atenolol [Ligand Id: 548] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL24 (Atenix-25, Unibloc, C07AB03, Esatenolol, Tenormin 25, Kentol, Atenolol, Totamol, Vasaten, Antipressan, Tenormin L.S., Atenamin, Atenix-100, Ibinolo, ICI 66082, ICI-66082, Atenix-50, Tenormin)
  • β1-adrenoceptor/Beta-1 adrenergic receptor in Human [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
  • Beta-1 adrenergic receptor in Guinea pig [ChEMBL: CHEMBL5471] [UniProtKB: B0FL73]
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  • β2-adrenoceptor/Beta-2 adrenergic receptor in Human [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
  • Beta-2 adrenergic receptor in Guinea pig [ChEMBL: CHEMBL5414] [UniProtKB: Q8K4Z4]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
ChEMBL Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation counting B 5.82 pKi 1513.56 nM Ki J Med Chem (2018) 61: 5380-5394 [PMID:29851481]
ChEMBL DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) B 6.12 pKi 758 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Displacement of radiolabeled atenolol from human adrenergic beta-1 receptor B 6.37 pKi 430 nM Ki J. Med. Chem. (2008) 51: 7094-7098 [PMID:18983139]
ChEMBL Displacement of [3H](-)-CGP12177 from human adrenergic beta1 receptor B 6.77 pKi 170 nM Ki J. Med. Chem. (2011) 54: 5320-5334 [PMID:21726069]
ChEMBL Binding affinity to human adrenergic beta1 receptor by radioligand displacement assay B 6.82 pKi 150 nM Ki Eur. J. Med. Chem. (2013) 63: 85-94 [PMID:23466604]
GtoPdb - - 7.6 pKi - - - Naunyn Schmiedebergs Arch. Pharmacol. (2004) 369: 525-32 [PMID:15060759];
Eur. J. Pharmacol. (1999) 367: 431-5 [PMID:10079020];
Br. J. Pharmacol. (2005) 144: 317-22 [PMID:15655528]
ChEMBL Inhibition of human beta 1 adrenergic receptor B 5.76 pIC50 1740 nM IC50 J. Med. Chem. (2008) 51: 4150-4169 [PMID:18588282]
ChEMBL Inhibition of human alpha1 adrenoceptor B 5.79 pIC50 1640 nM IC50 Bioorg. Med. Chem. (2010) 18: 7675-7699 [PMID:20875743]
ChEMBL DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) B 5.88 pIC50 1313 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Displacement of radiolabeled atenolol from human adrenergic beta-1 receptor B 6.22 pIC50 600 nM IC50 J. Med. Chem. (2008) 51: 7094-7098 [PMID:18983139]
ChEMBL Binding affinity to human adrenergic beta1 receptor by radioligand displacement assay B 6.59 pIC50 260 nM IC50 Eur. J. Med. Chem. (2013) 63: 85-94 [PMID:23466604]
ChEMBL Displacement of [3H]CGP 12177 from human recombinant beta1 adrenergic receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method B 6.68 pIC50 210 nM IC50 Bioorg Med Chem (2017) 25: 471-482 [PMID:27876250]
ChEMBL Displacement of [3H](-)CGP12177 from human recombinant Beta-1 adrenergic receptor expressed in HEK293 cells B 6.68 pIC50 210 nM IC50 Bioorg. Med. Chem. (2016) 24: 1793-1810 [PMID:26988801]
ChEMBL Percent inhibition against Beta-1 adrenergic receptor at 1 uM B 8.75 pIC50 1.77 nM IC50 J. Med. Chem. (2005) 48: 6887-6896 [PMID:16250647]
Beta-1 adrenergic receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5471] [UniProtKB: B0FL73]
ChEMBL Activity at beta-1 adrenergic receptor B 6.8 pKd 158.49 nM Kd J. Med. Chem. (1992) 35: 4676-4682 [PMID:1361581]
ChEMBL Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 mins B 7.36 pKd 43.65 nM Kd J. Med. Chem. (1978) 21: 1081-1084 [PMID:31474]
ChEMBL In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations B 7.62 pKd 23.99 nM Kd J. Med. Chem. (1983) 26: 950-957 [PMID:6134834]
ChEMBL In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria B 7.62 pKd 23.99 nM Kd J. Med. Chem. (1986) 29: 1065-1080 [PMID:2872332]
β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
ChEMBL DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177) B 5 pKi 10061 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting B 5.02 pKi 9549.93 nM Ki J Med Chem (2018) 61: 5380-5394 [PMID:29851481]
GtoPdb - - 6 pKi - - - Eur. J. Pharmacol. (1999) 367: 431-5 [PMID:10079020];
Br. J. Pharmacol. (2005) 144: 317-22 [PMID:15655528]
ChEMBL DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177) B 4.83 pIC50 14634 nM IC50 DrugMatrix in vitro pharmacology data
Beta-2 adrenergic receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5414] [UniProtKB: Q8K4Z4]
ChEMBL Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins B 5.9 pKd 1258.93 nM Kd J. Med. Chem. (1978) 21: 1081-1084 [PMID:31474]
ChEMBL In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha B 5.93 pKd 1174.9 nM Kd J. Med. Chem. (1983) 26: 950-957 [PMID:6134834]
ChEMBL In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea B 5.93 pKd 1174.9 nM Kd J. Med. Chem. (1986) 29: 1065-1080 [PMID:2872332]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL Binding affinity of a compound to rat brain 5-hydroxytryptamine 1A (serotonin) receptor assayed by radiolabeled [3H]-8-OH-DPAT ligand displacement B 5 pKi 10000 nM Ki J. Med. Chem. (1996) 39: 126-134 [PMID:8568799]

ChEMBL data shown on this page come from version 26:

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]