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Assay Detail

CHEMBL822543

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

Binding
Inhibitory activity was determined against human alpha IIb beta3 integrin
15
Total Activities
15
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-IIb/beta-3 (CHEMBL2093869)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Discovery of a potent and selective alpha v beta 3 integrin antagonist with strong inhibitory activity against neointima formation in rat balloon injury model.
Iwama S, Kitano T, Fukuya F, Honda Y, Sato Y, Notake M, Morie T.
Bioorg Med Chem Lett (2004) 14 : 2567 -2570
PubMed 15109653 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.61 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL86094 1 7.52
CHEMBL86321 1 7.06
CHEMBL87688 1 6.47
CHEMBL84578 1 6.27
CHEMBL312929 1 6.18
CHEMBL87130 1 6.14
CHEMBL407984 1 -
CHEMBL314636 1 -
CHEMBL84683 1 -
CHEMBL431208 1 -
CHEMBL315956 1 -
CHEMBL85196 1 -
CHEMBL84911 1 -
CHEMBL87372 1 -
CHEMBL313045 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL86094 IC50 = 30.0 nM 7.52
CHEMBL86321 IC50 = 88.0 nM 7.06
CHEMBL87688 IC50 = 340.0 nM 6.47
CHEMBL84578 IC50 = 540.0 nM 6.27
CHEMBL312929 IC50 = 660.0 nM 6.18
CHEMBL87130 IC50 = 720.0 nM 6.14
CHEMBL407984 IC50 > 1000.0 nM -
CHEMBL314636 IC50 > 1000.0 nM -
CHEMBL84683 IC50 > 1000.0 nM -
CHEMBL431208 IC50 > 1000.0 nM -
CHEMBL315956 IC50 > 1000.0 nM -
CHEMBL85196 IC50 > 1000.0 nM -
CHEMBL84911 IC50 > 1000.0 nM -
CHEMBL87372 IC50 > 1000.0 nM -
CHEMBL313045 IC50 > 1000.0 nM -