zolmitriptan [Ligand Id: 60] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1185 (311C90, 311-C-90, Cvt-427, NSC-760383, Zolmitriptan, Zomig, Zomig-zmt)
  • D1 receptor/Dopamine D1 receptor in Rat [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
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  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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  • 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]
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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
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 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]