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) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
|
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: 377, 374, 373, 376, 375] [UniProtKB: A5X5Y0, O95264, P46098, Q70Z44, Q8WXA8] | ||||||||
| 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: 373, 374] [UniProtKB: P35563, Q9JJ16] | ||||||||
| 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
