tolazoline [Ligand Id: 7310] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL770 (Tolazoline, Priscoline)
  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
1 CHEMBL770_lig_chart_1 Serotonin 1b (5-HT1b) receptor Human
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  • 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
2 CHEMBL770_lig_chart_2 Serotonin 1d (5-HT1d) receptor Human
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  • TA1 receptor/Trace amine-associated receptor 1 in Human [ChEMBL: CHEMBL5857] [GtoPdb: 364] [UniProtKB: Q96RJ0]
  • This target only has 1 pki data point
3 CHEMBL770_lig_chart_3 Trace amine-associated receptor 1 Human
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  • α2A-adrenoceptor in Human [GtoPdb: 25] [UniProtKB: P08913]
  • This target only has 1 pki data point
4 CHEMBL770_lig_chart_4 α2A-adrenoceptor Human
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  • α2B-adrenoceptor in Human [GtoPdb: 26] [UniProtKB: P18089]
  • This target only has 1 pki data point
5 CHEMBL770_lig_chart_5 α2B-adrenoceptor Human
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  • α2C-adrenoceptor in Human [GtoPdb: 27] [UniProtKB: P18825]
  • This target only has 1 pki data point
6 CHEMBL770_lig_chart_6 α2C-adrenoceptor Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
ChEMBL Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand B 5 pKi >10000 nM Ki J. Med. Chem. (1998) 41: 2243-2251 [PMID:9632357]
ChEMBL Binding affinity towards human 5-hydroxytryptamine 1B receptor B 5 pKi >10000 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 4697-4699 [PMID:15324890]
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
ChEMBL Binding affinity towards human 5-hydroxytryptamine 1D receptor using [3H]5-HT trifluoroacetate as radioligand B 5 pKi >10000 nM Ki J. Med. Chem. (1998) 41: 2243-2251 [PMID:9632357]
ChEMBL Binding affinity towards human 5-hydroxytryptamine 1D receptor B 5 pKi >10000 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 4697-4699 [PMID:15324890]
TA1 receptor/Trace amine-associated receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5857] [GtoPdb: 364] [UniProtKB: Q96RJ0]
ChEMBL Displacement of (S)-4-(2,4-difluorophenyl-3-tritio) -4,5-dihydro-2-oxazolamine from human TAAR1 receptor expressed in HEK293 cells after 90 mins by beta counting analysis B 5.79 pKi 1640 nM Ki Bioorg. Med. Chem. Lett. (2012) 22: 5244-5248 [PMID:22795332]
α2A-adrenoceptor in Human [GtoPdb: 25] [UniProtKB: P08913]
GtoPdb Inhibition of agonist-stimulated [35S]GTPγS binding - 6.7 pKi 199 nM Ki Biochem. Pharmacol. (1998) 55: 1035-43 [PMID:9605427]
α2B-adrenoceptor in Human [GtoPdb: 26] [UniProtKB: P18089]
GtoPdb Inhibition of agonist-stimulated [35S]GTPγS binding - 5.5 pKi 3162 nM Ki Biochem. Pharmacol. (1998) 55: 1035-43 [PMID:9605427]
α2C-adrenoceptor in Human [GtoPdb: 27] [UniProtKB: P18825]
GtoPdb Inhibition of agonist-stimulated [35S]GTPγS binding - 5.43 pKi 3715 nM Ki Biochem. Pharmacol. (1998) 55: 1035-43 [PMID:9605427]

ChEMBL data shown on this page come from version 27:

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