Page last updated: 2024-08-07 17:09:15
Leukotriene B4 receptor 1
A leukotriene B4 receptor 1 that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q15722]
Synonyms
LTB4-R 1;
LTB4-R1;
Chemoattractant receptor-like 1;
G-protein coupled receptor 16;
P2Y purinoceptor 7;
P2Y7
Research
Bioassay Publications (32)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 4 (12.50) | 18.7374 |
| 1990's | 25 (78.13) | 18.2507 |
| 2000's | 3 (9.38) | 29.6817 |
| 2010's | 0 (0.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (31)
Drugs with Potency Measurements
Drugs with Inhibition Measurements
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| bw-755c | Homo sapiens (human) | EC50 | 6.8000 | 1 | 1 |
| tepoxalin | Homo sapiens (human) | EC50 | 0.0700 | 1 | 1 |
| zileuton | Homo sapiens (human) | EC50 | 0.4700 | 1 | 1 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| nifedipine | Homo sapiens (human) | ID50 | 0.0100 | 1 | 1 |
Structure-activity relationships of (E)-3-(1,4-benzoquinonyl)-2-[(3-pyridyl)-alkyl]-2-propenoic acid derivatives that inhibit both 5-lipoxygenase and thromboxane A2 synthetase.Journal of medicinal chemistry, , Aug-02, Volume: 39, Issue:16, 1996
Benzothiazole hydroxy ureas as inhibitors of 5-lipoxygenase: use of the hydroxyurea moiety as a replacement for hydroxamic acid.Journal of medicinal chemistry, , Aug-21, Volume: 35, Issue:17, 1992
The most potent organophosphorus inhibitors of leucine aminopeptidase. Structure-based design, chemistry, and activity.Journal of medicinal chemistry, , Jun-19, Volume: 46, Issue:13, 2003
Synthesis of sulfur-containing analogues of bestatin. Inhibition of aminopeptidases by alpha-thiolbestatin analogues.Journal of medicinal chemistry, , Volume: 31, Issue:11, 1988
Modulators of leukotriene biosynthesis and receptor activation.Journal of medicinal chemistry, , Jul-05, Volume: 39, Issue:14, 1996
Synthetic and structure/activity studies on acid-substituted 2-arylphenols: discovery of 2-[2-propyl-3-[3-[2-ethyl-4-(4-fluorophenyl)-5- hydroxyphenoxy]-propoxy]phenoxy]benzoic acid, a high-affinity leukotriene B4 receptor antagonist.Journal of medicinal chemistry, , Oct-27, Volume: 38, Issue:22, 1995
Second-generation leukotriene B4 receptor antagonists related to SC-41930: heterocyclic replacement of the methyl ketone pharmacophore.Journal of medicinal chemistry, , Mar-17, Volume: 38, Issue:6, 1995
(E)-3-[[[[6-(2-carboxyethenyl)-5-[[8-(4- methoxyphenyl)octyl]oxy]-2-pyridinyl]-methyl]thio]methyl]benzoic acid: a novel high-affinity leukotriene B4 receptor antagonist.Journal of medicinal chemistry, , Sep-03, Volume: 36, Issue:18, 1993
Synthesis and LTB4 receptor antagonist activities of the naturally occurring LTB4 receptor antagonist Leucettamine A and related analogues.Journal of medicinal chemistry, , Oct-29, Volume: 36, Issue:22, 1993
4-[2-[Methyl(2-phenethyl)amino]-2-oxoethyl]-8-(phenylmethoxy)-2- naphthalenecarboxylic acid: a high affinity, competitive, orally active leukotriene B4 receptor antagonist.Journal of medicinal chemistry, , Oct-30, Volume: 35, Issue:22, 1992
7-[3-(4-acetyl-3-methoxy-2-propylphenoxy)propoxy]-3,4-dihydro-8- propyl-2H-1-benzopyran-2-carboxylic acid: an orally active selective leukotriene B4 receptor antagonist.Journal of medicinal chemistry, , Volume: 32, Issue:6, 1989
Modulators of leukotriene biosynthesis and receptor activation.Journal of medicinal chemistry, , Jul-05, Volume: 39, Issue:14, 1996
Synthetic and structure/activity studies on acid-substituted 2-arylphenols: discovery of 2-[2-propyl-3-[3-[2-ethyl-4-(4-fluorophenyl)-5- hydroxyphenoxy]-propoxy]phenoxy]benzoic acid, a high-affinity leukotriene B4 receptor antagonist.Journal of medicinal chemistry, , Oct-27, Volume: 38, Issue:22, 1995
Leukotriene B4 (LTB4) receptor antagonists: a series of (hydroxyphenyl)pyrazoles.Journal of medicinal chemistry, , Jul-22, Volume: 37, Issue:15, 1994
A novel series of [2-[methyl(2-phenethyl)amino]-2-oxoethyl] benzene-containing leukotriene B4 antagonists: initial structure-activity relationships.Journal of medicinal chemistry, , Sep-13, Volume: 39, Issue:19, 1996
Structure-activity relationships study of two series of leukotriene B4 antagonists: novel indolyl and naphthyl compounds substituted with a 2-[methyl(2-phenethyl)amino]-2-oxoethyl side chain.Journal of medicinal chemistry, , Sep-13, Volume: 39, Issue:19, 1996
(E)-3-[[[[6-(2-carboxyethenyl)-5-[[8-(4- methoxyphenyl)octyl]oxy]-2-pyridinyl]-methyl]thio]methyl]benzoic acid and related compounds: high affinity leukotriene B4 receptor antagonists.Journal of medicinal chemistry, , Sep-30, Volume: 37, Issue:20, 1994
(E)-3-[[[[6-(2-carboxyethenyl)-5-[[8-(4- methoxyphenyl)octyl]oxy]-2-pyridinyl]-methyl]thio]methyl]benzoic acid: a novel high-affinity leukotriene B4 receptor antagonist.Journal of medicinal chemistry, , Sep-03, Volume: 36, Issue:18, 1993
4-[2-[Methyl(2-phenethyl)amino]-2-oxoethyl]-8-(phenylmethoxy)-2- naphthalenecarboxylic acid: a high affinity, competitive, orally active leukotriene B4 receptor antagonist.Journal of medicinal chemistry, , Oct-30, Volume: 35, Issue:22, 1992
Modulators of leukotriene biosynthesis and receptor activation.Journal of medicinal chemistry, , Jul-05, Volume: 39, Issue:14, 1996
Synthetic and structure/activity studies on acid-substituted 2-arylphenols: discovery of 2-[2-propyl-3-[3-[2-ethyl-4-(4-fluorophenyl)-5- hydroxyphenoxy]-propoxy]phenoxy]benzoic acid, a high-affinity leukotriene B4 receptor antagonist.Journal of medicinal chemistry, , Oct-27, Volume: 38, Issue:22, 1995
Synthetic and structure/activity studies on acid-substituted 2-arylphenols: discovery of 2-[2-propyl-3-[3-[2-ethyl-4-(4-fluorophenyl)-5- hydroxyphenoxy]-propoxy]phenoxy]benzoic acid, a high-affinity leukotriene B4 receptor antagonist.Journal of medicinal chemistry, , Oct-27, Volume: 38, Issue:22, 1995
Biphenylyl-substituted xanthones: highly potent leukotriene B4 receptor antagonists.Journal of medicinal chemistry, , Nov-26, Volume: 36, Issue:24, 1993
The role of receptor binding in drug discovery.Journal of natural products, , Volume: 56, Issue:4, 1993
Benzophenone dicarboxylic acid antagonists of leukotriene B4. 2. Structure-activity relationships of the lipophilic side chain.Journal of medicinal chemistry, , Volume: 33, Issue:10, 1990
(E)-3-[6-[[(2,6-dichlorophenyl)thio]methyl]-3-(2-phenylethoxy)-2- pyridinyl]-2-propenoic acid: a high-affinity leukotriene B4 receptor antagonist with oral antiinflammatory activity.Journal of medicinal chemistry, , Sep-13, Volume: 39, Issue:19, 1996
Modulators of leukotriene biosynthesis and receptor activation.Journal of medicinal chemistry, , Jul-05, Volume: 39, Issue:14, 1996
(E)-3-[[[[6-(2-carboxyethenyl)-5-[[8-(4- methoxyphenyl)octyl]oxy]-2-pyridinyl]-methyl]thio]methyl]benzoic acid and related compounds: high affinity leukotriene B4 receptor antagonists.Journal of medicinal chemistry, , Sep-30, Volume: 37, Issue:20, 1994
(E)-3-[[[[6-(2-carboxyethenyl)-5-[[8-(4- methoxyphenyl)octyl]oxy]-2-pyridinyl]-methyl]thio]methyl]benzoic acid: a novel high-affinity leukotriene B4 receptor antagonist.Journal of medicinal chemistry, , Sep-03, Volume: 36, Issue:18, 1993
Modulators of leukotriene biosynthesis and receptor activation.Journal of medicinal chemistry, , Jul-05, Volume: 39, Issue:14, 1996
(E)-3-[[[[6-(2-carboxyethenyl)-5-[[8-(4- methoxyphenyl)octyl]oxy]-2-pyridinyl]-methyl]thio]methyl]benzoic acid and related compounds: high affinity leukotriene B4 receptor antagonists.Journal of medicinal chemistry, , Sep-30, Volume: 37, Issue:20, 1994
(E)-3-[[[[6-(2-carboxyethenyl)-5-[[8-(4- methoxyphenyl)octyl]oxy]-2-pyridinyl]-methyl]thio]methyl]benzoic acid: a novel high-affinity leukotriene B4 receptor antagonist.Journal of medicinal chemistry, , Sep-03, Volume: 36, Issue:18, 1993
(E)-3-[6-[[(2,6-dichlorophenyl)thio]methyl]-3-(2-phenylethoxy)-2- pyridinyl]-2-propenoic acid: a high-affinity leukotriene B4 receptor antagonist with oral antiinflammatory activity.Journal of medicinal chemistry, , Sep-13, Volume: 39, Issue:19, 1996
Modulators of leukotriene biosynthesis and receptor activation.Journal of medicinal chemistry, , Jul-05, Volume: 39, Issue:14, 1996
Modulators of leukotriene biosynthesis and receptor activation.Journal of medicinal chemistry, , Jul-05, Volume: 39, Issue:14, 1996
(E)-3-[[[[6-(2-carboxyethenyl)-5-[[8-(4- methoxyphenyl)octyl]oxy]-2-pyridinyl]-methyl]thio]methyl]benzoic acid and related compounds: high affinity leukotriene B4 receptor antagonists.Journal of medicinal chemistry, , Sep-30, Volume: 37, Issue:20, 1994
Synthesis and LTB4 receptor antagonist activities of the naturally occurring LTB4 receptor antagonist Leucettamine A and related analogues.Journal of medicinal chemistry, , Oct-29, Volume: 36, Issue:22, 1993
Design, synthesis, and pharmacological evaluation of potent xanthone dicarboxylic acid leukotriene B4 receptor antagonists.Journal of medicinal chemistry, , Jun-11, Volume: 36, Issue:12, 1993
(E)-3-[[[[6-(2-carboxyethenyl)-5-[[8-(4- methoxyphenyl)octyl]oxy]-2-pyridinyl]-methyl]thio]methyl]benzoic acid: a novel high-affinity leukotriene B4 receptor antagonist.Journal of medicinal chemistry, , Sep-03, Volume: 36, Issue:18, 1993
4-[2-[Methyl(2-phenethyl)amino]-2-oxoethyl]-8-(phenylmethoxy)-2- naphthalenecarboxylic acid: a high affinity, competitive, orally active leukotriene B4 receptor antagonist.Journal of medicinal chemistry, , Oct-30, Volume: 35, Issue:22, 1992
omega-[(4-Phenyl-2-quinolyl)oxy]alkanoic acid derivatives: a new family of potent LTB4 antagonists.Journal of medicinal chemistry, , Nov-13, Volume: 35, Issue:23, 1992
omega-[(4,6-Diphenyl-2-pyridyl)oxy]alkanoic acid derivatives: a new family of potent and orally active LTB4 antagonists.Journal of medicinal chemistry, , Nov-13, Volume: 35, Issue:23, 1992
Benzophenone dicarboxylic acid antagonists of leukotriene B4. 2. Structure-activity relationships of the lipophilic side chain.Journal of medicinal chemistry, , Volume: 33, Issue:10, 1990
trans-3-Benzyl-4-hydroxy-7-chromanylbenzoic acid derivatives as antagonists of the leukotriene B4 (LTB4) receptor.Bioorganic & medicinal chemistry letters, , Jul-21, Volume: 8, Issue:14, 1998
Modulators of leukotriene biosynthesis and receptor activation.Journal of medicinal chemistry, , Jul-05, Volume: 39, Issue:14, 1996
(+)-1-(3S,4R)-[3-(4-phenylbenzyl)-4-hydroxychroman-7-yl]cyclopentane carboxylic acid, a highly potent, selective leukotriene B4 antagonist with oral activity in the murine collagen-induced arthritis model.Journal of medicinal chemistry, , Sep-30, Volume: 37, Issue:20, 1994
Enables
This protein enables 4 target(s):
| Target | Category | Definition |
|---|
| nucleotide binding | molecular function | Binding to a nucleotide, any compound consisting of a nucleoside that is esterified with (ortho)phosphate or an oligophosphate at any hydroxyl group on the ribose or deoxyribose. [GOC:mah, ISBN:0198547684] |
| leukotriene receptor activity | molecular function | Combining with a leukotriene to initiate a change in cell activity. Leukotrienes are pharmacologically active substances with a set of three conjugated double bonds; some contain a peptide group based on cysteine. [GOC:ai, ISBN:0198506732] |
| G protein-coupled peptide receptor activity | molecular function | Combining with a peptide 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:dph, GOC:tb] |
| leukotriene B4 receptor activity | molecular function | Combining with leukotriene B4, LTB4, to initiate a change in cell activity. Leukotriene B4 is also known as (6Z, 8E, 10E, 14Z)-(5S, 12R)-5,12-dihydroxyicosa-6,8,10,14-tetraen-1-oate. [GOC:ai, ISBN:0198506732] |
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 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] |
Involved In
This protein is involved in 7 target(s):
| Target | Category | Definition |
|---|
| muscle contraction | biological process | A process in which force is generated within muscle tissue, resulting in a change in muscle geometry. Force generation involves a chemo-mechanical energy conversion step that is carried out by the actin/myosin complex activity, which generates force through ATP hydrolysis. [GOC:ef, GOC:mtg_muscle, ISBN:0198506732] |
| 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] |
| immune response | biological process | Any immune system process that functions in the calibrated response of an organism to a potential internal or invasive threat. [GO_REF:0000022, GOC:add] |
| G protein-coupled receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to its receptor, in which the activated receptor promotes the exchange of GDP for GTP on the alpha-subunit of an associated heterotrimeric G-protein complex. The GTP-bound activated alpha-G-protein then dissociates from the beta- and gamma-subunits to further transmit the signal within the cell. The pathway begins with receptor-ligand interaction, and ends with regulation of a downstream cellular process. The pathway can start from the plasma membrane, Golgi or nuclear membrane. [GOC:bf, GOC:mah, PMID:16902576, PMID:24568158, Wikipedia:G_protein-coupled_receptor] |
| phospholipase C-activating G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation of phospholipase C (PLC) and a subsequent increase in the intracellular concentration of inositol trisphosphate (IP3) and diacylglycerol (DAG). [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194] |
| leukotriene signaling pathway | biological process | A G protein-coupled receptor signaling pathway initiated by leukotriene binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process. [GOC:dph, PMID:21771892] |
| neuropeptide signaling pathway | biological process | A G protein-coupled receptor signaling pathway initiated by a neuropeptide binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process. [GOC:mah, ISBN:0815316194] |