Send to:

Choose Destination

PubMed Citations for PubChem BioAssay (Select 598540)

See comment in PubMed Commons below
Bioorg Med Chem Lett. 2011 Jun 15;21(12):3603-7. doi: 10.1016/j.bmcl.2011.04.104. Epub 2011 May 1.

Identification and optimisation of novel sulfonamide, selective vasopressin V1B receptor antagonists.

Author information

  • 1Department of Pharmacology, MSD, Newhouse, Motherwell, United Kingdom.


The synthesis and preliminary structure-activity relationships (SAR) of a novel class of vasopressin V(1B) receptor antagonists are described. Hit compound 5, identified via high throughput screening of the corporate collection, showed good activity in a V(1B) binding assay (K(i) 63 nM) but did not possess the lead-like physicochemical properties typically required in a hit compound. A 'deletion approach' on the HTS hit 5 was performed, with the focus on improvement of physicochemical properties, yielding the selective V(1B) antagonist 9f (K(i) 190 nM), with improved druglike characteristics.

Copyright © 2011 Elsevier Ltd. All rights reserved.

[PubMed - indexed for MEDLINE]
PubMed Commons home

PubMed Commons

How to join PubMed Commons

    Supplemental Content

    Full text links

    Icon for Elsevier Science
    Loading ...
    Write to the Help Desk