tertatolol [Ligand Id: 571] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL434200 (Artex, Tertatolol, S-2395)
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
  • 7.73
1 CHEMBL434200_lig_chart_1 Serotonin 1a (5-HT1a) receptor Rat
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  • β3-adrenoceptor in Human [GtoPdb: 30] [UniProtKB: P13945]
  • β3-adrenoceptor in Mouse [GtoPdb: 30] [UniProtKB: P25962]
  • β3-adrenoceptor in Rat [GtoPdb: 30] [UniProtKB: P26255]
  • 7
2 CHEMBL434200_lig_chart_2 β3-adrenoceptor HumanMouseRat
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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 Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL The compound was evaluated for binding affinity against 5-hydroxytryptamine 1A receptor in rat hippocampal membranes using [3H]8-OH-DPAT as radioligand in the presence of 3*10e-5 M GTP gamma S B 7.42 pKi 37.6 nM Ki Bioorg. Med. Chem. Lett. (1993) 3: 2035-2038
ChEMBL Binding affinity of a compound to rat brain 5-hydroxytryptamine 1A (serotonin) receptor assayed by radiolabeled [3H]-8-OH-DPAT ligand displacement B 7.73 pKi 18.62 nM Ki J. Med. Chem. (1996) 39: 126-134 [PMID:8568799]
ChEMBL Displacement of [3H]8-OH-DPAT from rat hippocampal 5-hydroxytryptamine 1A receptor B 7.74 pKi 18.2 nM Ki Bioorg. Med. Chem. Lett. (1993) 3: 2035-2038
ChEMBL The compound was evaluated for binding affinity against 5-hydroxytryptamine 1A receptor in rat hippocampal membranes using [3H]8-OH-DPAT as radioligand in the presence of 1 mM of MnCl2 B 8.11 pKi 7.71 nM Ki Bioorg. Med. Chem. Lett. (1993) 3: 2035-2038
β3-adrenoceptor in Human [GtoPdb: 30] [UniProtKB: P13945]
GtoPdb - - 8.6 pKi - - - Eur J Pharmacol (2004) 484: 323-31 [PMID:14744619]
β3-adrenoceptor in Mouse [GtoPdb: 30] [UniProtKB: P25962]
GtoPdb - - 7 pKi - - - Eur J Pharmacol (2004) 484: 323-31 [PMID:14744619]
β3-adrenoceptor in Rat [GtoPdb: 30] [UniProtKB: P26255]
GtoPdb - - 7 pKi - - - Eur J Pharmacol (2004) 484: 323-31 [PMID:14744619]

ChEMBL data shown on this page come from version 28:

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]