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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 | - | - | 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]