sumatriptan [Ligand Id: 54] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL128 (Imitrex, N02CC01, Sumatriptan, Tosymra)
  • 5-hydroxytryptamine 1D receptor in Bovine [ChEMBL: CHEMBL3638336] [UniProtKB: Q8MI13]
  • This target only has 0 pki data point
  • 0
1 CHEMBL128_lig_chart_1 5-hydroxytryptamine 1D receptor Bovine
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
  • 6.66
2 CHEMBL128_lig_chart_2 Dopamine D2 receptor HumanRat
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  • Multidrug and toxin extrusion/Multidrug and toxin extrusion protein 1 in Human [ChEMBL: CHEMBL1743126] [GtoPdb: 1216] [UniProtKB: Q96FL8]
  • This target only has 0 pki data point
  • 0
3 CHEMBL128_lig_chart_3 Multidrug and toxin extrusion protein 1 Human
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Mouse [ChEMBL: CHEMBL3737] [GtoPdb: 1] [UniProtKB: Q64264]
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
  • 6.34
4 CHEMBL128_lig_chart_4 Serotonin 1a (5-HT1a) receptor HumanMouseRat
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  • Serotonin 1b (5-HT1b) receptor in Gorilla [ChEMBL: CHEMBL2304408] [UniProtKB: Q9N2B7]
  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
  • 7.86
5 CHEMBL128_lig_chart_5 Serotonin 1b (5-HT1b) receptor GorillaHumanRat
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  • 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
  • Serotonin 1d (5-HT1d) receptor in Pig [ChEMBL: CHEMBL4105] [UniProtKB: P79400]
  • 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Rat [ChEMBL: CHEMBL5450] [GtoPdb: 3] [UniProtKB: P28565]
  • 0
6 CHEMBL128_lig_chart_6 Serotonin 1d (5-HT1d) receptor HumanPigRat
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  • 5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566]
  • This target only has 1 pki data point
  • 5.8
7 CHEMBL128_lig_chart_7 Serotonin 1e (5-HT1e) receptor Human
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  • 5-HT1F receptor/Serotonin 1f (5-HT1f) receptor in Human [ChEMBL: CHEMBL1805] [GtoPdb: 5] [UniProtKB: P30939]
  • 7.75
8 CHEMBL128_lig_chart_8 Serotonin 1f (5-HT1f) receptor Human
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
  • 0
9 CHEMBL128_lig_chart_9 Serotonin 2a (5-HT2a) receptor HumanRat
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
  • This target only has 1 pki data point
  • 6
10 CHEMBL128_lig_chart_10 Serotonin 2c (5-HT2c) receptor HumanRat
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11 CHEMBL128_lig_chart_11 Serotonin 3 (5-HT3) receptor HumanRat
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  • 5-HT3A/Serotonin 3a (5-HT3a) receptor in Human [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
  • This target only has 0 pki data point
  • 0
12 CHEMBL128_lig_chart_12 Serotonin 3a (5-HT3a) receptor Human
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  • 5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898]
  • 5-HT5A receptor in Mouse [GtoPdb: 10] [UniProtKB: P30966]
  • 4.8
13 CHEMBL128_lig_chart_13 Serotonin 5a (5-HT5a) receptor HumanMouse
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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
  • 5-HT7 receptor in Rat [GtoPdb: 12] [UniProtKB: P32305]
  • 6.6
14 CHEMBL128_lig_chart_14 Serotonin 7 (5-HT7) receptor HumanRat
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  • 5-HT6 receptor in Human [GtoPdb: 11] [UniProtKB: P50406]
  • 5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
  • 5.2
15 CHEMBL128_lig_chart_15 5-HT6 receptor HumanRat
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-hydroxytryptamine 1D receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3638336] [UniProtKB: Q8MI13]
ChEMBL Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12). B 7.23 pIC50 59 nM IC50 US-8586620-B2. Substituted indole compounds having NOS inhibitory activity (2013)
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL The compound was tested for CNS binding affinity towards Dopamine receptor D2 from cloned Human membranes. B 6.66 pKi >218 nM Ki J. Med. Chem. (1998) 41: 2180-2183 [PMID:9632349]
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL Binding affinity for rat dopamine D2 receptor expressed in CHO-K1 cells B 6.66 pKi >218 nM Ki J. Med. Chem. (1996) 39: 4717-4726 [PMID:8941384]
Multidrug and toxin extrusion/Multidrug and toxin extrusion protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743126] [GtoPdb: 1216] [UniProtKB: Q96FL8]
ChEMBL Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay B 5.17 pIC50 6700 nM IC50 J. Med. Chem. (2013) 56: 781-795 [PMID:23241029]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Binding affinity for 5-hydroxytryptamine 1A receptor in piglet hippocampus using [3H]8-OH-DPAT B 5.5 pKd 5.5 - pKD J. Med. Chem. (1993) 36: 1918-1919 [PMID:8515429]
ChEMBL Binding affinity to 5HT1A receptor B 6.4 pKd 398.11 nM Kd J. Med. Chem. (2009) 52: 6107-6125 [PMID:19754201]
GtoPdb - - 6 pKi - - - Eur J Pharmacol (1999) 368: 259-68 [PMID:10193663]
ChEMBL Binding affinity towards cloned human 5-hydroxy tryptamine 1A (5-HT1A) receptor was determined B 6.36 pKi 440 nM Ki Bioorg. Med. Chem. Lett. (1995) 5: 663-666
ChEMBL Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1A receptor in CHO-K1 cells F 6.36 pKi 440 nM Ki J. Med. Chem. (1996) 39: 4920-4927 [PMID:8960551]
ChEMBL Binding affinity for cloned human 5-hydroxytryptamine 1A receptor B 6.36 pKi 440 nM Ki J. Med. Chem. (1995) 38: 3602-3607 [PMID:7658447]
ChEMBL In vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT radioligand B 6.39 pKi 407.1 nM Ki Bioorg. Med. Chem. Lett. (1998) 8: 675-680 [PMID:9871581]
ChEMBL The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1A receptor from cloned Human membranes. B 6.47 pKi 341 nM Ki J. Med. Chem. (1998) 41: 2180-2183 [PMID:9632349]
ChEMBL Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1A receptor expressed in CHO-K1 cells. B 6.47 pKi 341 nM Ki J. Med. Chem. (1996) 39: 4717-4726 [PMID:8941384]
ChEMBL In vitro affinity at human cloned 5-hydroxytryptamine 1A receptor by [3H]8-OH-DPAT displacement. B 6.48 pKi 330 nM Ki J. Med. Chem. (1996) 39: 314-322 [PMID:8568822]
ChEMBL Binding affinity was measured on 5-hydroxytryptamine 1A receptor in AK cells transfected with human 5-HT1A gene labeled with [3H]-8-OH-DPAT B 6.48 pKi 330 nM Ki J. Med. Chem. (1994) 37: 2828-2830 [PMID:8071931]
ChEMBL In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1A receptor B 6.64 pKi 230 nM Ki J. Med. Chem. (1999) 42: 526-531 [PMID:9986723]
ChEMBL Binding activity radioligand. B 6.3 pIC50 501.19 nM IC50 J. Med. Chem. (1995) 38: 1799-1810 [PMID:7752204]
ChEMBL Binding activity radioligand. B 6.4 pIC50 398.11 nM IC50 J. Med. Chem. (1995) 38: 1799-1810 [PMID:7752204]
ChEMBL Ability to bind to 5-hydroxytryptamine 1A receptor from cloned human expressed in Ha7 cells B 6.4 pIC50 398.11 nM IC50 Bioorg. Med. Chem. Lett. (1995) 5: 2649-2654
ChEMBL Compound was tested for its ability to inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-HT 1A receptor in HeLa cells F 6 pEC50 >1000 nM EC50 Bioorg. Med. Chem. Lett. (1995) 5: 663-666
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3737] [GtoPdb: 1] [UniProtKB: Q64264]
ChEMBL Compound was evaluated for the affinity at 5-hydroxytryptamine 1A receptor B 6.35 pIC50 450 nM IC50 J. Med. Chem. (1997) 40: 3501-3503 [PMID:9357515]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) B 6.34 pKi 459 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) B 6.09 pIC50 804 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Binding affinity was measured against serotonin 5-hydroxytryptamine 1A receptor B 6.19 pIC50 640 nM IC50 J. Med. Chem. (1994) 37: 2509-2512 [PMID:8057297]
ChEMBL Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor F 5.89 pEC50 1300 nM EC50 J. Med. Chem. (1994) 37: 2509-2512 [PMID:8057297]
Serotonin 1b (5-HT1b) receptor in Gorilla (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304408] [UniProtKB: Q9N2B7]
ChEMBL The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells B 8.19 pKi 6.4 nM Ki J. Med. Chem. (1998) 41: 2180-2183 [PMID:9632349]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
ChEMBL Binding affinity towards cloned human 5-hydroxytryptamine 1B receptor B 7.32 pKi 47.9 nM Ki Bioorg. Med. Chem. Lett. (2000) 10: 1707-1709 [PMID:10937729]
ChEMBL Binding affinity for human 5-hydroxytryptamine 1B receptor B 7.44 pKi 36 nM Ki Bioorg. Med. Chem. Lett. (2000) 10: 903-905 [PMID:10853656]
ChEMBL Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP. F 7.62 pKi 24 nM Ki J. Med. Chem. (1996) 39: 4717-4726 [PMID:8941384]
ChEMBL Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells F 7.64 pKi 23.1 nM Ki J. Med. Chem. (1996) 39: 4920-4927 [PMID:8960551]
ChEMBL The compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta B 7.64 pKi 23.1 nM Ki J. Med. Chem. (1995) 38: 3602-3607 [PMID:7658447]
ChEMBL Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells. B 7.66 pKi 22 nM Ki J. Med. Chem. (1996) 39: 4717-4726 [PMID:8941384]
ChEMBL In vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligand B 7.72 pKi 19.1 nM Ki Bioorg. Med. Chem. Lett. (1998) 8: 675-680 [PMID:9871581]
ChEMBL Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta B 8 pKi 10 nM Ki J. Med. Chem. (1996) 39: 314-322 [PMID:8568822]
ChEMBL In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor B 8.02 pKi 9.6 nM Ki J. Med. Chem. (1999) 42: 526-531 [PMID:9986723]
ChEMBL Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting B 8.04 pKi 9.1 nM Ki J. Med. Chem. (2008) 51: 3609-3616 [PMID:18507369]
GtoPdb - - 8.1 pKi 7.94 nM Ki Eur J Pharmacol (1999) 380: 171-81 [PMID:10513577];
Mol Pharmacol (1996) 50: 1567-80 [PMID:8967979];
Synapse (2000) 35: 79-95 [PMID:10611634];
Eur J Pharmacol (1999) 368: 259-68 [PMID:10193663];
Mol Pharmacol (2000) 58: 1042-9 [PMID:11040052];
J Neurochem (1996) 67: 2096-103 [PMID:8863519];
Proc Natl Acad Sci USA (1992) 89: 3630-4 [PMID:1565658]
ChEMBL Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor B 8.11 pKi 7.7 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 727-729 [PMID:14741277]
ChEMBL Binding affinity towards cloned human 5-hydroxytryptamine 1B receptor B 8.11 pKi 7.7 nM Ki Bioorg. Med. Chem. Lett. (2003) 13: 3419-3421 [PMID:14505640]
ChEMBL Binding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HT B 8.26 pKi 5.5 nM Ki J. Med. Chem. (1994) 37: 2828-2830 [PMID:8071931]
ChEMBL Compound was evaluated for the affinity at 5-hydroxytryptamine 1B receptor B 7.57 pIC50 27 nM IC50 J. Med. Chem. (1997) 40: 3501-3503 [PMID:9357515]
ChEMBL Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells B 7.8 pIC50 16 nM IC50 J. Med. Chem. (1997) 40: 3501-3503 [PMID:9357515]
ChEMBL Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement. B 7.8 pIC50 16 nM IC50 J. Med. Chem. (1997) 40: 3497-3500 [PMID:9357514]
ChEMBL Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells. B 7.96 pIC50 11 nM IC50 J. Med. Chem. (1999) 42: 691-705 [PMID:10052976]
ChEMBL Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells B 7.96 pIC50 11 nM IC50 J. Med. Chem. (1999) 42: 677-690 [PMID:10052975]
ChEMBL Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement. B 8 pIC50 10 nM IC50 J. Med. Chem. (1999) 42: 4981-5001 [PMID:10585208]
ChEMBL Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor B 9.3 pIC50 0.5 nM IC50 J. Med. Chem. (2001) 44: 681-693 [PMID:11262079]
ChEMBL Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells F 7.11 pEC50 77 nM EC50 J. Med. Chem. (1996) 39: 4920-4927 [PMID:8960551]
ChEMBL Effective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell lines F 7.42 pEC50 38.3 nM EC50 Bioorg. Med. Chem. Lett. (1998) 8: 675-680 [PMID:9871581]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
ChEMBL Binding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HT B 7.64 pKi 23 nM Ki J. Med. Chem. (1994) 37: 2828-2830 [PMID:8071931]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol) B 8.09 pKi 8.19 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12). B 6.96 pIC50 110 nM IC50 US-8586620-B2. Substituted indole compounds having NOS inhibitory activity (2013)
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol) B 7.74 pIC50 18 nM IC50 DrugMatrix in vitro pharmacology data
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
ChEMBL Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor alpha measured as the reduction of forskolin-stimulated cAMP. F 7.52 pKi 30 nM Ki J. Med. Chem. (1996) 39: 4717-4726 [PMID:8941384]
ChEMBL Binding affinity towards cloned human 5-hydroxytryptamine 1D receptor beta was determined B 7.64 pKi 23.1 nM Ki Bioorg. Med. Chem. Lett. (1995) 5: 663-666
ChEMBL Binding affinity for human 5-hydroxytryptamine 1D receptor B 7.96 pKi 11 nM Ki Bioorg. Med. Chem. Lett. (2000) 10: 903-905 [PMID:10853656]
ChEMBL In vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1D receptor using [3H]5-CT radioligand B 8.07 pKi 8.6 nM Ki Bioorg. Med. Chem. Lett. (1998) 8: 675-680 [PMID:9871581]
ChEMBL Binding affinity towards cloned human 5-hydroxytryptamine 1D receptor alpha was determined B 8.07 pKi 8.5 nM Ki Bioorg. Med. Chem. Lett. (1995) 5: 663-666
ChEMBL Binding affinity to recombinant human 5-hydroxytryptamine 1D receptor alpha B 8.07 pKi 8.5 nM Ki J. Med. Chem. (1995) 38: 3602-3607 [PMID:7658447]
ChEMBL Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1D receptor in CHO-K1 cells F 8.07 pKi 8.5 nM Ki J. Med. Chem. (1996) 39: 4920-4927 [PMID:8960551]
ChEMBL Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor alpha expressed in CHO-K1 cells. B 8.24 pKi 5.7 nM Ki J. Med. Chem. (1996) 39: 4717-4726 [PMID:8941384]
ChEMBL Binding affinity for human 5-hydroxytryptamine 1D receptor B 8.26 pKi 5.5 nM Ki Bioorg. Med. Chem. Lett. (2000) 10: 1707-1709 [PMID:10937729]
ChEMBL In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1D receptor B 8.36 pKi 4.4 nM Ki J. Med. Chem. (1999) 42: 526-531 [PMID:9986723]
ChEMBL Binding affinity towards cloned human 5-hydroxytryptamine 1D receptor B 8.47 pKi 3.4 nM Ki Bioorg. Med. Chem. Lett. (2003) 13: 3419-3421 [PMID:14505640]
ChEMBL Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1D receptor B 8.47 pKi 3.4 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 727-729 [PMID:14741277]
ChEMBL The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1D receptor from cloned gorilla membranes expressed in cultured HEK 293 cells B 8.7 pKi 2 nM Ki J. Med. Chem. (1998) 41: 2180-2183 [PMID:9632349]
GtoPdb - - 8.7 pKi 1.99 nM Ki Synapse (2000) 35: 79-95 [PMID:10611634];
Eur J Pharmacol (1999) 368: 259-68 [PMID:10193663];
Proc Natl Acad Sci USA (1992) 89: 3630-4 [PMID:1565658];
Mol Pharmacol (1996) 50: 1567-80 [PMID:8967979];
Mol Pharmacol (1991) 40: 143-8 [PMID:1652050]
ChEMBL Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1D receptor expressed in CHOK1 cells by liquid scintillation counting B 8.92 pKi 1.2 nM Ki J. Med. Chem. (2008) 51: 3609-3616 [PMID:18507369]
ChEMBL Compound was evaluated for the affinity at 5-hydroxytryptamine 1D receptor B 5.62 pIC50 2400 nM IC50 J. Med. Chem. (1997) 40: 3501-3503 [PMID:9357515]
ChEMBL Ability to bind to 5-hydroxytryptamine 1D receptor of calf substantia nigra B 7 pIC50 100 nM IC50 Bioorg. Med. Chem. Lett. (1995) 5: 2649-2654
ChEMBL Binding activity radioligand. B 7.4 pIC50 39.81 nM IC50 J. Med. Chem. (1995) 38: 1799-1810 [PMID:7752204]
ChEMBL Compound was tested for the displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1D receptor stably expressed in CHO cells. B 8.17 pIC50 6.8 nM IC50 J. Med. Chem. (1999) 42: 4981-5001 [PMID:10585208]
ChEMBL Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1D receptor stably expressed in CHO cells B 8.17 pIC50 6.7 nM IC50 J. Med. Chem. (1999) 42: 677-690 [PMID:10052975]
ChEMBL Displacement of [3H]5-HT binding from human 5-hydroxytryptamine 1D receptor expressed in CHO cells B 8.17 pIC50 6.7 nM IC50 J. Med. Chem. (1999) 42: 691-705 [PMID:10052976]
ChEMBL Displacement of [3H]5-HT from human 5-hydroxytryptamine 1D receptor expressed in CHO cells B 8.3 pIC50 5 nM IC50 J. Med. Chem. (1997) 40: 3501-3503 [PMID:9357515]
ChEMBL Binding affinity by displacement to human cloned 5-hydroxytryptamine 1D receptor in CHO cells by [3H]5-HT displacement. B 8.3 pIC50 5 nM IC50 J. Med. Chem. (1997) 40: 3497-3500 [PMID:9357514]
ChEMBL Binding affinity in CHO-K1 cells transfected with human 5-hydroxytryptamine 1D receptor B 8.53 pIC50 2.95 nM IC50 J. Med. Chem. (2001) 44: 681-693 [PMID:11262079]
ChEMBL Compound was tested for 5-hydroxytryptamine 1D like receptor-mediated vascular effect in rabbit saphenous vein (RSV) B 6.66 pEC50 220 nM EC50 J. Med. Chem. (1998) 41: 2243-2251 [PMID:9632357]
ChEMBL Compound was tested for its ability inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-hydroxytryptamine 1D receptor beta in CHO-K1 cells; value ranges from 30-70 F 7.52 pEC50 30 nM EC50 Bioorg. Med. Chem. Lett. (1995) 5: 663-666
ChEMBL Compound was evaluated for the stimulation of [35S]GTP-gamma-S, binding in CHO cells expressing the 5-hydroxytryptamine 1D receptor. F 7.8 pEC50 16 nM EC50 J. Med. Chem. (1997) 40: 3501-3503 [PMID:9357515]
ChEMBL Measurement of agonist induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with 5-hydroxytryptamine 1D receptor. F 7.8 pEC50 16 nM EC50 J. Med. Chem. (1997) 40: 3497-3500 [PMID:9357514]
ChEMBL Stimulation of [35S]GTP-gamma-S, binding in CHO cells expressing the 5-hydroxytryptamine 1D receptor F 7.85 pEC50 14 nM EC50 J. Med. Chem. (1999) 42: 677-690 [PMID:10052975]
ChEMBL Stimulation of [35S]GTP-gamma-S, binding in CHO cells expressing the 5-hydroxytryptamine 1D receptor F 7.85 pEC50 14 nM EC50 J. Med. Chem. (1999) 42: 691-705 [PMID:10052976]
ChEMBL Agonist-induced [35S]- GTPgammaS binding in CHO cells stably transfected with 5-hydroxytryptamine 1D receptor B 7.92 pEC50 12 nM EC50 J. Med. Chem. (1999) 42: 4981-5001 [PMID:10585208]
ChEMBL Ability to inhibit forskolin-stimulated adenylate cyclase activity in Chinese hamster ovary (CHO) stable cell lines expressing human 5-hydroxytryptamine 1D receptor F 8.28 pEC50 5.3 nM EC50 Bioorg. Med. Chem. Lett. (2003) 13: 4409-4413 [PMID:14643336]
ChEMBL Ability to inhibit forskolin-stimulated adenylate cyclase in a cell line expressing human 5-hydroxytryptamine 1D receptor F 8.37 pEC50 4.3 nM EC50 J. Med. Chem. (1999) 42: 526-531 [PMID:9986723]
Serotonin 1d (5-HT1d) receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105] [UniProtKB: P79400]
ChEMBL Binding affinity for 5-hydroxytryptamine 1D receptor in piglet caudate using [3H]5-HT B 7.6 pKd 7.6 - pKD J. Med. Chem. (1993) 36: 1918-1919 [PMID:8515429]
ChEMBL Binding activity radioligand. B 7.7 pIC50 19.95 nM IC50 J. Med. Chem. (1995) 38: 1799-1810 [PMID:7752204]
ChEMBL Displacement of radioligand [3H]5-HT binding to 5-hydroxytryptamine 1D receptor in pig caudate membrane B 7.7 pIC50 19.95 nM IC50 J. Med. Chem. (1993) 36: 1529-1538 [PMID:8496922]
ChEMBL Displacement of [3H]5-HT binding to 5-hydroxytryptamine 1D receptor from pig caudate membrane B 7.7 pIC50 19.95 nM IC50 J. Med. Chem. (1994) 37: 3023-3032 [PMID:7932524]
ChEMBL Compound was tested for the displacement of [3H]-5-HT to 5-hydroxytryptamine 1D receptor recognition sites in pig caudate membranes B 7.7