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Assay Detail

CHEMBL824551

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

Binding
Inhibition of platelet aggregation in human platelet-rich plasma alpha IIb beta-3 integrin to assess the selectivity for the alpha-v beta-3 over the GPIIb/IIIa integrin receptor
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Plasma
Confidence 4 — Cell-line / Tissue
Curated By Expert

Target

Integrin alpha-V/beta-3 and alpha-IIb/beta 3 (CHEMBL2111443)
Type SELECTIVITY GROUP
Organism Homo sapiens

Publication

Synthesis and biological evaluation of nonpeptide integrin antagonists containing spirocyclic scaffolds.
Smallheer JM, Weigelt CA, Woerner FJ, Wells JS, Daneker WF, Mousa SA, Wexler RR, Jadhav PK.
Bioorg Med Chem Lett (2004) 14 : 383 -387
PubMed 14698164 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 5.42 6.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL338865 1 6.51
CHEMBL127525 1 6.31
CHEMBL127377 1 6.10
CHEMBL126925 1 6.08
CHEMBL340703 1 6.00
CHEMBL126416 1 5.85
CHEMBL339751 1 5.25
CHEMBL419795 1 5.15
CHEMBL340309 1 5.14
CHEMBL126341 1 5.14
CHEMBL127492 1 5.08
CHEMBL127133 1 5.08
CHEMBL2111839 1 5.04
CHEMBL126983 1 4.96
CHEMBL339476 1 4.48
CHEMBL338806 1 4.47
CHEMBL435806 1 -
CHEMBL338439 1 -
CHEMBL338665 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL338865 IC50 = 310.0 nM 6.51
CHEMBL127525 IC50 = 490.0 nM 6.31
CHEMBL127377 IC50 = 800.0 nM 6.10
CHEMBL126925 IC50 = 830.0 nM 6.08
CHEMBL340703 IC50 = 1000.0 nM 6.00
CHEMBL126416 IC50 = 1400.0 nM 5.85
CHEMBL339751 IC50 = 5600.0 nM 5.25
CHEMBL419795 IC50 = 7100.0 nM 5.15
CHEMBL340309 IC50 = 7300.0 nM 5.14
CHEMBL126341 IC50 = 7300.0 nM 5.14
CHEMBL127492 IC50 = 8300.0 nM 5.08
CHEMBL127133 IC50 = 8300.0 nM 5.08
CHEMBL2111839 IC50 = 9200.0 nM 5.04
CHEMBL126983 IC50 = 11000.0 nM 4.96
CHEMBL339476 IC50 = 33000.0 nM 4.48
CHEMBL338806 IC50 = 34000.0 nM 4.47
CHEMBL435806 IC50 > 100000.0 nM -
CHEMBL338439 IC50 > 100000.0 nM -
CHEMBL338665 IC50 > 100000.0 nM -