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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL905 (L-705126, Maxalt, Maxalt-Mlt, MK-462, MK-462 FREE BASE, Rizatriptan)
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • GPR17/Uracil nucleotide/cysteinyl leukotriene receptor in Human [ChEMBL: CHEMBL1075162] [GtoPdb: 88] [UniProtKB: Q13304]
There should be some charts here, you may need to enable JavaScript!
  • 5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939]
There should be some charts here, you may need to enable JavaScript!
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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]