betaxolol [Ligand Id: 549] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL423 (Kerlone, SL-7521210 FREE BASE, Betaxolol, Betoptic, ALO-140102 FREE BASE, Betoptic susp, Kerledex)
  • 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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  • Beta-2 adrenergic receptor in Bovine [ChEMBL: CHEMBL3373] [UniProtKB: Q28044]
  • Beta-2 adrenergic receptor in Guinea pig [ChEMBL: CHEMBL5414] [UniProtKB: Q8K4Z4]
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  • β2-adrenoceptor in Human [GtoPdb: 29] [UniProtKB: P07550]
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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 8.8 pKd 1.58 nM Kd J. Med. Chem. (2015) 58: 5691-5698 [PMID:25799158]
GtoPdb - - 8.8 pKi - - - Eur J Pharmacol (1999) 367: 431-5 [PMID:10079020]
ChEMBL Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heart B 7.43 pIC50 37.1 nM IC50 J. Med. Chem. (1982) 25: 931-936 [PMID:6126588]
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 6.9 pKd 125.89 nM Kd J. Med. Chem. (1987) 30: 1003-1011 [PMID:2884312]
ChEMBL Antagonist activity at rat beta1 adrenoceptor B 8.53 pKd 2.95 nM Kd J Med Chem (2016) 59: 8712-8756 [PMID:27299736]
Beta-1 adrenergic receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5471] [UniProtKB: B0FL73]
ChEMBL Compound was tested for the biological activity at the Beta-1 adrenergic receptor B 7.4 pKd 39.81 nM Kd J. Med. Chem. (1992) 35: 4676-4682 [PMID:1361581]
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 8.76 pKd 1.74 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 8.76 pKd 1.74 nM Kd J. Med. Chem. (1986) 29: 1065-1080 [PMID:2872332]
Beta-2 adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3373] [UniProtKB: Q28044]
ChEMBL Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA) B 7.03 pKd 7.03 - -Log KD J. Med. Chem. (1985) 28: 1328-1334 [PMID:2993621]
ChEMBL Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes. B 6.18 pIC50 657 nM IC50 J. Med. Chem. (1982) 25: 931-936 [PMID:6126588]
Beta-2 adrenergic receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5414] [UniProtKB: Q8K4Z4]
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 6.98 pKd 104.71 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 6.98 pKd 104.71 nM Kd J. Med. Chem. (1986) 29: 1065-1080 [PMID:2872332]
β2-adrenoceptor in Human [GtoPdb: 29] [UniProtKB: P07550]
GtoPdb - - 7.2 pKi - - - Eur J Pharmacol (1999) 367: 431-5 [PMID:10079020]

ChEMBL data shown on this page come from version 28:

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]