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)
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] 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] 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] 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 31:

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]