Co-Target(s) Information
| Target General Information | Top | ||||
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| Target ID | T47094 | Target Info | |||
| Target Name | Substance-P receptor (TACR1) | ||||
| Synonyms |
Tachykinin receptor 1; Tachykinin neurokinin 1 receptor; Tachykinin 1 receptor; TACR1; Substance P receptor; SPR; Neurokinin 1 receptor; NK-1R; NK-1 receptor
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| Target Type | Successful Target | ||||
| Gene Name | TACR1 | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
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| Co-Target Name | Monoamine oxidase type B (MAO-B) | Successful Target | ||||
| UniProt ID | AOFB_HUMAN | |||||
| Gene Name | MAOB | |||||
| Synonyms |
MAO-B; Amine oxidase [flavin-containing] B
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| Representative Drug(s) | Selegiline | Drug Info | IC50 = 0.017 nM | [1] | ||
| Co-Target Name | Endothelin A receptor (EDNRA) | Successful Target | ||||
| UniProt ID | EDNRA_HUMAN | |||||
| Gene Name | EDNRA | |||||
| Synonyms |
HET-AR; Endothelin-1 receptor; Endothelin receptor type A; Endothelin receptor A; ETRA; ETA-R; ETA receptor; ETA; ET-A
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| Representative Drug(s) | FR139317 | Drug Info | IC50 = 5.3 nM | [2] | ||
| Co-Target Name | Debrisoquine 4-hydroxylase (CYP2D6) | Successful Target | ||||
| UniProt ID | CP2D6_HUMAN | |||||
| Gene Name | CYP2D6 | |||||
| Synonyms |
P450-DB1; Cytochrome P450-DB1; Cytochrome P450 2D6; CYPIID6; CYP2DL1
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| Representative Drug(s) | CP-122721 | Drug Info | Ki = 20 nM | [3] | ||
| Co-Target Name | Monoamine oxidase type A (MAO-A) | Successful Target | ||||
| UniProt ID | AOFA_HUMAN | |||||
| Gene Name | MAOA | |||||
| Synonyms |
Monoamine oxidase A; Amine oxidase [flavin-containing] A
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| Representative Drug(s) | Selegiline | Drug Info | IC50 = 67.25 nM | [4] | ||
| Co-Target Name | Opioid receptor sigma 1 (OPRS1) | Successful Target | ||||
| UniProt ID | SGMR1_HUMAN | |||||
| Gene Name | SIGMAR1 | |||||
| Synonyms |
hSigmaR1; Sigma1R; Sigma1-receptor; Sigma non-opioid intracellular receptor 1; Sigma 1-type opioid receptor; SRBP; SR31747-binding protein; SR31747 binding protein 1; SR-BP; SIG-1R; Opioid receptor, sigma 1, isoform 1; OPRS1 protein; Aging-associated gene 8 protein; AAG8
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| Representative Drug(s) | Orvepitant | Drug Info | Ki = 940 nM | [5] | ||
| Co-Target Name | Substance-K receptor (TACR2) | Clinical trial Target | ||||
| UniProt ID | NK2R_HUMAN | |||||
| Gene Name | TACR2 | |||||
| Synonyms |
Tachykinin receptor 2; Tachykinin neurokinin 2 receptor; TACR2; SKR; Neurokinin A receptor; NK-2R; NK-2 receptor
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| Representative Drug(s) | Serlopitant | Drug Info | Ki = 2.4 nM | [6] | ||
| Co-Target Name | Neuromedin-K receptor (TACR3) | Successful Target | ||||
| UniProt ID | NK3R_HUMAN | |||||
| Gene Name | TACR3 | |||||
| Synonyms |
Tachykinin receptor 3; TACR3; Neuromedin K receptor; Neurokinin-3 receptor; Neurokinin B receptor; NKR; NK-3R; NK-3 receptor
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| Representative Drug(s) | Serlopitant | Drug Info | Ki = 2.4 nM | Click to Show More | [6] | |
| 2 | Aprepitant | Drug Info | Ki = 454.1 nM | [8] | ||
| Co-Target Name | Albendazole monooxygenase (CYP3A4) | Clinical trial Target | ||||
| UniProt ID | CP3A4_HUMAN | |||||
| Gene Name | CYP3A4 | |||||
| Synonyms |
Taurochenodeoxycholate 6-alpha-hydroxylase; Quinine 3-monooxygenase; P450-PCN1; Nifedipine oxidase; NF-25; HLp; Cytochrome P450-PCN1; Cytochrome P450 NF-25; Cytochrome P450 HLp; Cytochrome P450 3A4; Cytochrome P450 3A3; CYPIIIA4; CYPIIIA3; CYP3A3; Albendazole sulfoxidase; Albendazole monooxygenase (sulfoxide-forming); 1,8-cineole 2-exo-monooxygenase
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| Representative Drug(s) | Aprepitant | Drug Info | IC50 = 46 nM | [7] | ||
| References | Top | ||||
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| REF 1 | Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: design, synthesis, and structure-activity relationships. Bioorg Med Chem. 2010 Nov 1;18(21):7675-99. | ||||
| REF 2 | The combinatorial synthesis of a 30,752-compound library: discovery of SAR around the endothelin antagonist, FR-139,317. Bioorg Med Chem Lett. 1995 May 4;5(9):917-22. | ||||
| REF 3 | Discovery and stereoselective synthesis of the novel isochroman neurokinin-1 receptor antagonist 'CJ-17,493'. Bioorg Med Chem. 2008 Aug 1;16(15):7193-205. | ||||
| REF 4 | Synthesis and selective human monoamine oxidase inhibition of 3-carbonyl, 3-acyl, and 3-carboxyhydrazido coumarin derivatives. Eur J Med Chem. 2011 Oct;46(10):4846-52. | ||||
| REF 5 | Identification, biological characterization and pharmacophoric analysis of a new potent and selective NK1 receptor antagonist clinical candidate. Bioorg Med Chem. 2013 Nov 1;21(21):6264-73. | ||||
| REF 6 | Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists. J Med Chem. 2009 May 14;52(9):3039-46. | ||||
| REF 7 | Pyrrolidine-carboxamides and oxadiazoles as potent hNK1 antagonists. Bioorg Med Chem Lett. 2007 Oct 1;17(19):5310-5. | ||||
| REF 8 | Identification of a crucial amino acid in the helix position 6.51 of human tachykinin neurokinin 1 and 3 receptors contributing to the insurmountable mode of antagonism by dual NK?/NK? antagonists. J Med Chem. 2012 Jun 14;55(11):5061-76. | ||||
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