Abstract
A series of acrylic acids and their structurally related compounds were evaluated for their binding affinity to four EP receptor subtypes (EP1-4). Starting from the initial hit 3, which was discovered in our in-house library, compounds 4 and 5 were identified as new chemical leads as candidates for further optimization towards a selective EP3 receptor antagonist. The identification process of these compounds and their pharmacokinetic profiles are presented.
MeSH terms
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Acrylates / chemistry*
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Acrylates / pharmacokinetics
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Acrylates / pharmacology*
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Animals
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Binding, Competitive
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CHO Cells
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Cricetinae
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Cricetulus
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Humans
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Mice
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Microsomes, Liver / metabolism
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Molecular Structure
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Protein Binding
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Pyrazoles / chemistry*
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Rats
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Receptors, Prostaglandin E / antagonists & inhibitors*
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Receptors, Prostaglandin E / metabolism*
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Receptors, Prostaglandin E, EP3 Subtype
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Structure-Activity Relationship
Substances
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Acrylates
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PTGER3 protein, human
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Ptger3 protein, mouse
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Pyrazoles
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Receptors, Prostaglandin E
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Receptors, Prostaglandin E, EP3 Subtype
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pyrazole
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acrylic acid