ChEMBL ligand: CHEMBL13 (Beatrolol, CGP-2175, Dl-metoprolol, Lopressidone, Metoprolol, Metoprolol slow release, (rs)-metoprolol, Seroken, Toprol-XL)
β1-adrenoceptor/Beta-1 adrenergic receptor in Human [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588] β1-adrenoceptor/Beta-1 adrenergic receptor in Mouse [ChEMBL: CHEMBL3440] [GtoPdb: 28] [UniProtKB: P34971] β1-adrenoceptor/Beta-1 adrenergic receptor in Rat [ChEMBL: CHEMBL3252] [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!

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	Antagonist activity against beta-1 adrenergic receptor (unknown origin)	B	7.8	pKd	15.85	nM	Kd	J Med Chem (2015) 58: 5691-5698 [PMID:25799158]
ChEMBL	DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)	B	6.99	pKi	102	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Displacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T cell membranes	B	7.26	pKi	55	nM	Ki	Bioorg Med Chem (2019) 27: 2959-2971 [PMID:31151791]
GtoPdb	-	-	7.9	pKi	-	-	-	Eur J Pharmacol (1999) 367: 431-5 [PMID:10079020]; Br J Pharmacol (2005) 144: 317-22 [PMID:15655528]; J Pharmacol Exp Ther (1999) 290: 649-55 [PMID:10411574]; Naunyn Schmiedebergs Arch Pharmacol (2004) 369: 151-9 [PMID:14730417]; Mol Pharmacol (2003) 64: 1357-69 [PMID:14645666]
ChEMBL	DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)	B	6.75	pIC50	176	nM	IC50	DrugMatrix in vitro pharmacology data
β1-adrenoceptor/Beta-1 adrenergic receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3440] [GtoPdb: 28] [UniProtKB: P34971]
ChEMBL	Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranes	B	7.31	pKi	49	nM	Ki	Bioorg Med Chem (2019) 27: 2959-2971 [PMID:31151791]
β1-adrenoceptor/Beta-1 adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3252] [GtoPdb: 28] [UniProtKB: P18090]
ChEMBL	Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria	F	7.64	pKd	22.91	nM	Kd	J Med Chem (1987) 30: 1003-1011 [PMID:2884312]
ChEMBL	Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria	F	7.64	pKd	22.91	nM	Kd	J Med Chem (1987) 30: 1003-1011 [PMID:2884312]
ChEMBL	Antagonist activity at rat beta1 adrenoceptor	B	7.64	pKd	22.91	nM	Kd	J Med Chem (2016) 59: 8712-8756 [PMID:27299736]
ChEMBL	Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells	F	5.3	pKi	5011.87	nM	Ki	J Med Chem (2006) 49: 3467-3477 [PMID:16759089]
ChEMBL	Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells	F	5.6	pKi	2511.89	nM	Ki	J Med Chem (2006) 49: 3467-3477 [PMID:16759089]
ChEMBL	Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells	F	5.6	pKi	2511.89	nM	Ki	J Med Chem (2006) 49: 3467-3477 [PMID:16759089]
ChEMBL	Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells	F	6.2	pKi	630.96	nM	Ki	J Med Chem (2006) 49: 3467-3477 [PMID:16759089]
ChEMBL	Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells	F	6.4	pKi	398.11	nM	Ki	J Med Chem (2006) 49: 3467-3477 [PMID:16759089]
Beta-1 adrenergic receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5471] [UniProtKB: B0FL73]
ChEMBL	Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig trachea	F	6.14	pKd	724.44	nM	Kd	J Med Chem (1987) 30: 1003-1011 [PMID:2884312]
ChEMBL	Compound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig arteria	F	7.83	pKd	14.79	nM	Kd	J Med Chem (1982) 25: 931-936 [PMID:6126588]
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	7.83	pKd	14.79	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	7.83	pKd	14.79	nM	Kd	J Med Chem (1986) 29: 1065-1080 [PMID:2872332]
ChEMBL	Tested for beta-2-adrenergic blocking effect by measuring the ability to inhibit the relaxing effect of epinephrine on the isolated tracheal muscle of guinea pigs	F	6.49	pIC50	320	nM	IC50	Bioorg Med Chem Lett (1997) 7: 1273-1274
ChEMBL	Tested for beta-1-adrenergic blocking effect by measuring the ability to inhibit the positive inotropic effect of isoproterenol on the isolated right atrium of guinea pigs	F	6.72	pIC50	190	nM	IC50	Bioorg Med Chem Lett (1997) 7: 1273-1274
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	4.81	pKd	15500	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	6.89	pKd	130	nM	Kd	J Med Chem (2016) 59: 5780-5789 [PMID:27239696]
ChEMBL	DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)	B	5.75	pKi	1769	nM	Ki	DrugMatrix in vitro pharmacology data
GtoPdb	-	-	6.3	pKi	-	-	-	Eur J Pharmacol (1999) 367: 431-5 [PMID:10079020]
ChEMBL	Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes	B	6.66	pKi	220	nM	Ki	Bioorg Med Chem (2019) 27: 2959-2971 [PMID:31151791]
ChEMBL	DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)	B	5.59	pIC50	2573	nM	IC50	DrugMatrix in vitro pharmacology data
Beta-2 adrenergic receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5414] [UniProtKB: Q8K4Z4]
ChEMBL	Beta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chains	F	6.79	pKd	162.18	nM	Kd	J Med Chem (1982) 25: 931-936 [PMID:6126588]
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	6.79	pKd	162.18	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	6.79	pKd	162.18	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]