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ChEMBL ligand: CHEMBL423 (ALO-140102 FREE BASE, Betaxolol, Betoptic, Betoptic susp, Kerledex, Kerlone, SL-7521210 FREE BASE) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 31:
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]