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Assay Detail

CHEMBL948223

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

Binding
Displacement of vitronectin from integrin alphavbeta3 receptor
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Design and synthesis of novel potent and selective integrin alphanubeta3 antagonists--novel synthetic routes to isoquinolinone, benzoxazinone, and quinazolinone acetates.
Seitz W, Geneste H, Backfisch G, Delzer J, Graef C, Hornberger W, Kling A, Subkowski T, Zimmermann N.
Bioorg Med Chem Lett (2008) 18 : 527 -531
PubMed 18068982 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.27 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL256672 1 9.15
CHEMBL269950 1 8.82
CHEMBL256673 1 8.38
CHEMBL404371 1 8.36
CHEMBL255952 1 8.13
CHEMBL258325 1 8.00
CHEMBL269961 1 7.96
CHEMBL401660 1 7.89
CHEMBL255741 1 7.57
CHEMBL258327 1 7.43
CHEMBL271284 1 7.30
CHEMBL402115 1 7.30
CHEMBL273168 1 6.91
CHEMBL442705 1 6.30
CHEMBL271486 1 6.00
CHEMBL257730 1 5.30
CHEMBL273169 1 5.00
CHEMBL255789 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL256672 IC50 = 0.7 nM 9.15
CHEMBL269950 IC50 = 1.5 nM 8.82
CHEMBL256673 IC50 = 4.2 nM 8.38
CHEMBL404371 IC50 = 4.4 nM 8.36
CHEMBL255952 IC50 = 7.4 nM 8.13
CHEMBL258325 IC50 = 10.0 nM 8.00
CHEMBL269961 IC50 = 11.0 nM 7.96
CHEMBL401660 IC50 = 13.0 nM 7.89
CHEMBL255741 IC50 = 27.0 nM 7.57
CHEMBL258327 IC50 = 37.0 nM 7.43
CHEMBL271284 IC50 = 50.0 nM 7.30
CHEMBL402115 IC50 = 50.0 nM 7.30
CHEMBL273168 IC50 = 122.0 nM 6.91
CHEMBL442705 IC50 = 500.0 nM 6.30
CHEMBL271486 IC50 = 1000.0 nM 6.00
CHEMBL257730 IC50 = 5000.0 nM 5.30
CHEMBL273169 IC50 = 10000.0 nM 5.00
CHEMBL255789 IC50 = 10000.0 nM 5.00