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 (Antipressan, Atenamin, Atenix-100, Atenix-25, Atenix-50, Atenolol, Atenololum, Betacard, C07AB03, Corotenol, Duraatenolol, Esatenolol, Ibinolo, ICI 66082, ICI 66,082, ICI-66082, Juvental, Kentol, Myocord, Novaten, NSC-757832, Prenormine, Tenormin, Tenormin 25, Tenormin l.s., Totamol, Unibloc, Urosin, Vasaten) |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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 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 32:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]