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Assay Detail

CHEMBL816229

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

Binding
Displacement of vitronectin from human integrin alphaV-beta5
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Integrin alpha-V/beta-5 (CHEMBL2096675)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Substituted benzocyloheptenes as potent and selective alpha(v) integrin antagonists.
Perron-Sierra F, Saint Dizier D, Bertrand M, Genton A, Tucker GC, Casara P.
Bioorg Med Chem Lett (2002) 12 : 3291 -3296
PubMed 12392735 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 8.64 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL109930 1 10.00
CHEMBL327102 1 9.70
CHEMBL109703 1 9.52
CHEMBL113063 1 9.30
CHEMBL113853 1 9.10
CHEMBL111401 1 9.05
CHEMBL110039 1 7.70
CHEMBL109817 1 7.66
CHEMBL111986 1 7.40
CHEMBL421890 1 6.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL109930 IC50 = 0.1 nM 10.00
CHEMBL327102 IC50 = 0.2 nM 9.70
CHEMBL109703 IC50 = 0.3 nM 9.52
CHEMBL113063 IC50 = 0.5 nM 9.30
CHEMBL113853 IC50 = 0.8 nM 9.10
CHEMBL111401 IC50 = 0.9 nM 9.05
CHEMBL110039 IC50 = 20.0 nM 7.70
CHEMBL109817 IC50 = 22.0 nM 7.66
CHEMBL111986 IC50 = 40.0 nM 7.40
CHEMBL421890 IC50 = 119.0 nM 6.92