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Assay Detail

CHEMBL867620

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

Binding
Displacement of [125I]echistatin from AlphaV-beta-3 integrin receptor
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

Incorporation of the unusual C(alpha)-fluoroalkylamino acids into cyclopeptides: synthesis of arginine-glycine-aspartate (RGD) analogues and study of their conformational and biological behavior.
Dal Pozzo A, Ni M, Muzi L, de Castiglione R, Mondelli R, Mazzini S, Penco S, Pisano C, Castorina M, Giannini G.
J Med Chem (2006) 49 : 1808 -1817
PubMed 16509596 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.90 7.99

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL380434 1 7.99
CHEMBL413574 1 7.73
CHEMBL429876 CILENGITIDE 3.0 1 7.72
CHEMBL383747 1 7.70
CHEMBL204309 1 7.45
CHEMBL203693 1 7.44
CHEMBL411941 CYCLORGDFV 1 6.71
CHEMBL379056 1 6.62
CHEMBL203077 1 6.54
CHEMBL2371899 1 6.48
CHEMBL381590 1 6.15
CHEMBL377066 1 5.99
CHEMBL381589 1 5.14
CHEMBL203930 1 -
CHEMBL409143 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL380434 IC50 = 10.31 nM 7.99
CHEMBL413574 IC50 = 18.8 nM 7.73
CHEMBL429876 CILENGITIDE IC50 = 18.9 nM 7.72
CHEMBL383747 IC50 = 19.75 nM 7.70
CHEMBL204309 IC50 = 35.5 nM 7.45
CHEMBL203693 IC50 = 36.3 nM 7.44
CHEMBL411941 CYCLORGDFV IC50 = 195.9 nM 6.71
CHEMBL379056 IC50 = 237.1 nM 6.62
CHEMBL203077 IC50 = 285.3 nM 6.54
CHEMBL2371899 IC50 = 331.8 nM 6.48
CHEMBL381590 IC50 = 704.4 nM 6.15
CHEMBL377066 IC50 = 1017.8 nM 5.99
CHEMBL381589 IC50 = 7237.9 nM 5.14
CHEMBL203930 IC50 > 1000.0 nM -
CHEMBL409143 IC50 > 1000.0 nM -