Griffin Discoveries

H4R Development candidate identified with long receptor residence time

admin — Fri, 10 Feb 2012 12:55:01 +0000

Griffin Discoveries aims to develop novel H4R antagonist with a differentiated profile compared to reference ligands and competitor clincical candidates. The antagonist JNJ7777120 is a very potent compound in a variety of in vivo models despite its relatively short pharmacokinetic half-life. We have studied the residence time of this compound and found a dissociative half-life for the histamine H4 receptor of approximately 60 minutes. This relatively long dissociative half-life may explain the exceptional potency of this well known reference antagonist.

Studying target residence time is a concept that is proving to be increasingly important in late stage lead optimization. Not only can it confer improved efficacy to drug candidates, but it also contributes to an improved safety profile because of the lower doses that are needed for pharmacodynamic efficacy.

Griffin Discoveries has recently identified a development candidate that combines an excellent PK profile in rodents with a long dissociative half-life, and thus increased H4 receptor residence time.

Patent Application for new series of histamine H4 antagonists filed.

admin — Mon, 21 Nov 2011 11:43:08 +0000

Griffin has just filed a new patent application to protect a series of selective H4R antagonists with an excellent in vitro profile and improved toxicological properties when compared to a known reference clinical candidate. In addition to this new series, several other chemotypes are under development as back-ups for this novel lead series.

Griffin Discoveries launches comprehensive histamine receptor profiling service

admin — Sun, 31 Jul 2011 19:54:21 +0000

Early stage drug discovery faces many challenges. Therefore, experimental data has to be generated as efficiently and reliably as possible. Recent insights in the molecular pharmacology of the histamine H4 receptor has shown that significant species differences exist, causing H4R ligands to show distinct pharmacodynamic behavior. Between the species, a single H4R ligand can show the entire spectrum of functional activities ranging from inverse agonist to antagonist to agonist. Griffin Discoveries offers a unique histamine receptor profiling service that can accurately show your compounds’ behavior at the different histamine receptor subtypes (H1R-H4R) as well a many of the species orthologues including human, mouse, rat, monkey and dog receptors and several others. The histamine receptor profiling service allows for the reliable interpretation of the observed in vivo experimental data of H4R ligands.

Griffin Discoveries to participate at CHI Drug Discovery Chemistry 2011

admin — Sat, 12 Mar 2011 07:51:14 +0000

Griffin Discoveries will attend the sixth annual CHI Drug Discovery meeting in San Diego, April 12-14 2011.
A new series of histamine H4R receptor ligands will be presented during the poster sessions.

New dual action non-imidazole H1/H4 antagonists identified.

Rogier — Sat, 12 Feb 2011 14:20:58 +0000

Griffin Discoveries has identified a novel dual action non imidazole H1/H4 histamine receptor antagonist that shows anti-inflammatory effects in vivo. This compound was identified among a larger series of close analogues with a favourable PK profile after oral administration. With high selectivity over the other histamine receptor subtypes, this discovery demonstrates that targeting both the H1R and H4R subtype can be achieved with a single molecule that has drug-like properties.

Griffin Discoveries participate in the International Cost Action Workshop BM0806 WG4, in Frankfurt am Main, Germany.

admin — Mon, 05 Oct 2009 16:25:22 +0000

Griffin Discoveries participate in the International Cost Action Workshop BM0806 WG4, in Frankfurt am Main, Germany.

Patent Application for new series of histamine H4 antagonists filed.

admin — Thu, 18 Jun 2009 14:56:23 +0000

Patent Application for new series of histamine H4 antagonists filed.

Griffin Discoveries BV, a GPCR focused drug discovery company, succesfully spun out of VU University Amsterdam.

admin — Wed, 17 Jun 2009 15:50:27 +0000

Griffin Discoveries BV, a GPCR focused drug discovery company, succesfully spun out of VU University Amsterdam.