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Assay Detail

CHEMBL824059

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Binding
Inhibitory activity against human alpha V beta3 receptor using SPAV3 assay
15
Total Activities
15
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-3 (CHEMBL1907598)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Non-peptide alphavbeta3 antagonists. Part 6: design and synthesis of alphavbeta3 antagonists containing a pyridone or pyrazinone central scaffold.
Breslin MJ, Duggan ME, Halczenko W, Fernandez-Metzler C, Hunt CA, Leu CT, Merkle KM, Naylor-Olsen AM, Prueksaritanont T, Stump G, Wallace A, Rodan SB, Hutchinson JH.
Bioorg Med Chem Lett (2003) 13 : 1809 -1812
PubMed 12729670 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 8.83 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL51391 1 9.70
CHEMBL53003 1 9.70
CHEMBL51152 1 9.70
CHEMBL54148 1 9.52
CHEMBL300008 1 9.40
CHEMBL301131 1 9.15
CHEMBL53503 1 8.96
CHEMBL53822 1 8.89
CHEMBL53122 1 8.85
CHEMBL54259 1 8.72
CHEMBL301301 1 8.68
CHEMBL299110 1 8.57
CHEMBL53145 1 8.03
CHEMBL301282 1 7.68
CHEMBL50698 1 6.95

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL51391 IC50 = 0.2 nM 9.70
CHEMBL53003 IC50 = 0.2 nM 9.70
CHEMBL51152 IC50 = 0.2 nM 9.70
CHEMBL54148 IC50 = 0.3 nM 9.52
CHEMBL300008 IC50 = 0.4 nM 9.40
CHEMBL301131 IC50 = 0.7 nM 9.15
CHEMBL53503 IC50 = 1.1 nM 8.96
CHEMBL53822 IC50 = 1.3 nM 8.89
CHEMBL53122 IC50 = 1.4 nM 8.85
CHEMBL54259 IC50 = 1.9 nM 8.72
CHEMBL301301 IC50 = 2.1 nM 8.68
CHEMBL299110 IC50 = 2.7 nM 8.57
CHEMBL53145 IC50 = 9.3 nM 8.03
CHEMBL301282 IC50 = 21.0 nM 7.68
CHEMBL50698 IC50 = 112.0 nM 6.95