6.18