Target Validation Information
TTD ID	T07806
Target Name	5-HT 1B receptor (HTR1B)
Type of Target	Successful
Drug Potency against Target	Almogran	Drug Info	IC50 = 12 nM	[12]
	Eletriptan	Drug Info	Ki = 3.14 nM	[13]
	Frovatriptan	Drug Info	Ki = 2.51 nM	[5]
	Zolmitriptan	Drug Info	EC50 = 478 nM	[11]
	(+/-)-nantenine	Drug Info	Ki = 100 nM	[8]
	1-(7-Methoxy-naphthalen-2-yl)-piperazine	Drug Info	Ki = 2 nM	[10]
	1-Naphthalen-2-yl-piperazine	Drug Info	Ki = 10.1 nM	[10]
	2-(5-Thiophen-2-yl-1H-indol-3-yl)-ethylamine	Drug Info	Ki = 32 nM	[1]
	5-amino-3-(N-methylpiperidin-4-yl)-1H-indole	Drug Info	Ki = 353 nM	[6]
	5-Ethyl-3-(2-pyrrolidin-1-yl-ethyl)-1H-indole	Drug Info	Ki = 1625 nM	[2]
	5-Isopropyl-3-(2-pyrrolidin-1-yl-ethyl)-1H-indole	Drug Info	Ki = 472 nM	[2]
	GR-127935	Drug Info	Ki = 0.14 nM	[4]
	L-747201	Drug Info	IC50 = 30.2 nM	[9]
	L-775606	Drug Info	IC50 = 75 nM	[9]
	LY-334370	Drug Info	Ki = 83 nM	[6]
	SEROTONIN	Drug Info	Ki = 18 nM	[7]
	WAY-466	Drug Info	Ki = 9.3 nM	[3]
	[2-(5-Ethyl-1H-indol-3-yl)-ethyl]-dimethyl-amine	Drug Info	Ki = 286 nM	[2]
Action against Disease Model	Frovatriptan	Drug Info	-logEC50 on isolated basilar artery: 7.86	[14]
References
REF 1	5-Thienyltryptamine derivatives as serotonin 5-HT1B/1D receptor agonists: potential treatments for migraine. Bioorg Med Chem Lett. 2000 May 1;10(9):903-5.
REF 2	5-Alkyltryptamine derivatives as highly selective and potent 5-HT1D receptor agonists. Bioorg Med Chem Lett. 2000 Aug 7;10(15):1707-9.
REF 3	Discovery of 5-arylsulfonamido-3-(pyrrolidin-2-ylmethyl)-1H-indole derivatives as potent, selective 5-HT6 receptor agonists and antagonists. J Med Chem. 2005 Jan 27;48(2):353-6.
REF 4	Synthesis of potent and selective serotonin 5-HT1B receptor ligands. Bioorg Med Chem Lett. 2005 Nov 1;15(21):4786-9.
REF 5	Adenosine receptors as therapeutic targets. Nat Rev Drug Discov. 2006 Mar;5(3):247-64.
REF 6	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-pip... J Med Chem. 2008 Jun 26;51(12):3609-16.
REF 7	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... J Med Chem. 2008 Nov 27;51(22):7094-8.
REF 8	Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31.
REF 9	Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents. J Med Chem. 1997 Oct 24;40(22):3501-3.
REF 10	5-HT1B receptor antagonist properties of novel arylpiperazide derivatives of 1-naphthylpiperazine. J Med Chem. 1997 Nov 21;40(24):3974-8.
REF 11	Comparison 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.
REF 12	Pharmacological 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 13	Molecular design and clinical development of VEGFR kinase inhibitors. Curr Top Med Chem. 2007;7(14):1379-93.
REF 14	Effects 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.

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