Discovery and functional evaluation of diverse novel human CB(1) receptor ligands.

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Foloppe N, Benwell K, Brooks TD, Kennett G, Knight AR, Misra A, Monck NJ

Discovery and functional evaluation of diverse novel human CB(1) receptor ligands.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4183-90. doi: 10.1016/j.bmcl.2009.05.114. Epub 2009 Jun 2.

PubMed ID

19520572 [ View in PubMed

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Abstract

Ligand-based virtual screening with a 3D pharmacophore led to the discovery of 30 novel, diverse and drug-like ligands of the human cannabinoid receptor 1 (hCB(1)). The pharmacophore was validated with a hit rate of 16%, binding selectivity versus hCB(2), and expected functional profiles. The discovered compounds provide new tools for exploring cannabinoid pharmacology.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Rimonabant	Cannabinoid receptor 1	EC 50 (nM)	4	N/A	N/A	Details
Rimonabant	Cannabinoid receptor 1	Ki (nM)	1.9	N/A	N/A	Details