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ChEMBL ligand: CHEMBL905 (L-705126, Maxalt, Maxalt-Mlt, MK-462, MK-462 FREE BASE, Rizatriptan) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 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]