Target Validation Information
Target ID T07806
Target Name 5-hydroxytryptamine 1B receptor
Target Type
Successful
Drug Potency against Target WAY-466 Drug Info Ki = 9.3 nM [527381]
SEROTONIN Drug Info Ki = 18 nM [529789]
1-(7-Methoxy-naphthalen-2-yl)-piperazine Drug Info Ki = 2 nM [534528]
L-775606 Drug Info IC50 = 75 nM [534500]
Eletriptan Drug Info Ki = 3.14 nM [552727]
2-(5-Thiophen-2-yl-1H-indol-3-yl)-ethylamine Drug Info Ki = 32 nM [525792]
Frovatriptan Drug Info Ki = 2.51 nM [528068]
LY-334370 Drug Info Ki = 83 nM [529496]
5-Isopropyl-3-(2-pyrrolidin-1-yl-ethyl)-1H-indole Drug Info Ki = 472 nM [525845]
(+/-)-nantenine Drug Info Ki = 100 nM [530558]
[2-(5-Ethyl-1H-indol-3-yl)-ethyl]-dimethyl-amine Drug Info Ki = 286 nM [525845]
GR-127935 Drug Info Ki = 0.14 nM [527726]
Almogran Drug Info IC50 = 12 nM [552239]
1-Naphthalen-2-yl-piperazine Drug Info Ki = 10.1 nM [534528]
5-Ethyl-3-(2-pyrrolidin-1-yl-ethyl)-1H-indole Drug Info Ki = 1625 nM [525845]
L-747201 Drug Info IC50 = 30.2 nM [534500]
5-amino-3-(N-methylpiperidin-4-yl)-1H-indole Drug Info Ki = 353 nM [529496]
Zolmitriptan Drug Info EC50 = 478 nM [552212]
Action against Disease Model Frovatriptan -logEC50 on isolated basilar artery: 7.86 [553276] Drug Info
References
Ref 527381J Med Chem. 2005 Jan 27;48(2):353-6.Discovery of 5-arylsulfonamido-3-(pyrrolidin-2-ylmethyl)-1H-indole derivatives as potent, selective 5-HT6 receptor agonists and antagonists.
Ref 529789J Med Chem. 2008 Nov 27;51(22):7094-8.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.
Ref 534528J Med Chem. 1997 Nov 21;40(24):3974-8.5-HT1B receptor antagonist properties of novel arylpiperazide derivatives of 1-naphthylpiperazine.
Ref 534500J Med Chem. 1997 Oct 24;40(22):3501-3.Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.
Ref 552727Molecular design and clinical development of VEGFR kinase inhibitors. Curr Top Med Chem. 2007;7(14):1379-93.
Ref 525792Bioorg Med Chem Lett. 2000 May 1;10(9):903-5.5-Thienyltryptamine derivatives as serotonin 5-HT1B/1D receptor agonists: potential treatments for migraine.
Ref 528068Nat Rev Drug Discov. 2006 Mar;5(3):247-64.Adenosine receptors as therapeutic targets.
Ref 529496J Med Chem. 2008 Jun 26;51(12):3609-16. Epub 2008 May 29.Designing selective, high affinity ligands of 5-HT1D receptor by covalent dimerization of 5-HT1F ligands derived from 4-fluoro-N-[3-(1-methyl-4-piperidinyl)-1H-indol-5-yl]benzamide.
Ref 525845Bioorg Med Chem Lett. 2000 Aug 7;10(15):1707-9.5-Alkyltryptamine derivatives as highly selective and potent 5-HT1D receptor agonists.
Ref 530558Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31. Epub 2009 Nov 20.Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine.
Ref 525845Bioorg Med Chem Lett. 2000 Aug 7;10(15):1707-9.5-Alkyltryptamine derivatives as highly selective and potent 5-HT1D receptor agonists.
Ref 527726Bioorg Med Chem Lett. 2005 Nov 1;15(21):4786-9.Synthesis of potent and selective serotonin 5-HT1B receptor ligands.
Ref 552239Pharmacological characterization of almotriptan: an indolic 5-HT receptor agonist for the treatment of migraine. Eur J Pharmacol. 2000 Dec 20;410(1):33-41.
Ref 534528J Med Chem. 1997 Nov 21;40(24):3974-8.5-HT1B receptor antagonist properties of novel arylpiperazide derivatives of 1-naphthylpiperazine.
Ref 525845Bioorg Med Chem Lett. 2000 Aug 7;10(15):1707-9.5-Alkyltryptamine derivatives as highly selective and potent 5-HT1D receptor agonists.
Ref 553276Effects of the novel high-affinity 5-HT(1B/1D)-receptor ligand frovatriptan in human isolated basilar and coronary arteries. J Cardiovasc Pharmacol. 1998 Aug;32(2):220-4.
Ref 534500J Med Chem. 1997 Oct 24;40(22):3501-3.Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.
Ref 529496J Med Chem. 2008 Jun 26;51(12):3609-16. Epub 2008 May 29.Designing selective, high affinity ligands of 5-HT1D receptor by covalent dimerization of 5-HT1F ligands derived from 4-fluoro-N-[3-(1-methyl-4-piperidinyl)-1H-indol-5-yl]benzamide.
Ref 552212Comparison of the vasoconstrictor effects of the selective 5-HT1D-receptor agonist L-775,606 with the mixed 5-HT1B/1D-receptor agonist sumatriptan and 5-HT in human isolated coronary artery. Br J Clin Pharmacol. 2000 Feb;49(2):126-31.

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