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• W2069728305 abstract "Optimisation of the potency of a bicyclic CRF antagonist whilst retaining metabolic stability is described. A core change and incorporation of metabolically stable lipophilic groups resulted in a further potency gain without increasing metabolic liability. Pharmacological investigation of binding kinetics led to the identification of compound 25, a sub-nanomolar CRF-1 antagonist with slow dissociation kinetics and an encouraging pharmacokinetic profile." @default.
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• W2069728305 date "2011-10-01" @default.
• W2069728305 modified "2023-10-16" @default.
• W2069728305 title "Discovery of potent, metabolically stable purine CRF-1 antagonists with differentiated binding kinetic profiles" @default.
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• W2069728305 doi "https://doi.org/10.1016/j.bmcl.2011.08.040" @default.
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