metoprolol [Ligand Id: 553] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL13 (CGP-2175, Lopressidone, Toprol-XL, Metoprolol)
  • β1-adrenoceptor/Beta-1 adrenergic receptor in Human [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
  • 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]
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  • 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]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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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
GtoPdb - - 7.6 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]
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 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 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 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 26:

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]