rizatriptan [Ligand Id: 51] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL905 (L-705126, MK-462, MK-462 FREE BASE, Rizatriptan, Maxalt, Maxalt-Mlt)
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
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  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
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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]
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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]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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  • GPR17/Uracil nucleotide/cysteinyl leukotriene receptor in Human [ChEMBL: CHEMBL1075162] [GtoPdb: 88] [UniProtKB: Q13304]
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  • 5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566]
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  • 5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
GtoPdb - - 6.4 pKi - - - Eur J Pharmacol (1999) 368: 259-68 [PMID:10193663]
ChEMBL Binding affinity for cloned human 5-hydroxytryptamine 1A receptor B 6.53 pKi 293 nM Ki J. Med. Chem. (1995) 38: 3602-3607 [PMID:7658447]
ChEMBL In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1A receptor B 6.85 pKi 140 nM Ki J. Med. Chem. (1999) 42: 526-531 [PMID:9986723]
ChEMBL Binding activity against 5-hydroxytryptamine 3 receptor from rat cortex homogenate using [3H]-Q-ICS 205-930 as radioligand. B 6.4 pIC50 398.11 nM IC50 J. Med. Chem. (1995) 38: 1799-1810 [PMID:7752204]
ChEMBL Binding activity against 5-hydroxytryptamine 1A receptor from pig cortex membrane using [3H]8-OH-DPAT-HT as radioligand. B 6.5 pIC50 316.23 nM IC50 J. Med. Chem. (1995) 38: 1799-1810 [PMID:7752204]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
GtoPdb - - 6.9 pKi - - - Eur J Pharmacol (1999) 368: 259-68 [PMID:10193663]
ChEMBL In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor B 8 pKi 10.1 nM Ki J. Med. Chem. (1999) 42: 526-531 [PMID:9986723]
ChEMBL Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement. B 7.39 pIC50 41 nM IC50 J. Med. Chem. (1997) 40: 3497-3500 [PMID:9357514]
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
ChEMBL Binding affinity for cloned human 5-hydroxytryptamine 1D receptor beta B 7.4 pKi 40 nM Ki J. Med. Chem. (1995) 38: 3602-3607 [PMID:7658447]
ChEMBL Binding affinity to recombinant human 5-hydroxytryptamine 1D receptor alpha B 7.87 pKi 13.5 nM Ki J. Med. Chem. (1995) 38: 3602-3607 [PMID:7658447]
GtoPdb - - 7.9 pKi - - - Eur J Pharmacol (1999) 368: 259-68 [PMID:10193663]
ChEMBL In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1D receptor B 8.37 pKi 4.3 nM Ki J. Med. Chem. (1999) 42: 526-531 [PMID:9986723]
ChEMBL Binding activity against 5-hydroxytryptamine 3 receptor from rat cortex homogenate using [3H]-Q-ICS 205-930 as radioligand. B 7.1 pIC50 79.43 nM IC50 J. Med. Chem. (1995) 38: 1799-1810 [PMID:7752204]
ChEMBL Binding affinity by displacement to human cloned 5-hydroxytryptamine 1D receptor in CHO cells by [3H]5-HT displacement. B 7.96 pIC50 11 nM IC50 J. Med. Chem. (1997) 40: 3497-3500 [PMID:9357514]
ChEMBL Measurement of agonist induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with 5-hydroxytryptamine 1D receptor. F 8.08 pEC50 8.4 nM EC50 J. Med. Chem. (1997) 40: 3497-3500 [PMID:9357514]
ChEMBL Ability to inhibit forskolin-stimulated adenylate cyclase in a cell line expressing human 5-hydroxytryptamine 1D receptor F 8.52 pEC50 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 activity against 5-hydroxytryptamine 2C receptor from human brain cortex using [3H]mesulergine as radioligand. B 7.3 pIC50 50.12 nM IC50 J. Med. Chem. (1995) 38: 1799-1810 [PMID:7752204]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL Binding activity against 5-hydroxytryptamine 2C receptor from human brain cortex using [3H]mesulergine as radioligand. B 5.1 pIC50 7943.28 nM IC50 J. Med. Chem. (1995) 38: 1799-1810 [PMID:7752204]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
ChEMBL Binding activity against 5-hydroxytryptamine 2C receptor from pig cortex membrane using [3H]mesulergine as radioligand. B 5.2 pIC50 6309.57 nM IC50 J. Med. Chem. (1995) 38: 1799-1810 [PMID:7752204]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL Binding activity against 5-hydroxytryptamine 2C receptor from human brain cortex using [3H]mesulergine as radioligand. B 5 pIC50 >10000 nM IC50 J. Med. Chem. (1995) 38: 1799-1810 [PMID:7752204]
ChEMBL Binding activity against 5-hydroxytryptamine 2C receptor from pig cortex membrane using [3H]mesulergine as radioligand. B 5.1 pIC50 7943.28 nM IC50 J. Med. Chem. (1995) 38: 1799-1810 [PMID:7752204]
5-HT3E/5-HT3B/5-HT3A/5-HT3D/5-HT3C/Serotonin 3 (5-HT3) receptor in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094132] [GtoPdb: 377374373376375] [UniProtKB: A5X5Y0O95264P46098Q70Z44Q8WXA8]
ChEMBL Binding activity against 5-hydroxytryptamine 1A receptor from human brain cortex using [3H]8-OH-DPAT-HT as radioligand. B 5 pIC50 >10000 nM IC50 J. Med. Chem. (1995) 38: 1799-1810 [PMID:7752204]
5-HT3A/5-HT3B/Serotonin 3 (5-HT3) receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094116] [GtoPdb: 373374] [UniProtKB: P35563Q9JJ16]
ChEMBL Binding activity radioligand. B 5.4 pIC50 3981.07 nM IC50 J. Med. Chem. (1995) 38: 1799-1810 [PMID:7752204]
GPR17/Uracil nucleotide/cysteinyl leukotriene receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075162] [GtoPdb: 88] [UniProtKB: Q13304]
ChEMBL Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of MDL 29,951-induced calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay F 4.52 pIC50 >30000 nM IC50 J Med Chem (2018) 61: 8136-8154 [PMID:30048589]
5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566]
GtoPdb - - 6.8 pKi - - - Eur J Pharmacol (1999) 368: 259-68 [PMID:10193663]
5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939]
GtoPdb - - 6.8 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2005) 371: 169-77 [PMID:15900510];
Eur J Pharmacol (1999) 368: 259-68 [PMID:10193663]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]