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Histamine H4 receptor
An H4 histamine receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q9H3N8]
Synonyms
H4R;
HH4R;
AXOR35;
G-protein coupled receptor 105;
GPRv53;
Pfi-013;
SP9144
Research
Bioassay Publications (80)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 30 (37.50) | 29.6817 |
| 2010's | 43 (53.75) | 24.3611 |
| 2020's | 7 (8.75) | 2.80 |
Compounds (74)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| histamine | Homo sapiens (human) | Ki | 0.0144 | 18 | 18 |
| n-methylhistamine | Homo sapiens (human) | Ki | 0.3161 | 2 | 2 |
| octoclothepine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| amoxapine | Homo sapiens (human) | Ki | 5.0120 | 1 | 1 |
| astemizole | Homo sapiens (human) | Ki | 7.9433 | 1 | 1 |
| cetirizine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| cimetidine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| clobenpropit | Homo sapiens (human) | Ki | 0.0258 | 19 | 19 |
| dimaprit | Homo sapiens (human) | Ki | 0.2407 | 3 | 3 |
| diphenhydramine | Homo sapiens (human) | Ki | 42.6579 | 1 | 1 |
| ebastine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| fexofenadine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| tele-methylhistamine | Homo sapiens (human) | Ki | 11.0000 | 1 | 1 |
| hydroxyzine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| imetit | Homo sapiens (human) | Ki | 0.0050 | 6 | 6 |
| loratadine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| loxapine | Homo sapiens (human) | Ki | 4.2759 | 2 | 2 |
| pyrilamine | Homo sapiens (human) | Ki | 5.0235 | 2 | 2 |
| n-methylquipazine | Homo sapiens (human) | Ki | 6.9183 | 1 | 1 |
| histamine dihydrochloride | Homo sapiens (human) | Ki | 0.0781 | 10 | 10 |
| indopan | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| perlapine | Homo sapiens (human) | Ki | 4.7863 | 1 | 1 |
| pimozide | Homo sapiens (human) | Ki | 2.0000 | 1 | 1 |
| azatadine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| 1-(3-chloro-5-benzo[b][1]benzoxepinyl)-4-methylpiperazine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| 4-methylhistamine | Homo sapiens (human) | Ki | 0.0501 | 2 | 2 |
| impromidine | Homo sapiens (human) | Ki | 0.0208 | 3 | 3 |
| tiotidine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| mizolastine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| mifentidine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| 2-(2-aminoethyl)pyridine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| 2-(2-aminoethyl)thiazole | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| 2-methylhistamine | Homo sapiens (human) | Ki | 0.7942 | 2 | 2 |
| pramipexole | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| amthamine | Homo sapiens (human) | Ki | 5.0119 | 2 | 2 |
| iodoproxyfan | Homo sapiens (human) | Ki | 0.0127 | 3 | 3 |
| alpha-methylhistamine | Homo sapiens (human) | Ki | 833,738,000,000.1664 | 5 | 5 |
| aminopotentidine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| imidazolyl-4-propylamine | Homo sapiens (human) | Ki | 9,613,433,333,333.3540 | 3 | 3 |
| nantenine, (+-)-isomer | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| conessine | Homo sapiens (human) | Ki | 6.6716 | 2 | 6 |
| ranitidine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| burimamide | Homo sapiens (human) | Ki | 0.0866 | 3 | 3 |
| triptorelin | Homo sapiens (human) | Ki | 0.0123 | 4 | 4 |
| 4-(1h-imidazol-4-ylmethyl)piperidine | Homo sapiens (human) | Ki | 6,529,828,571,428.5910 | 7 | 7 |
| thioperamide | Homo sapiens (human) | IC50 | 0.5666 | 5 | 5 |
| thioperamide | Homo sapiens (human) | Ki | 1.0012 | 31 | 36 |
| vuf 8430 | Homo sapiens (human) | Ki | 0.0316 | 2 | 2 |
| jnj 7777120 | Homo sapiens (human) | IC50 | 0.0909 | 10 | 10 |
| jnj 7777120 | Homo sapiens (human) | Ki | 0.7202 | 49 | 69 |
| 2-(3-trifluoromethylphenyl)histamine | Homo sapiens (human) | Ki | 1.2589 | 1 | 1 |
| famotidine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| proxyfan | Homo sapiens (human) | Ki | 0.0501 | 2 | 2 |
| ciproxifan | Homo sapiens (human) | Ki | 3.8902 | 4 | 9 |
| (2S)-1-(1H-imidazol-5-yl)-2-propanamine | Homo sapiens (human) | Ki | 3.9810 | 2 | 2 |
| impentamine | Homo sapiens (human) | Ki | 672,882,500,000.1884 | 4 | 4 |
| dibutyl phthalate | Homo sapiens (human) | Ki | 3.1623 | 1 | 1 |
| jnj 10181457 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| pitolisant | Homo sapiens (human) | Ki | 70.0000 | 3 | 3 |
| gsk239512 | Homo sapiens (human) | Ki | 3.1623 | 1 | 1 |
| 4-(1H-imidazol-5-ylmethyl)pyridine | Homo sapiens (human) | Ki | 0.2492 | 3 | 3 |
| 4-[3-(1H-imidazol-5-yl)propyl]piperidine | Homo sapiens (human) | Ki | 1,621,810,000,000.0000 | 1 | 1 |
| jnj 10191584 | Homo sapiens (human) | IC50 | 0.3340 | 2 | 2 |
| jnj 10191584 | Homo sapiens (human) | Ki | 0.0391 | 9 | 9 |
| histaprodifen | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| 6,7-dichloro 3-(4-methylpiperazin-1-yl)quinoxalin-2(1h)-one | Homo sapiens (human) | Ki | 0.0057 | 3 | 3 |
| methimepip | Homo sapiens (human) | Ki | 1.9952 | 3 | 3 |
| mk-0249 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| 4-(1h-imidazol-4-yl)butanamine | Homo sapiens (human) | Ki | 11,530,516,666,666.6760 | 6 | 6 |
| sp 203 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| gsk 1004723 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| vuf10166 | Homo sapiens (human) | Ki | 0.2291 | 1 | 1 |
| pf-3893787 | Homo sapiens (human) | IC50 | 0.0181 | 5 | 5 |
| pf-3893787 | Homo sapiens (human) | Ki | 0.0048 | 6 | 6 |
| n,n-diallyl-5-methoxytryptamine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| clozapine | Homo sapiens (human) | Ki | 0.1925 | 3 | 3 |
Drugs with Activation Measurements
Drugs with Other Measurements
[no title available]Journal of medicinal chemistry, , 06-24, Volume: 64, Issue:12, 2021
[no title available]Bioorganic & medicinal chemistry, , 01-15, Volume: 30, 2021
Pharmacological characterization of a new series of carbamoylguanidines reveals potent agonism at the HEuropean journal of medicinal chemistry, , Mar-15, Volume: 214, 2021
[no title available]Journal of medicinal chemistry, , 09-12, Volume: 62, Issue:17, 2019
2,4-Diaminopyrimidines as dual ligands at the histamine H1 and H4 receptor-H1/H4-receptor selectivity.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 26, Issue:2, 2016
Synthesis and evaluation of a 2-benzothiazolylphenylmethyl ether class of histamine H4 receptor antagonists.Bioorganic & medicinal chemistry letters, , 11-01, Volume: 26, Issue:21, 2016
Conformational Restriction and Enantioseparation Increase Potency and Selectivity of Cyanoguanidine-Type Histamine H4 Receptor Agonists.Journal of medicinal chemistry, , Apr-14, Volume: 59, Issue:7, 2016
Functional Profiling of 2-Aminopyrimidine Histamine H4 Receptor Modulators.Journal of medicinal chemistry, , Sep-24, Volume: 58, Issue:18, 2015
Ligand based design of novel histamine H₄ receptor antagonists; fragment optimization and analysis of binding kinetics.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
Molecular determinants of ligand binding modes in the histamine H(4) receptor: linking ligand-based three-dimensional quantitative structure-activity relationship (3D-QSAR) models to in silico guided receptor mutagenesis studies.Journal of medicinal chemistry, , Dec-08, Volume: 54, Issue:23, 2011
Triazole ligands reveal distinct molecular features that induce histamine H4 receptor affinity and subtly govern H4/H3 subtype selectivity.Journal of medicinal chemistry, , Mar-24, Volume: 54, Issue:6, 2011
Synthesis and QSAR of quinazoline sulfonamides as highly potent human histamine H4 receptor inverse agonists.Journal of medicinal chemistry, , Mar-25, Volume: 53, Issue:6, 2010
Histamine H4 receptor agonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
Chiral NG-acylated hetarylpropylguanidine-type histamine H2 receptor agonists do not show significant stereoselectivity.Bioorganic & medicinal chemistry letters, , May-15, Volume: 20, Issue:10, 2010
Agonist/antagonist modulation in a series of 2-aryl benzimidazole H4 receptor ligands.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 20, Issue:11, 2010
2,4-Diaminopyrimidines as histamine H4 receptor ligands--Scaffold optimization and pharmacological characterization.Bioorganic & medicinal chemistry, , Oct-15, Volume: 17, Issue:20, 2009
Synthesis and structure-activity relationships of cyanoguanidine-type and structurally related histamine H4 receptor agonists.Journal of medicinal chemistry, , Oct-22, Volume: 52, Issue:20, 2009
N(G)-acylated imidazolylpropylguanidines as potent histamine H4 receptor agonists: selectivity by variation of the N(G)-substituent.Journal of medicinal chemistry, , Apr-23, Volume: 52, Issue:8, 2009
Acylguanidines as bioisosteres of guanidines: NG-acylated imidazolylpropylguanidines, a new class of histamine H2 receptor agonists.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Discovery of novel human histamine H4 receptor ligands by large-scale structure-based virtual screening.Journal of medicinal chemistry, , Jun-12, Volume: 51, Issue:11, 2008
Fragment based design of new H4 receptor-ligands with anti-inflammatory properties in vivo.Journal of medicinal chemistry, , Apr-24, Volume: 51, Issue:8, 2008
Stereochemical diversity-oriented conformational restriction strategy. Development of potent histamine H3 and/or H4 receptor antagonists with an imidazolylcyclopropane structure.Journal of medicinal chemistry, , Sep-07, Volume: 49, Issue:18, 2006
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.The Journal of pharmacology and experimental therapeutics, , Volume: 314, Issue:3, 2005
Synthesis and structure-activity relationships of indole and benzimidazole piperazines as histamine H(4) receptor antagonists.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 14, Issue:21, 2004
A selective human H(4)-receptor agonist: (-)-2-cyano-1-methyl-3-[(2R,5R)-5- [1H-imidazol-4(5)-yl]tetrahydrofuran-2-y] methylguanidine.Journal of medicinal chemistry, , Jul-03, Volume: 46, Issue:14, 2003
Synthesis and structure-activity relationships of conformationally constrained histamine H(3) receptor agonists.Journal of medicinal chemistry, , Dec-04, Volume: 46, Issue:25, 2003
Cyclopropane-based conformational restriction of histamine. (1S,2S)-2-(2-aminoethyl)-1-(1H-imidazol-4-yl)cyclopropane, a highly selective agonist for the histamine H3 receptor, having a cis-cyclopropane structure.Journal of medicinal chemistry, , May-08, Volume: 46, Issue:10, 2003
Histamine H4 receptor agonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.The Journal of pharmacology and experimental therapeutics, , Volume: 314, Issue:3, 2005
[no title available]Journal of medicinal chemistry, , 06-23, Volume: 65, Issue:12, 2022
[no title available]Journal of medicinal chemistry, , 05-28, Volume: 63, Issue:10, 2020
[no title available]Journal of medicinal chemistry, , 09-12, Volume: 62, Issue:17, 2019
Molecular determinants of ligand binding modes in the histamine H(4) receptor: linking ligand-based three-dimensional quantitative structure-activity relationship (3D-QSAR) models to in silico guided receptor mutagenesis studies.Journal of medicinal chemistry, , Dec-08, Volume: 54, Issue:23, 2011
N-Alkenyl and cycloalkyl carbamates as dual acting histamine H3 and H4 receptor ligands.Bioorganic & medicinal chemistry, , May-01, Volume: 19, Issue:9, 2011
Histamine H3 and H4 receptor affinity of branched 3-(1H-imidazol-4-yl)propyl N-alkylcarbamates.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 19, Issue:23, 2009
Clobenpropit analogs as dual activity ligands for the histamine H3 and H4 receptors: synthesis, pharmacological evaluation, and cross-target QSAR studies.Bioorganic & medicinal chemistry, , Jun-01, Volume: 17, Issue:11, 2009
Discovery of novel human histamine H4 receptor ligands by large-scale structure-based virtual screening.Journal of medicinal chemistry, , Jun-12, Volume: 51, Issue:11, 2008
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.The Journal of pharmacology and experimental therapeutics, , Volume: 314, Issue:3, 2005
Histamine H4 receptor agonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
Discovery of novel human histamine H4 receptor ligands by large-scale structure-based virtual screening.Journal of medicinal chemistry, , Jun-12, Volume: 51, Issue:11, 2008
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.The Journal of pharmacology and experimental therapeutics, , Volume: 314, Issue:3, 2005
Histamine H3 receptor as a drug discovery target.Journal of medicinal chemistry, , Jan-13, Volume: 54, Issue:1, 2011
Molecular determinants of ligand binding modes in the histamine H(4) receptor: linking ligand-based three-dimensional quantitative structure-activity relationship (3D-QSAR) models to in silico guided receptor mutagenesis studies.Journal of medicinal chemistry, , Dec-08, Volume: 54, Issue:23, 2011
N-Alkenyl and cycloalkyl carbamates as dual acting histamine H3 and H4 receptor ligands.Bioorganic & medicinal chemistry, , May-01, Volume: 19, Issue:9, 2011
Histamine H4 receptor agonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
Clobenpropit analogs as dual activity ligands for the histamine H3 and H4 receptors: synthesis, pharmacological evaluation, and cross-target QSAR studies.Bioorganic & medicinal chemistry, , Jun-01, Volume: 17, Issue:11, 2009
Discovery of novel human histamine H4 receptor ligands by large-scale structure-based virtual screening.Journal of medicinal chemistry, , Jun-12, Volume: 51, Issue:11, 2008
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.The Journal of pharmacology and experimental therapeutics, , Volume: 314, Issue:3, 2005
Cyclopropane-based conformational restriction of histamine. (1S,2S)-2-(2-aminoethyl)-1-(1H-imidazol-4-yl)cyclopropane, a highly selective agonist for the histamine H3 receptor, having a cis-cyclopropane structure.Journal of medicinal chemistry, , May-08, Volume: 46, Issue:10, 2003
Characterization of the histamine H4 receptor binding site. Part 1. Synthesis and pharmacological evaluation of dibenzodiazepine derivatives.Journal of medicinal chemistry, , Jul-27, Volume: 49, Issue:15, 2006
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.The Journal of pharmacology and experimental therapeutics, , Volume: 314, Issue:3, 2005
Mepyramine-JNJ7777120-hybrid compounds show high affinity to hH(1)R, but low affinity to hH(4)R.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 21, Issue:21, 2011
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.The Journal of pharmacology and experimental therapeutics, , Volume: 314, Issue:3, 2005
[no title available]Journal of medicinal chemistry, , 05-28, Volume: 63, Issue:10, 2020
Discovery of S-(2-guanidylethyl)-isothiourea (VUF 8430) as a potent nonimidazole histamine H4 receptor agonist.Journal of medicinal chemistry, , Nov-16, Volume: 49, Issue:23, 2006
Histamine H4 receptor agonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
Synthesis and structure-activity relationships of cyanoguanidine-type and structurally related histamine H4 receptor agonists.Journal of medicinal chemistry, , Oct-22, Volume: 52, Issue:20, 2009
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.The Journal of pharmacology and experimental therapeutics, , Volume: 314, Issue:3, 2005
Histamine H4 receptor agonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.The Journal of pharmacology and experimental therapeutics, , Volume: 314, Issue:3, 2005
The first potent and selective non-imidazole human histamine H4 receptor antagonists.Journal of medicinal chemistry, , Sep-11, Volume: 46, Issue:19, 2003
Histamine H4 receptor agonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.The Journal of pharmacology and experimental therapeutics, , Volume: 314, Issue:3, 2005
[no title available]Journal of medicinal chemistry, , 06-24, Volume: 64, Issue:12, 2021
Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective DJournal of medicinal chemistry, , 05-28, Volume: 63, Issue:10, 2020
Histamine H4 receptor agonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.The Journal of pharmacology and experimental therapeutics, , Volume: 314, Issue:3, 2005
Molecular determinants of ligand binding modes in the histamine H(4) receptor: linking ligand-based three-dimensional quantitative structure-activity relationship (3D-QSAR) models to in silico guided receptor mutagenesis studies.Journal of medicinal chemistry, , Dec-08, Volume: 54, Issue:23, 2011
Histamine H4 receptor agonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.The Journal of pharmacology and experimental therapeutics, , Volume: 314, Issue:3, 2005
Histamine H4 receptor agonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
Discovery of novel human histamine H4 receptor ligands by large-scale structure-based virtual screening.Journal of medicinal chemistry, , Jun-12, Volume: 51, Issue:11, 2008
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.The Journal of pharmacology and experimental therapeutics, , Volume: 314, Issue:3, 2005
The first potent and selective non-imidazole human histamine H4 receptor antagonists.Journal of medicinal chemistry, , Sep-11, Volume: 46, Issue:19, 2003
Synthesis and structure-activity relationships of conformationally constrained histamine H(3) receptor agonists.Journal of medicinal chemistry, , Dec-04, Volume: 46, Issue:25, 2003
Histamine H4 receptor agonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.The Journal of pharmacology and experimental therapeutics, , Volume: 314, Issue:3, 2005
Synthesis and structure-activity relationships of conformationally constrained histamine H(3) receptor agonists.Journal of medicinal chemistry, , Dec-04, Volume: 46, Issue:25, 2003
Histamine H4 receptor agonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.The Journal of pharmacology and experimental therapeutics, , Volume: 314, Issue:3, 2005
The first potent and selective non-imidazole human histamine H4 receptor antagonists.Journal of medicinal chemistry, , Sep-11, Volume: 46, Issue:19, 2003
[no title available]Journal of medicinal chemistry, , 09-12, Volume: 62, Issue:17, 2019
Conformational Restriction and Enantioseparation Increase Potency and Selectivity of Cyanoguanidine-Type Histamine H4 Receptor Agonists.Journal of medicinal chemistry, , Apr-14, Volume: 59, Issue:7, 2016
Synthesis and structure-activity relationships of cyanoguanidine-type and structurally related histamine H4 receptor agonists.Journal of medicinal chemistry, , Oct-22, Volume: 52, Issue:20, 2009
Discovery of novel human histamine H4 receptor ligands by large-scale structure-based virtual screening.Journal of medicinal chemistry, , Jun-12, Volume: 51, Issue:11, 2008
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.The Journal of pharmacology and experimental therapeutics, , Volume: 314, Issue:3, 2005
Histamine H3 receptor as a drug discovery target.Journal of medicinal chemistry, , Jan-13, Volume: 54, Issue:1, 2011
Molecular determinants of ligand binding modes in the histamine H(4) receptor: linking ligand-based three-dimensional quantitative structure-activity relationship (3D-QSAR) models to in silico guided receptor mutagenesis studies.Journal of medicinal chemistry, , Dec-08, Volume: 54, Issue:23, 2011
Histamine H4 receptor agonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
Synthesis and structure-activity relationships of N-aryl-piperidine derivatives as potent (partial) agonists for human histamine H3 receptor.Bioorganic & medicinal chemistry, , Jul-15, Volume: 18, Issue:14, 2010
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.The Journal of pharmacology and experimental therapeutics, , Volume: 314, Issue:3, 2005
N-substituted piperidinyl alkyl imidazoles: discovery of methimepip as a potent and selective histamine H3 receptor agonist.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Identification of 4-(1H-imidazol-4(5)-ylmethyl)pyridine (immethridine) as a novel, potent, and highly selective histamine H(3) receptor agonist.Journal of medicinal chemistry, , May-06, Volume: 47, Issue:10, 2004
Synthesis and structure-activity relationships of conformationally constrained histamine H(3) receptor agonists.Journal of medicinal chemistry, , Dec-04, Volume: 46, Issue:25, 2003
[no title available]Journal of medicinal chemistry, , 05-28, Volume: 63, Issue:10, 2020
New Dual Small Molecules for Alzheimer's Disease Therapy Combining Histamine HJournal of medicinal chemistry, , 12-26, Volume: 62, Issue:24, 2019
Design, synthesis, and MedChemComm, , Feb-01, Volume: 10, Issue:2, 2019
2,4-Diaminopyrimidines as dual ligands at the histamine H1 and H4 receptor-H1/H4-receptor selectivity.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 26, Issue:2, 2016
Conformational Restriction and Enantioseparation Increase Potency and Selectivity of Cyanoguanidine-Type Histamine H4 Receptor Agonists.Journal of medicinal chemistry, , Apr-14, Volume: 59, Issue:7, 2016
Non-imidazole histamine H3 receptor ligands incorporating antiepileptic moieties.European journal of medicinal chemistry, , Apr-22, Volume: 77, 2014
Anticonvulsant properties of histamine H3 receptor ligands belonging to N-substituted carbamates of imidazopropanol.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 23, Issue:17, 2013
Ligand based design of novel histamine H₄ receptor antagonists; fragment optimization and analysis of binding kinetics.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
Searching for the Multi-Target-Directed Ligands against Alzheimer's disease: discovery of quinoxaline-based hybrid compounds with AChE, H₃R and BACE 1 inhibitory activities.Bioorganic & medicinal chemistry, , Dec-01, Volume: 19, Issue:23, 2011
Histamine H3 receptor as a drug discovery target.Journal of medicinal chemistry, , Jan-13, Volume: 54, Issue:1, 2011
N-Alkenyl and cycloalkyl carbamates as dual acting histamine H3 and H4 receptor ligands.Bioorganic & medicinal chemistry, , May-01, Volume: 19, Issue:9, 2011
Triazole ligands reveal distinct molecular features that induce histamine H4 receptor affinity and subtly govern H4/H3 subtype selectivity.Journal of medicinal chemistry, , Mar-24, Volume: 54, Issue:6, 2011
Synthesis and QSAR of quinazoline sulfonamides as highly potent human histamine H4 receptor inverse agonists.Journal of medicinal chemistry, , Mar-25, Volume: 53, Issue:6, 2010
Identification and hit-to-lead exploration of a novel series of histamine H4 receptor inverse agonists.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 20, Issue:8, 2010
Histamine H3 and H4 receptor affinity of branched 3-(1H-imidazol-4-yl)propyl N-alkylcarbamates.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 19, Issue:23, 2009
Synthesis and structure-activity relationships of cyanoguanidine-type and structurally related histamine H4 receptor agonists.Journal of medicinal chemistry, , Oct-22, Volume: 52, Issue:20, 2009
2,4-Diaminopyrimidines as histamine H4 receptor ligands--Scaffold optimization and pharmacological characterization.Bioorganic & medicinal chemistry, , Oct-15, Volume: 17, Issue:20, 2009
Clobenpropit analogs as dual activity ligands for the histamine H3 and H4 receptors: synthesis, pharmacological evaluation, and cross-target QSAR studies.Bioorganic & medicinal chemistry, , Jun-01, Volume: 17, Issue:11, 2009
N(G)-acylated imidazolylpropylguanidines as potent histamine H4 receptor agonists: selectivity by variation of the N(G)-substituent.Journal of medicinal chemistry, , Apr-23, Volume: 52, Issue:8, 2009
The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.Journal of medicinal chemistry, , Sep-11, Volume: 51, Issue:17, 2008
Discovery of novel human histamine H4 receptor ligands by large-scale structure-based virtual screening.Journal of medicinal chemistry, , Jun-12, Volume: 51, Issue:11, 2008
Fragment based design of new H4 receptor-ligands with anti-inflammatory properties in vivo.Journal of medicinal chemistry, , Apr-24, Volume: 51, Issue:8, 2008
Stereochemical diversity-oriented conformational restriction strategy. Development of potent histamine H3 and/or H4 receptor antagonists with an imidazolylcyclopropane structure.Journal of medicinal chemistry, , Sep-07, Volume: 49, Issue:18, 2006
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.The Journal of pharmacology and experimental therapeutics, , Volume: 314, Issue:3, 2005
The first potent and selective non-imidazole human histamine H4 receptor antagonists.Journal of medicinal chemistry, , Sep-11, Volume: 46, Issue:19, 2003
[no title available]Journal of medicinal chemistry, , 09-12, Volume: 62, Issue:17, 2019
Molecular determinants of ligand binding modes in the histamine H(4) receptor: linking ligand-based three-dimensional quantitative structure-activity relationship (3D-QSAR) models to in silico guided receptor mutagenesis studies.Journal of medicinal chemistry, , Dec-08, Volume: 54, Issue:23, 2011
Histamine H4 receptor agonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
[no title available]Journal of medicinal chemistry, , 05-28, Volume: 63, Issue:10, 2020
Alkyl derivatives of 1,3,5-triazine as histamine HBioorganic & medicinal chemistry, , 04-01, Volume: 27, Issue:7, 2019
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
Discovery of a Novel Highly Selective Histamine H4 Receptor Antagonist for the Treatment of Atopic Dermatitis.Journal of medicinal chemistry, , 04-12, Volume: 61, Issue:7, 2018
2,4-Diaminopyrimidines as dual ligands at the histamine H1 and H4 receptor-H1/H4-receptor selectivity.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 26, Issue:2, 2016
Conformational Restriction and Enantioseparation Increase Potency and Selectivity of Cyanoguanidine-Type Histamine H4 Receptor Agonists.Journal of medicinal chemistry, , Apr-14, Volume: 59, Issue:7, 2016
Diaminopyrimidines, diaminopyridines and diaminopyridazines as histamine H4 receptor modulators.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 25, Issue:4, 2015
Functional Profiling of 2-Aminopyrimidine Histamine H4 Receptor Modulators.Journal of medicinal chemistry, , Sep-24, Volume: 58, Issue:18, 2015
Discovery and SAR of 6-alkyl-2,4-diaminopyrimidines as histamine H₄ receptor antagonists.Journal of medicinal chemistry, , Mar-27, Volume: 57, Issue:6, 2014
The effect of pK(a) on pyrimidine/pyridine-derived histamine H4 ligands.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 24, Issue:23, 2014
Biased ligand modulation of seven transmembrane receptors (7TMRs): functional implications for drug discovery.Journal of medicinal chemistry, , Aug-28, Volume: 57, Issue:16, 2014
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
Bispyrimidines as potent histamine H(4) receptor ligands: delineation of structure-activity relationships and detailed H(4) receptor binding mode.Journal of medicinal chemistry, , Jun-13, Volume: 56, Issue:11, 2013
Ligand based design of novel histamine H₄ receptor antagonists; fragment optimization and analysis of binding kinetics.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
Detailed structure-activity relationship of indolecarboxamides as H4 receptor ligands.European journal of medicinal chemistry, , Volume: 54, 2012
Synthesis of novel histamine H4 receptor antagonists.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 22, Issue:2, 2012
Molecular determinants of ligand binding modes in the histamine H(4) receptor: linking ligand-based three-dimensional quantitative structure-activity relationship (3D-QSAR) models to in silico guided receptor mutagenesis studies.Journal of medicinal chemistry, , Dec-08, Volume: 54, Issue:23, 2011
Discovery of a series of potent and selective human H4 antagonists using ligand efficiency and libraries to explore structure-activity relationship (SAR).Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 21, Issue:21, 2011
Mepyramine-JNJ7777120-hybrid compounds show high affinity to hH(1)R, but low affinity to hH(4)R.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 21, Issue:21, 2011
Triamino pyrimidines and pyridines as histamine H(4) receptor modulators.Bioorganic & medicinal chemistry letters, , May-15, Volume: 21, Issue:10, 2011
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
Synthesis and structure-activity relationships of cyanoguanidine-type and structurally related histamine H4 receptor agonists.Journal of medicinal chemistry, , Oct-22, Volume: 52, Issue:20, 2009
2,4-Diaminopyrimidines as histamine H4 receptor ligands--Scaffold optimization and pharmacological characterization.Bioorganic & medicinal chemistry, , Oct-15, Volume: 17, Issue:20, 2009
Discovery of quinazolines as histamine H4 receptor inverse agonists using a scaffold hopping approach.Journal of medicinal chemistry, , Dec-25, Volume: 51, Issue:24, 2008
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
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
Discovery of novel human histamine H4 receptor ligands by large-scale structure-based virtual screening.Journal of medicinal chemistry, , Jun-12, Volume: 51, Issue:11, 2008
Fragment based design of new H4 receptor-ligands with anti-inflammatory properties in vivo.Journal of medicinal chemistry, , Apr-24, Volume: 51, Issue:8, 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
Characterization of the histamine H4 receptor binding site. Part 1. Synthesis and pharmacological evaluation of dibenzodiazepine derivatives.Journal of medicinal chemistry, , Jul-27, Volume: 49, Issue:15, 2006
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.The Journal of pharmacology and experimental therapeutics, , Volume: 314, Issue:3, 2005
Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists.Journal of medicinal chemistry, , Dec-29, Volume: 48, Issue:26, 2005
A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties.The Journal of pharmacology and experimental therapeutics, , Volume: 309, Issue:1, 2004
Synthesis and structure-activity relationships of indole and benzimidazole piperazines as histamine H(4) receptor antagonists.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 14, Issue:21, 2004
The first potent and selective non-imidazole human histamine H4 receptor antagonists.Journal of medicinal chemistry, , Sep-11, Volume: 46, Issue:19, 2003
Histamine H4 receptor agonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.The Journal of pharmacology and experimental therapeutics, , Volume: 314, Issue:3, 2005
N-Alkenyl and cycloalkyl carbamates as dual acting histamine H3 and H4 receptor ligands.Bioorganic & medicinal chemistry, , May-01, Volume: 19, Issue:9, 2011
Histamine H3 and H4 receptor affinity of branched 3-(1H-imidazol-4-yl)propyl N-alkylcarbamates.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 19, Issue:23, 2009
The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.Journal of medicinal chemistry, , Sep-11, Volume: 51, Issue:17, 2008
Histamine H4 receptor agonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.The Journal of pharmacology and experimental therapeutics, , Volume: 314, Issue:3, 2005
Histamine H4 receptor agonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
A chemical switch for the modulation of the functional activity of higher homologues of histamine on the human histamine H3 receptor: effect of various substitutions at the primary amino function.Journal of medicinal chemistry, , Apr-20, Volume: 49, Issue:8, 2006
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.The Journal of pharmacology and experimental therapeutics, , Volume: 314, Issue:3, 2005
Synthesis and structure-activity relationships of conformationally constrained histamine H(3) receptor agonists.Journal of medicinal chemistry, , Dec-04, Volume: 46, Issue:25, 2003
Structural modifications in the distal, regulatory region of histamine HEuropean journal of medicinal chemistry, , Mar-05, Volume: 213, 2021
Synthesis and biological activity of novel tert-butyl and tert-pentylphenoxyalkyl piperazine derivatives as histamine HEuropean journal of medicinal chemistry, , May-25, Volume: 152, 2018
Non-imidazole histamine H3 receptor ligands incorporating antiepileptic moieties.European journal of medicinal chemistry, , Apr-22, Volume: 77, 2014
Histamine H4 receptor agonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.The Journal of pharmacology and experimental therapeutics, , Volume: 314, Issue:3, 2005
Identification of 4-(1H-imidazol-4(5)-ylmethyl)pyridine (immethridine) as a novel, potent, and highly selective histamine H(3) receptor agonist.Journal of medicinal chemistry, , May-06, Volume: 47, Issue:10, 2004
Discovery and SAR of 6-alkyl-2,4-diaminopyrimidines as histamine H₄ receptor antagonists.Journal of medicinal chemistry, , Mar-27, Volume: 57, Issue:6, 2014
Ligand based design of novel histamine H₄ receptor antagonists; fragment optimization and analysis of binding kinetics.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
Synthesis of novel histamine H4 receptor antagonists.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 22, Issue:2, 2012
Discovery of a series of potent and selective human H4 antagonists using ligand efficiency and libraries to explore structure-activity relationship (SAR).Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 21, Issue:21, 2011
Triamino pyrimidines and pyridines as histamine H(4) receptor modulators.Bioorganic & medicinal chemistry letters, , May-15, Volume: 21, Issue:10, 2011
Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists.Journal of medicinal chemistry, , Dec-29, Volume: 48, Issue:26, 2005
Synthesis and structure-activity relationships of indole and benzimidazole piperazines as histamine H(4) receptor antagonists.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 14, Issue:21, 2004
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
Ligand based design of novel histamine H₄ receptor antagonists; fragment optimization and analysis of binding kinetics.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
Discovery of quinazolines as histamine H4 receptor inverse agonists using a scaffold hopping approach.Journal of medicinal chemistry, , Dec-25, Volume: 51, Issue:24, 2008
Fragment based design of new H4 receptor-ligands with anti-inflammatory properties in vivo.Journal of medicinal chemistry, , Apr-24, Volume: 51, Issue:8, 2008
Histamine H4 receptor agonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.The Journal of pharmacology and experimental therapeutics, , Volume: 314, Issue:3, 2005
N-substituted piperidinyl alkyl imidazoles: discovery of methimepip as a potent and selective histamine H3 receptor agonist.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Conformational Restriction and Enantioseparation Increase Potency and Selectivity of Cyanoguanidine-Type Histamine H4 Receptor Agonists.Journal of medicinal chemistry, , Apr-14, Volume: 59, Issue:7, 2016
Histamine H4 receptor agonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
A chemical switch for the modulation of the functional activity of higher homologues of histamine on the human histamine H3 receptor: effect of various substitutions at the primary amino function.Journal of medicinal chemistry, , Apr-20, Volume: 49, Issue:8, 2006
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.The Journal of pharmacology and experimental therapeutics, , Volume: 314, Issue:3, 2005
Identification of 4-(1H-imidazol-4(5)-ylmethyl)pyridine (immethridine) as a novel, potent, and highly selective histamine H(3) receptor agonist.Journal of medicinal chemistry, , May-06, Volume: 47, Issue:10, 2004
Synthesis and structure-activity relationships of conformationally constrained histamine H(3) receptor agonists.Journal of medicinal chemistry, , Dec-04, Volume: 46, Issue:25, 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
Molecular determinants of ligand binding modes in the histamine H(4) receptor: linking ligand-based three-dimensional quantitative structure-activity relationship (3D-QSAR) models to in silico guided receptor mutagenesis studies.Journal of medicinal chemistry, , Dec-08, Volume: 54, Issue:23, 2011
Characterization of the histamine H4 receptor binding site. Part 1. Synthesis and pharmacological evaluation of dibenzodiazepine derivatives.Journal of medicinal chemistry, , Jul-27, Volume: 49, Issue:15, 2006
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.The Journal of pharmacology and experimental therapeutics, , Volume: 314, Issue:3, 2005
Enables
This protein enables 3 target(s):
| Target | Category | Definition |
|---|
| histamine receptor activity | molecular function | Combining with histamine to initiate a change in cell activity. Histamine is a physiologically active amine, found in plant and animal tissue and released from mast cells as part of an allergic reaction in humans. [GOC:ai] |
| G protein-coupled serotonin receptor activity | molecular function | Combining with the biogenic amine serotonin and transmitting the signal across the membrane by activating an associated G-protein. Serotonin (5-hydroxytryptamine) is a neurotransmitter and hormone found in vertebrates and invertebrates. [GOC:ai] |
| G protein-coupled acetylcholine receptor activity | molecular function | Combining with acetylcholine and transmitting the signal across the membrane by activating an associated G-protein; promotes the exchange of GDP for GTP on the alpha subunit of a heterotrimeric G-protein complex. [GOC:bf, GOC:fj, GOC:mah] |
Located In
This protein is located in 1 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
Active In
This protein is active in 3 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| dendrite | cellular component | A neuron projection that has a short, tapering, morphology. Dendrites receive and integrate signals from other neurons or from sensory stimuli, and conduct nerve impulses towards the axon or the cell body. In most neurons, the impulse is conveyed from dendrites to axon via the cell body, but in some types of unipolar neuron, the impulse does not travel via the cell body. [GOC:aruk, GOC:bc, GOC:dos, GOC:mah, GOC:nln, ISBN:0198506732] |
| synapse | cellular component | The junction between an axon of one neuron and a dendrite of another neuron, a muscle fiber or a glial cell. As the axon approaches the synapse it enlarges into a specialized structure, the presynaptic terminal bouton, which contains mitochondria and synaptic vesicles. At the tip of the terminal bouton is the presynaptic membrane; facing it, and separated from it by a minute cleft (the synaptic cleft) is a specialized area of membrane on the receiving cell, known as the postsynaptic membrane. In response to the arrival of nerve impulses, the presynaptic terminal bouton secretes molecules of neurotransmitters into the synaptic cleft. These diffuse across the cleft and transmit the signal to the postsynaptic membrane. [GOC:aruk, ISBN:0198506732, PMID:24619342, PMID:29383328, PMID:31998110] |
Involved In
This protein is involved in 8 target(s):
| Target | Category | Definition |
|---|
| inflammatory response | biological process | The immediate defensive reaction (by vertebrate tissue) to infection or injury caused by chemical or physical agents. The process is characterized by local vasodilation, extravasation of plasma into intercellular spaces and accumulation of white blood cells and macrophages. [GO_REF:0000022, ISBN:0198506732] |
| positive regulation of cytosolic calcium ion concentration | biological process | Any process that increases the concentration of calcium ions in the cytosol. [GOC:ai] |
| biological_process | biological process | A biological process is the execution of a genetically-encoded biological module or program. It consists of all the steps required to achieve the specific biological objective of the module. A biological process is accomplished by a particular set of molecular functions carried out by specific gene products (or macromolecular complexes), often in a highly regulated manner and in a particular temporal sequence. [GOC:pdt] |
| regulation of MAPK cascade | biological process | Any process that modulates the frequency, rate or extent of signal transduction mediated by the MAP kinase (MAPK) cascade. [GOC:go_curators] |
| G protein-coupled serotonin receptor signaling pathway | biological process | The series of molecular signals generated as a consequence of a G protein-coupled serotonin receptor binding to one of its physiological ligands. [GOC:mah] |
| adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathway | biological process | An adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway initiated by acetylcholine binding to its receptor, and ending with the regulation of a downstream cellular process. [GOC:dph, GOC:mah, GOC:signaling, GOC:tb] |
| G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation or inhibition of a nucleotide cyclase activity and a subsequent change in the concentration of a cyclic nucleotide. [GOC:mah, GOC:signaling, ISBN:0815316194] |
| chemical synaptic transmission | biological process | The vesicular release of classical neurotransmitter molecules from a presynapse, across a chemical synapse, the subsequent activation of neurotransmitter receptors at the postsynapse of a target cell (neuron, muscle, or secretory cell) and the effects of this activation on the postsynaptic membrane potential and ionic composition of the postsynaptic cytosol. This process encompasses both spontaneous and evoked release of neurotransmitter and all parts of synaptic vesicle exocytosis. Evoked transmission starts with the arrival of an action potential at the presynapse. [GOC:jl, MeSH:D009435] |