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Histamine H4 receptor
An H4 histamine receptor that is encoded in the genome of rat. [OMA:Q91ZY1, PRO:DNx]
Synonyms
H4R;
HH4R
Research
Bioassay Publications (12)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 5 (41.67) | 29.6817 |
| 2010's | 7 (58.33) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (6)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| histamine | Rattus norvegicus (Norway rat) | Ki | 0.0996 | 2 | 2 |
| thioperamide | Rattus norvegicus (Norway rat) | Ki | 0.0501 | 1 | 1 |
| jnj 7777120 | Rattus norvegicus (Norway rat) | Ki | 1.8011 | 10 | 27 |
| pf-3893787 | Rattus norvegicus (Norway rat) | Ki | 0.0265 | 3 | 3 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| histamine | Rattus norvegicus (Norway rat) | EC50 | 14.1624 | 4 | 4 |
| histamine | Rattus norvegicus (Norway rat) | Kd | 0.1340 | 1 | 1 |
| 4-methylhistamine | Rattus norvegicus (Norway rat) | EC50 | 2.5119 | 1 | 1 |
| vuf 8430 | Rattus norvegicus (Norway rat) | EC50 | 33.8844 | 1 | 1 |
| jnj 7777120 | Rattus norvegicus (Norway rat) | EC50 | 0.2622 | 3 | 3 |
[no title available]Journal of medicinal chemistry, , 09-12, Volume: 62, Issue:17, 2019
Functional Profiling of 2-Aminopyrimidine Histamine H4 Receptor Modulators.Journal of medicinal chemistry, , Sep-24, Volume: 58, Issue:18, 2015
Histamine H4 receptor agonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
[no title available]Journal of medicinal chemistry, , 09-12, Volume: 62, Issue:17, 2019
Ligand based design of novel histamine Hâ‚„ receptor antagonists; fragment optimization and analysis of binding kinetics.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 21, Issue:21, 2011
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Rotationally constrained 2,4-diamino-5,6-disubstituted pyrimidines: a new class of histamine H4 receptor antagonists with improved druglikeness and in vivo efficacy in pain and inflammation models.Journal of medicinal chemistry, , Oct-23, Volume: 51, Issue:20, 2008
Structure-activity studies on a series of a 2-aminopyrimidine-containing histamine H4 receptor ligands.Journal of medicinal chemistry, , Oct-23, Volume: 51, Issue:20, 2008
A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties.The Journal of pharmacology and experimental therapeutics, , Volume: 309, Issue:1, 2004
The first potent and selective non-imidazole human histamine H4 receptor antagonists.Journal of medicinal chemistry, , Sep-11, Volume: 46, Issue:19, 2003
Functional Profiling of 2-Aminopyrimidine Histamine H4 Receptor Modulators.Journal of medicinal chemistry, , Sep-24, Volume: 58, Issue:18, 2015
A novel series of histamine H4 receptor antagonists based on the pyrido[3,2-d]pyrimidine scaffold: comparison of hERG binding and target residence time with PF-3893787.Bioorganic & medicinal chemistry letters, , May-01, Volume: 23, Issue:9, 2013
Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 21, Issue:21, 2011