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

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ChEMBL ligand: CHEMBL423 (ALO-140102 FREE BASE, Betaxolol, Betoptic, Betoptic susp, Kerledex, Kerlone, SL-7521210 FREE BASE)
  • 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 - - 9.12 pKi - - - Eur J Pharmacol (1999) 367: 431-5 [PMID:10079020];
Br J Pharmacol (2005) 144: 317-22 [PMID:15655528];
J Ocul Pharmacol Ther (2001) 17: 305-17 [PMID:11572462]
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 - - 8.2 pKi - - - Eur J Pharmacol (1999) 367: 431-5 [PMID:10079020];
Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599];
J Ocul Pharmacol Ther (2001) 17: 305-17 [PMID:11572462]

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]