Nonpeptide GPIIB/IIIA receptor antagonists. Part 21: C-6 flexibility and amide bond orientation are important factors in determining the affinity of compounds for activated or resting platelet receptors.

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Egbertson MS, Bednar B, Askew BC, Bednar RA, Brashear K, Breslin MJ, Duggan ME, Fisher TE, Halczenko W, Hutchinson JH, Ihle N, Prugh JD, Wai JS, Gould RJ, Hartman GD

Nonpeptide GPIIB/IIIA receptor antagonists. Part 21: C-6 flexibility and amide bond orientation are important factors in determining the affinity of compounds for activated or resting platelet receptors.

Bioorg Med Chem Lett. 2000 Sep 4;10(17):1943-8.

PubMed ID
10987423 [ View in PubMed
]
Abstract

Compound affinity for activated and resting GPIIb/IIIa receptors may differ, and comparison of those differences determines selectivity. Structural features that influence selectivity are discussed.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
TirofibanIntegrin beta-3Kd (nM)1.9N/AN/ADetails
TirofibanIntegrin beta-3Kd (nM)13N/AN/ADetails
TirofibanIntegrin beta-3IC 50 (nM)15N/AN/ADetails