zolmitriptan [Ligand Id: 60] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1185 (311-C-90, 311C90, Cvt-427, NSC-760383, Zolmitriptan, Zomig, Zomig-zmt) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901] | ||||||||
| ChEMBL | Binding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligand | B | 9.52 | pKd | 0.3 | nM | Kd | J Med Chem (1995) 38: 3566-3580 [PMID:7658443] |
| D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
| ChEMBL | Binding affinity against Dopamine receptor D2 in rat striatum using [3H]-spiperone as radioligand | B | 10.4 | pKd | 0.04 | nM | Kd | J Med Chem (1995) 38: 3566-3580 [PMID:7658443] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Binding affinity against 5-hydroxytryptamine 1 receptor using rabbit jugular vein assay in the absence of endothelium | B | 8.74 | pKd | 1.8 | nM | Kd | J Med Chem (1995) 38: 3566-3580 [PMID:7658443] |
| GtoPdb | - | - | 6.6 | pKi | - | - | - | Eur J Pharmacol (1999) 368: 259-68 [PMID:10193663] |
| ChEMBL | In vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT radioligand | B | 6.91 | pKi | 124 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 675-680 [PMID:9871581] |
| ChEMBL | Binding affinity for cloned human 5-hydroxytryptamine 1A receptor | B | 7.1 | pKi | 78.6 | nM | Ki | J Med Chem (1995) 38: 3602-3607 [PMID:7658447] |
| 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222] | ||||||||
| ChEMBL | Binding affinity against 5-hydroxytryptamine 1D receptor beta using rabbit saphenous vein assay. | B | 8.82 | pKd | 1.5 | nM | Kd | J Med Chem (1995) 38: 3566-3580 [PMID:7658443] |
| GtoPdb | - | - | 7.7 | pKi | - | - | - | Eur J Pharmacol (1999) 368: 259-68 [PMID:10193663] |
| ChEMBL | In vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligand | B | 8.38 | pKi | 4.2 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 675-680 [PMID:9871581] |
| ChEMBL | Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor | B | 8.21 | pIC50 | 6.17 | nM | IC50 | J Med Chem (2001) 44: 681-693 [PMID:11262079] |
| 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 | 7.8 | pEC50 | 15.7 | nM | EC50 | Bioorg Med Chem Lett (1998) 8: 675-680 [PMID:9871581] |
| 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221] | ||||||||
| ChEMBL | Binding affinity against 5-hydroxytryptamine 1D receptor beta using rabbit saphenous vein assay. | B | 8.82 | pKd | 1.5 | nM | Kd | J Med Chem (1995) 38: 3566-3580 [PMID:7658443] |
| ChEMBL | Binding affinity for cloned human 5-hydroxytryptamine 1D receptor beta | B | 8.4 | pKi | 4 | nM | Ki | J Med Chem (1995) 38: 3602-3607 [PMID:7658447] |
| GtoPdb | - | - | 8.9 | pKi | - | - | - | Eur J Pharmacol (1999) 368: 259-68 [PMID:10193663] |
| ChEMBL | Binding affinity to recombinant human 5-hydroxytryptamine 1D receptor alpha | B | 9.04 | pKi | 0.92 | nM | Ki | J Med Chem (1995) 38: 3602-3607 [PMID:7658447] |
| ChEMBL | In vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1D receptor using [3H]5-CT radioligand | B | 9.12 | pKi | 0.76 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 675-680 [PMID:9871581] |
| ChEMBL | Binding affinity in CHO-K1 cells transfected with human 5-hydroxytryptamine 1D receptor | B | 8.55 | pIC50 | 2.82 | nM | IC50 | J Med Chem (2001) 44: 681-693 [PMID:11262079] |
| 5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566] | ||||||||
| GtoPdb | - | - | 7.7 | pKi | - | - | - | Eur J Pharmacol (1999) 368: 259-68 [PMID:10193663] |
| 5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939] | ||||||||
| GtoPdb | - | - | 7.5 | 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]
