Target family: 5-Hydroxytryptamine receptors (type: gpcr)
Target: 5-HT<sub>1D</sub> receptor

Ligand: 1-naphthylpiperazine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta.
Published in: Proc Natl Acad Sci USA

Ligand: 1-naphthylpiperazine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): 5-HT1B receptor antagonist properties of novel arylpiperazide derivatives of 1-naphthylpiperazine.
Published in: J Med Chem

Ligand: 2-methyl-5-HT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Alniditan, a new 5-hydroxytryptamine1D agonist and migraine-abortive agent: ligand-binding properties of human 5-hydroxytryptamine1D alpha, human 5-hydroxytryptamine1D beta, and calf 5-hydroxytryptamine1D receptors investigated with [3H]5-hydroxytryptamine and [3H]alniditan.
Published in: Mol Pharmacol

Ligand: 2-methyl-5-HT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta.
Published in: Proc Natl Acad Sci USA

Ligand: 5-CT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor.
Published in: Mol Pharmacol

Ligand: 5-CT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta.
Published in: Proc Natl Acad Sci USA

Ligand: 5-CT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Alniditan, a new 5-hydroxytryptamine1D agonist and migraine-abortive agent: ligand-binding properties of human 5-hydroxytryptamine1D alpha, human 5-hydroxytryptamine1D beta, and calf 5-hydroxytryptamine1D receptors investigated with [3H]5-hydroxytryptamine and [3H]alniditan.
Published in: Mol Pharmacol

Ligand: 5-HT-moduline (Peptide)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 12 pIC50
Reference (Journal): Specific interaction of 5-HT-moduline with human 5-HT1b as well as 5-HT1d receptors expressed in transfected cultured cells.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Actions of roxindole at recombinant human dopamine D2, D3 and D4 and serotonin 5-HT1A, 5-HT1B and 5-HT1D receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): (+)-WAY 100135, a partial agonist, at native and recombinant 5-HT1B/1D receptors.
Published in: Br J Pharmacol

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): GR127935 acts as a partial agonist at recombinant human 5-HT1D alpha and 5-HT1D beta receptors.
Published in: Eur J Pharmacol

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor.
Published in: Mol Pharmacol

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): SB-224289--a novel selective (human) 5-HT1B receptor antagonist with negative intrinsic activity.
Published in: Br J Pharmacol

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta.
Published in: Proc Natl Acad Sci USA

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Alniditan, a new 5-hydroxytryptamine1D agonist and migraine-abortive agent: ligand-binding properties of human 5-hydroxytryptamine1D alpha, human 5-hydroxytryptamine1D beta, and calf 5-hydroxytryptamine1D receptors investigated with [3H]5-hydroxytryptamine and [3H]alniditan.
Published in: Mol Pharmacol

Ligand: 5-MeOT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Alniditan, a new 5-hydroxytryptamine1D agonist and migraine-abortive agent: ligand-binding properties of human 5-hydroxytryptamine1D alpha, human 5-hydroxytryptamine1D beta, and calf 5-hydroxytryptamine1D receptors investigated with [3H]5-hydroxytryptamine and [3H]alniditan.
Published in: Mol Pharmacol

Ligand: 5-MeOT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta.
Published in: Proc Natl Acad Sci USA

Ligand: 5-MeOT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor.
Published in: Mol Pharmacol

Ligand: 7-methoxy-1-naphthylpiperazine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.2 pKi
Reference (Journal): 5-HT1B receptor antagonist properties of novel arylpiperazide derivatives of 1-naphthylpiperazine.
Published in: J Med Chem

Ligand: 8-OH-DPAT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Alniditan, a new 5-hydroxytryptamine1D agonist and migraine-abortive agent: ligand-binding properties of human 5-hydroxytryptamine1D alpha, human 5-hydroxytryptamine1D beta, and calf 5-hydroxytryptamine1D receptors investigated with [3H]5-hydroxytryptamine and [3H]alniditan.
Published in: Mol Pharmacol

Ligand: 8-OH-DPAT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors.
Published in: Eur J Pharmacol

Ligand: 8-OH-DPAT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterization of human serotonin 1D and 1B receptors using [3H]-GR-125743, a novel radiolabelled serotonin 5HT1D/1B receptor antagonist.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: 9-OH-risperidone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.9 pKi
Reference (Journal): Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
Published in: Psychopharmacology (Berl.)

Ligand: almotriptan (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2001), UK (2013)
Primary target: no
Median affinity: 7.889999866485596 pIC50
Reference (Journal): Pharmacological characterization of almotriptan: an indolic 5-HT receptor agonist for the treatment of migraine.
Published in: Eur J Pharmacol

Ligand: alniditan (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Alniditan, a new 5-hydroxytryptamine1D agonist and migraine-abortive agent: ligand-binding properties of human 5-hydroxytryptamine1D alpha, human 5-hydroxytryptamine1D beta, and calf 5-hydroxytryptamine1D receptors investigated with [3H]5-hydroxytryptamine and [3H]alniditan.
Published in: Mol Pharmacol

Ligand: alniditan (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Agonistic properties of alniditan, sumatriptan and dihydroergotamine on human 5-HT1B and 5-HT1D receptors expressed in various mammalian cell lines.
Published in: Br J Pharmacol

Ligand: α-methyl-5-HT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Alniditan, a new 5-hydroxytryptamine1D agonist and migraine-abortive agent: ligand-binding properties of human 5-hydroxytryptamine1D alpha, human 5-hydroxytryptamine1D beta, and calf 5-hydroxytryptamine1D receptors investigated with [3H]5-hydroxytryptamine and [3H]alniditan.
Published in: Mol Pharmacol

Ligand: aripiprazole (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (2002), EMA (2004)
Median affinity: 7.2 pKi
Reference (Journal): Aripiprazole, a novel atypical antipsychotic drug with a unique and robust pharmacology.
Published in: Neuropsychopharmacology

Ligand: asenapine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (2009), EMA (2010)
Median affinity: 8.4 pKi
Reference (Journal): Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
Published in: Psychopharmacology (Berl.)

Ligand: avitriptan (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.359999656677246 pKi
Reference (Journal): Effects of avitriptan, a new 5-HT 1B/1D receptor agonist, in experimental models predictive of antimigraine activity and coronary side-effect potential.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: BRL-15572 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 7.900000095367432 pKi
Reference (Journal): SB-216641 and BRL-15572--compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: bromocriptine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1978)
Median affinity: 8 pKi
Reference (Journal): Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.
Published in: J Pharmacol Exp Ther

Ligand: bufotenine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Alniditan, a new 5-hydroxytryptamine1D agonist and migraine-abortive agent: ligand-binding properties of human 5-hydroxytryptamine1D alpha, human 5-hydroxytryptamine1D beta, and calf 5-hydroxytryptamine1D receptors investigated with [3H]5-hydroxytryptamine and [3H]alniditan.
Published in: Mol Pharmacol

Ligand: cabergoline (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1996)
Median affinity: 8.1 pKi
Reference (Journal): Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.
Published in: J Pharmacol Exp Ther

Ligand: capeserod (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 5.1 pKi
Reference (Journal): SL65.0155, a novel 5-hydroxytryptamine(4) receptor partial agonist with potent cognition-enhancing properties.
Published in: J Pharmacol Exp Ther

Ligand: CGS-12066 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta.
Published in: Proc Natl Acad Sci USA

Ligand: CGS-12066 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor.
Published in: Mol Pharmacol

Ligand: clozapine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1989)
Median affinity: 6.4 pKi
Reference (Journal): Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
Published in: Psychopharmacology (Berl.)

Ligand: CP-122288 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.7 pIC50
Reference (Journal): Characterization of human serotonin 1D and 1B receptors using [3H]-GR-125743, a novel radiolabelled serotonin 5HT1D/1B receptor antagonist.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: cyanopindolol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.1 pKi
Reference (Journal): Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor.
Published in: Mol Pharmacol

Ligand: dihydroergotamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1997)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor.
Published in: Mol Pharmacol

Ligand: dihydroergotamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1997)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Alniditan, a new 5-hydroxytryptamine1D agonist and migraine-abortive agent: ligand-binding properties of human 5-hydroxytryptamine1D alpha, human 5-hydroxytryptamine1D beta, and calf 5-hydroxytryptamine1D receptors investigated with [3H]5-hydroxytryptamine and [3H]alniditan.
Published in: Mol Pharmacol

Ligand: dihydroergotamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1997)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Agonistic properties of alniditan, sumatriptan and dihydroergotamine on human 5-HT1B and 5-HT1D receptors expressed in various mammalian cell lines.
Published in: Br J Pharmacol

Ligand: dimethyltryptamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Alniditan, a new 5-hydroxytryptamine1D agonist and migraine-abortive agent: ligand-binding properties of human 5-hydroxytryptamine1D alpha, human 5-hydroxytryptamine1D beta, and calf 5-hydroxytryptamine1D receptors investigated with [3H]5-hydroxytryptamine and [3H]alniditan.
Published in: Mol Pharmacol

Ligand: dipropyl-5-CT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.9 pIC50
Reference (Journal): Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta.
Published in: Proc Natl Acad Sci USA

Ligand: donitriptan (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.6 pKi
Reference (Journal): F 11356, a novel 5-hydroxytryptamine (5-HT) derivative with potent, selective, and unique high intrinsic activity at 5-HT1B/1D receptors in models relevant to migraine.
Published in: J Pharmacol Exp Ther

Ligand: donitriptan (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.3 pKi
Reference (Journal): F 11356, a novel 5-hydroxytryptamine (5-HT) derivative with potent, selective, and unique high intrinsic activity at 5-HT1B/1D receptors in models relevant to migraine.
Published in: J Pharmacol Exp Ther

Ligand: eletriptan (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (2002)
Primary target: yes
Median affinity: 8.899999618530273 pKi
Reference (Journal): Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors.
Published in: Eur J Pharmacol

Ligand: EMDT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.5 pKi
Reference (Journal): 2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors.
Published in: J Med Chem

Ligand: ergotamine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1960)
Primary target: yes
Median affinity: 9.100000381469727 pKi
Reference (Journal): 2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors.
Published in: J Med Chem

Ligand: fluspirilene (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity: 6 pKi
Reference (Journal): Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
Published in: Psychopharmacology (Berl.)

Ligand: frovatriptan (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2001)
Primary target: yes
Median affinity: 8.359999656677246 pKi
Reference (Journal): N-Methyl-5-tert-butyltryptamine: A novel, highly potent 5-HT1D receptor agonist.
Published in: J Med Chem

Ligand: GR 127935 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): 5-HT1B receptor antagonist properties of novel arylpiperazide derivatives of 1-naphthylpiperazine.
Published in: J Med Chem

Ligand: GR 127935 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Alniditan, a new 5-hydroxytryptamine1D agonist and migraine-abortive agent: ligand-binding properties of human 5-hydroxytryptamine1D alpha, human 5-hydroxytryptamine1D beta, and calf 5-hydroxytryptamine1D receptors investigated with [3H]5-hydroxytryptamine and [3H]alniditan.
Published in: Mol Pharmacol

Ligand: GR 127935 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): SB-216641 and BRL-15572--compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: GR 127935 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): SB-224289--a novel selective (human) 5-HT1B receptor antagonist with negative intrinsic activity.
Published in: Br J Pharmacol

Ligand: GR 127935 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2, 4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydro- spiro[furo[2,3-f]indole-3,4'-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function both in vitro and in vivo.
Published in: J Med Chem

Ligand: GR 127935 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): GR127935 acts as a partial agonist at recombinant human 5-HT1D alpha and 5-HT1D beta receptors.
Published in: Eur J Pharmacol

Ligand: haloperidol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1967)
Median affinity: 6.6 pKi
Reference (Journal): Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
Published in: Psychopharmacology (Berl.)

Ligand: m-chlorophenylpiperazine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.7 pKi
Reference (Journal): Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor.
Published in: Mol Pharmacol

Ligand: ketanserin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity:  pKi
Reference (Journal): Characterization of human serotonin 1D and 1B receptors using [3H]-GR-125743, a novel radiolabelled serotonin 5HT1D/1B receptor antagonist.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: ketanserin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity:  pKi
Reference (Journal): Alniditan, a new 5-hydroxytryptamine1D agonist and migraine-abortive agent: ligand-binding properties of human 5-hydroxytryptamine1D alpha, human 5-hydroxytryptamine1D beta, and calf 5-hydroxytryptamine1D receptors investigated with [3H]5-hydroxytryptamine and [3H]alniditan.
Published in: Mol Pharmacol

Ligand: L-694,247 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9 pKi
Reference (Journal): Chimeric receptor analysis of the ketanserin binding site in the human 5-Hydroxytryptamine1D receptor: importance of the second extracellular loop and fifth transmembrane domain in antagonist binding.
Published in: Mol Pharmacol

Ligand: L-772,405 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9 pIC50
Reference (Journal): 3-[3-(Piperidin-1-yl)propyl]indoles as highly selective h5-HT(1D) receptor agonists.
Published in: J Med Chem

Ligand: lisuride (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: EMA (2011)
Median affinity: 9 pKi
Reference (Journal): Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.
Published in: J Pharmacol Exp Ther

Ligand: LY344864 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.2 pKi
Reference (Journal): Characterization of LY344864 as a pharmacological tool to study 5-HT1F receptors: binding affinities, brain penetration and activity in the neurogenic dural inflammation model of migraine.
Published in: Life Sci

Ligand: lysergic acid (Natural product)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Alniditan, a new 5-hydroxytryptamine1D agonist and migraine-abortive agent: ligand-binding properties of human 5-hydroxytryptamine1D alpha, human 5-hydroxytryptamine1D beta, and calf 5-hydroxytryptamine1D receptors investigated with [3H]5-hydroxytryptamine and [3H]alniditan.
Published in: Mol Pharmacol

Ligand: lysergol (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.2 pKi
Reference (Journal): Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta.
Published in: Proc Natl Acad Sci USA

Ligand: metergoline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor.
Published in: Mol Pharmacol

Ligand: metergoline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Alniditan, a new 5-hydroxytryptamine1D agonist and migraine-abortive agent: ligand-binding properties of human 5-hydroxytryptamine1D alpha, human 5-hydroxytryptamine1D beta, and calf 5-hydroxytryptamine1D receptors investigated with [3H]5-hydroxytryptamine and [3H]alniditan.
Published in: Mol Pharmacol

Ligand: metergoline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterization of human serotonin 1D and 1B receptors using [3H]-GR-125743, a novel radiolabelled serotonin 5HT1D/1B receptor antagonist.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: methiothepin (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Alniditan, a new 5-hydroxytryptamine1D agonist and migraine-abortive agent: ligand-binding properties of human 5-hydroxytryptamine1D alpha, human 5-hydroxytryptamine1D beta, and calf 5-hydroxytryptamine1D receptors investigated with [3H]5-hydroxytryptamine and [3H]alniditan.
Published in: Mol Pharmacol

Ligand: methiothepin (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterization of human serotonin 1D and 1B receptors using [3H]-GR-125743, a novel radiolabelled serotonin 5HT1D/1B receptor antagonist.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: methiothepin (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor.
Published in: Mol Pharmacol

Ligand: methiothepin (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): GR127935 acts as a partial agonist at recombinant human 5-HT1D alpha and 5-HT1D beta receptors.
Published in: Eur J Pharmacol

Ligand: methysergide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1962)
Median affinity:  pKi
Reference (Journal): Alniditan, a new 5-hydroxytryptamine1D agonist and migraine-abortive agent: ligand-binding properties of human 5-hydroxytryptamine1D alpha, human 5-hydroxytryptamine1D beta, and calf 5-hydroxytryptamine1D receptors investigated with [3H]5-hydroxytryptamine and [3H]alniditan.
Published in: Mol Pharmacol

Ligand: methysergide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1962)
Median affinity:  pKi
Reference (Journal): Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta.
Published in: Proc Natl Acad Sci USA

Ligand: MPDT (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.2 pKi
Reference (Journal): 2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors.
Published in: J Med Chem

Ligand: naratriptan (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1998)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Characterization of human serotonin 1D and 1B receptors using [3H]-GR-125743, a novel radiolabelled serotonin 5HT1D/1B receptor antagonist.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: naratriptan (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1998)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors.
Published in: Eur J Pharmacol

Ligand: naratriptan (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1998)
Primary target: yes
Median affinity:  pKi
Reference (Journal): 5-Hydroxytryptamine (5-HT)4 receptors in post mortem human brain tissue: distribution, pharmacology and effects of neurodegenerative diseases.
Published in: Br J Pharmacol

Ligand: ocaperidone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Alniditan, a new 5-hydroxytryptamine1D agonist and migraine-abortive agent: ligand-binding properties of human 5-hydroxytryptamine1D alpha, human 5-hydroxytryptamine1D beta, and calf 5-hydroxytryptamine1D receptors investigated with [3H]5-hydroxytryptamine and [3H]alniditan.
Published in: Mol Pharmacol

Ligand: olanzapine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: EMA & FDA (1996)
Median affinity: 6.2 pKi
Reference (Journal): Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
Published in: Psychopharmacology (Berl.)

Ligand: oxymetazoline (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1986)
Median affinity: 9.4 pKi
Reference (Journal): Benzylimidazolines as h5-HT1B/1D serotonin receptor ligands: a structure-affinity investigation.
Published in: J Med Chem

Ligand: pergolide (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1988)
Median affinity: 7.9 pKi
Reference (Journal): Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.
Published in: J Pharmacol Exp Ther

Ligand: pipamperone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.8 pKi
Reference (Journal): Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
Published in: Psychopharmacology (Berl.)

Ligand: PNU109291 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 9.1 pKi
Reference (Journal): Isochroman-6-carboxamides as highly selective 5-HT1D agonists: potential new treatment for migraine without cardiovascular side effects.
Published in: J Med Chem

Ligand: quetiapine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1997)
Median affinity: 5.7 pKi
Reference (Journal): Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
Published in: Psychopharmacology (Berl.)

Ligand: rauwolscine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.8 pKi
Reference (Journal): Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta.
Published in: Proc Natl Acad Sci USA

Ligand: risperidone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1993), EMA (2022)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
Published in: Psychopharmacology (Berl.)

Ligand: risperidone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1993), EMA (2022)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Alniditan, a new 5-hydroxytryptamine1D agonist and migraine-abortive agent: ligand-binding properties of human 5-hydroxytryptamine1D alpha, human 5-hydroxytryptamine1D beta, and calf 5-hydroxytryptamine1D receptors investigated with [3H]5-hydroxytryptamine and [3H]alniditan.
Published in: Mol Pharmacol

Ligand: ritanserin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.6 pKi
Reference (Journal): Alniditan, a new 5-hydroxytryptamine1D agonist and migraine-abortive agent: ligand-binding properties of human 5-hydroxytryptamine1D alpha, human 5-hydroxytryptamine1D beta, and calf 5-hydroxytryptamine1D receptors investigated with [3H]5-hydroxytryptamine and [3H]alniditan.
Published in: Mol Pharmacol

Ligand: rizatriptan (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1998)
Primary target: yes
Median affinity: 7.900000095367432 pKi
Reference (Journal): Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors.
Published in: Eur J Pharmacol

Ligand: roxindole (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.
Published in: J Pharmacol Exp Ther

Ligand: roxindole (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Actions of roxindole at recombinant human dopamine D2, D3 and D4 and serotonin 5-HT1A, 5-HT1B and 5-HT1D receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: RU 24969 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.7 pKi
Reference (Journal): Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor.
Published in: Mol Pharmacol

Ligand: S33084 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.9 pKi
Reference (Journal): S33084, a novel, potent, selective, and competitive antagonist at dopamine D(3)-receptors: I. Receptorial, electrophysiological and neurochemical profile compared with GR218,231 and L741,626.
Published in: J Pharmacol Exp Ther

Ligand: SB 216641 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 7.6 pKi
Reference (Journal): SB-216641 and BRL-15572--compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: SB 224289 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.3 pKi
Reference (Journal): SB-224289--a novel selective (human) 5-HT1B receptor antagonist with negative intrinsic activity.
Published in: Br J Pharmacol

Ligand: SB 224289 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.3 pKi
Reference (Journal): The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2, 4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydro- spiro[furo[2,3-f]indole-3,4'-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function both in vitro and in vivo.
Published in: J Med Chem

Ligand: SB 272183 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.7 pKi
Reference (Journal): SB-272183, a selective 5-HT(1A), 5-HT(1B) and 5-HT(1D) receptor antagonist in native tissue.
Published in: Br J Pharmacol

Ligand: SB 277011-A (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.8 pKi
Reference (Journal): Pharmacological actions of a novel, high-affinity, and selective human dopamine D(3) receptor antagonist, SB-277011-A.
Published in: J Pharmacol Exp Ther

Ligand: SB 649915 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.8 pKi
Reference (Journal): Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist.
Published in: J Med Chem

Ligand: SB 714786 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.100000381469727 pKi
Reference (Journal): Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist.
Published in: J Med Chem

Ligand: sertindole (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity: 7.2 pKi
Reference (Journal): Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
Published in: Psychopharmacology (Berl.)

Ligand: spiperone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor.
Published in: Mol Pharmacol

Ligand: spiperone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta.
Published in: Proc Natl Acad Sci USA

Ligand: sumatriptan (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1992)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta.
Published in: Proc Natl Acad Sci USA

Ligand: sumatriptan (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1992)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor.
Published in: Mol Pharmacol

Ligand: sumatriptan (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1992)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors.
Published in: Eur J Pharmacol

Ligand: sumatriptan (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1992)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Alniditan, a new 5-hydroxytryptamine1D agonist and migraine-abortive agent: ligand-binding properties of human 5-hydroxytryptamine1D alpha, human 5-hydroxytryptamine1D beta, and calf 5-hydroxytryptamine1D receptors investigated with [3H]5-hydroxytryptamine and [3H]alniditan.
Published in: Mol Pharmacol

Ligand: sumatriptan (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1992)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT(1B), 5-HT(1D) and dopamine D(2) and D(3) receptors. Significance for the modulation of frontocortical monoaminergic transmission and depressive states.
Published in: Synapse

Ligand: [125I]GTI (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.899999618530273 pKd
Reference (Journal): Biochemical and pharmacological characterization of serotonin-O-carboxymethylglycyl[125I]iodotyrosinamide, a new radioiodinated probe for 5-HT1B and 5-HT1D binding sites.
Published in: J Neurochem

Ligand: [125I]GTI (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.899999618530273 pKd
Reference (Journal): Autoradiographic characterisation and localisation of 5-HT1D compared to 5-HT1B binding sites in rat brain.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: [3H]5-CT (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 9.1 pKd
Reference (Journal): Serotonin 5-HT1B and 5-HT1D receptors form homodimers when expressed alone and heterodimers when co-expressed.
Published in: FEBS Lett

Ligand: [3H]5-HT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta.
Published in: Proc Natl Acad Sci USA

Ligand: [3H]5-HT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): SB-224289--a novel selective (human) 5-HT1B receptor antagonist with negative intrinsic activity.
Published in: Br J Pharmacol

Ligand: [3H]5-HT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Agonistic properties of alniditan, sumatriptan and dihydroergotamine on human 5-HT1B and 5-HT1D receptors expressed in various mammalian cell lines.
Published in: Br J Pharmacol

Ligand: [3H]8-OH-DPAT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9 pKd
Reference (Journal): Actions of roxindole at recombinant human dopamine D2, D3 and D4 and serotonin 5-HT1A, 5-HT1B and 5-HT1D receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: [3H]alniditan (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Agonistic properties of alniditan, sumatriptan and dihydroergotamine on human 5-HT1B and 5-HT1D receptors expressed in various mammalian cell lines.
Published in: Br J Pharmacol

Ligand: [3H]eletriptan (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.1 pKd
Reference (Journal): Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors.
Published in: Eur J Pharmacol

Ligand: [3H]GR 125,743 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.6 pKd
Reference (Journal): Serotonin 5-HT1B and 5-HT1D receptors form homodimers when expressed alone and heterodimers when co-expressed.
Published in: FEBS Lett

Ligand: [3H]sumatriptan (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.2 pKd
Reference (Journal): Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors.
Published in: Eur J Pharmacol

Ligand: terguride (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Median affinity: 7.8 pKi
Reference (Journal): Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.
Published in: J Pharmacol Exp Ther

Ligand: TFMPP (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta.
Published in: Proc Natl Acad Sci USA

Ligand: TFMPP (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor.
Published in: Mol Pharmacol

Ligand: tryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta.
Published in: Proc Natl Acad Sci USA

Ligand: tryptamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Alniditan, a new 5-hydroxytryptamine1D agonist and migraine-abortive agent: ligand-binding properties of human 5-hydroxytryptamine1D alpha, human 5-hydroxytryptamine1D beta, and calf 5-hydroxytryptamine1D receptors investigated with [3H]5-hydroxytryptamine and [3H]alniditan.
Published in: Mol Pharmacol

Ligand: vortioxetine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA and EMA (2013)
Primary target: no
Median affinity: 5.400000095367432 pIC50
Reference (Journal): Synthesis and structure--activity relationship in a class of indolebutylpiperazines as dual 5-HT(1A) receptor agonists and serotonin reuptake inhibitors.
Published in: J Med Chem

Ligand: (+)-WAY 100135 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.6 pKi
Reference (Journal): (+)-WAY 100135, a partial agonist, at native and recombinant 5-HT1B/1D receptors.
Published in: Br J Pharmacol

Ligand: xanomeline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.2 pKi
Reference (Journal): Functional effects of the muscarinic receptor agonist, xanomeline, at 5-HT1 and 5-HT2 receptors.
Published in: Br J Pharmacol

Ligand: yohimbine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (no date available)
Median affinity:  pKi
Reference (Journal): Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT(1B), 5-HT(1D) and dopamine D(2) and D(3) receptors. Significance for the modulation of frontocortical monoaminergic transmission and depressive states.
Published in: Synapse

Ligand: yohimbine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (no date available)
Median affinity:  pKi
Reference (Journal): Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor.
Published in: Mol Pharmacol

Ligand: yohimbine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (no date available)
Median affinity:  pKi
Reference (Journal): Alniditan, a new 5-hydroxytryptamine1D agonist and migraine-abortive agent: ligand-binding properties of human 5-hydroxytryptamine1D alpha, human 5-hydroxytryptamine1D beta, and calf 5-hydroxytryptamine1D receptors investigated with [3H]5-hydroxytryptamine and [3H]alniditan.
Published in: Mol Pharmacol

Ligand: yohimbine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (no date available)
Median affinity:  pKi
Reference (Journal): Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta.
Published in: Proc Natl Acad Sci USA

Ligand: ziprasidone (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (2001)
Median affinity: 9 pKi
Reference (Journal): Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
Published in: Psychopharmacology (Berl.)

Ligand: zolmitriptan (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1997)
Primary target: yes
Median affinity: 8.899999618530273 pKi
Reference (Journal): Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors.
Published in: Eur J Pharmacol

Ligand: zotepine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity: 9.3 pKi
Reference (Journal): Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.
Published in: Psychopharmacology (Berl.)