ChEMBL ligand: CHEMBL24 (Antipressan, Atenamin, Atenix-100, Atenix-25, Atenix-50, Atenolol, Atenololum, Betacard, C07AB03, Corotenol, Duraatenolol, Esatenolol, Ibinolo, ICI 66,082, ICI 66082, 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] β1-adrenoceptor in Rat [GtoPdb: 28] [UniProtKB: P18090] 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!
Urease in Canavalia ensiformis [ChEMBL: CHEMBL4161] [UniProtKB: P07374] 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]
β1-adrenoceptor in Rat [GtoPdb: 28] [UniProtKB: P18090]
GtoPdb	-	-	6.8	pA2	-	-	-	Life Sci (2020) 241: 117155 [PMID:31837330]
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]
Urease in Canavalia ensiformis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4161] [UniProtKB: P07374]
ChEMBL	Inhibition of jack bean urease assessed as reduction on ammonia production using urea as substrate preincubated for 15 mins followed by substrate addition and measured after 15 mins by indophenol method	B	4.19	pIC50	64360	nM	IC50	Eur J Med Chem (2022) 234: 114273-114273 [PMID:35305460]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]