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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL24 (Tenormin l.s., Atenix-25, ICI 66,082, Unibloc, C07AB03, Esatenolol, Tenormin 25, Kentol, Atenolol, Totamol, Vasaten, Antipressan, Atenamin, Atenix-100, Ibinolo, ICI 66082, Atenix-50, ICI-66082, 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]
  • 0
1 CHEMBL24_lig_chart_1 Beta-1 adrenergic receptor HumanGuinea pig
There should be some charts here, you may need to enable JavaScript!
  • 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]
  • 0
2 CHEMBL24_lig_chart_2 Beta-2 adrenergic receptor HumanGuinea pig
There should be some charts here, you may need to enable JavaScript!
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
  • This target only has 1 pki data point
  • 5
3 CHEMBL24_lig_chart_3 Serotonin 1a (5-HT1a) receptor Rat
There should be some charts here, you may need to enable JavaScript!
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 Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting B 5.92 pKd 1200 nM Kd J Med Chem (2016) 59: 5780-5789 [PMID:27239696]
ChEMBL Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting B 5.92 pKd 1200 nM Kd J Med Chem (2016) 59: 5780-5789 [PMID:27239696]
ChEMBL Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting B 6.59 pKd 260 nM Kd J Med Chem (2016) 59: 5780-5789 [PMID:27239696]
ChEMBL Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting B 6.59 pKd 260 nM Kd J Med Chem (2016) 59: 5780-5789 [PMID:27239696]
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 28:

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]