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NEW CLASS OF POTENT LIGANDS FOR THE HUMAN PERIPHERAL CANNABINOID RECEPTOR
Abstract A new class of potent ligand for the human peripheral cannabinoid (hCB 2 ) receptor is described. Two indole analogs 13 and 17 exhibited nanomolar potencies (K i ) with good selectivity forExpand
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A cost-effectiveness analysis of interactive paediatric telecardiology
We analysed the cost-effectiveness of a teleconsultation service after five years of operation. The service provides diagnostic consultation at a distance for children suffering from cardiacExpand
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Identification of potent, selective KDM5 inhibitors.
This communication describes the identification and optimization of a series of pan-KDM5 inhibitors derived from compound 1, a hit initially identified against KDM4C. Compound 1 was optimized toExpand
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Chemical noise reduction via mass spectrometry and ion/ion charge inversion: amino acids.
Charge inversion ion/ion reactions can provide a significant reduction in chemical noise associated with mass spectra derived from complex mixtures for species composed of both acidic and basicExpand
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From indomethacin to a selective COX-2 inhibitor: Development of indolalkanoic acids as potent and selective cyclooxygenase-2 inhibitors
Abstract A series of potent and highly selective cyclooxygenase-2 inhibitors have been prepared by replacing the benzoyl group of indomethacin with a 4-bromobenzyl group, and by extending the aceticExpand
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Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials.
In recent years, inhibition of the interaction between the bromodomain and extra-terminal domain (BET) family of chromatin adaptors and acetyl-lysine residues on chromatin has emerged as a promisingExpand
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Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors.
The identification of a novel series of small molecule BET inhibitors is described. Using crystallographic binding modes of an amino-isoxazole fragment and known BET inhibitors, a structure-basedExpand
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