practolol [Ligand Id: 555] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL6995 ([3-(4-Acetylamino-Phenoxy)-2-Hydroxy-Propyl]-Isopropyl-Ammonium, AY-21,011, AY-21011, Dalzic, Eraldin, I.C.I. 50,172, I.C.I.-50,172, ICI-50172, Practolol) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| β1-adrenoceptor in Human [GtoPdb: 28] [UniProtKB: P08588] | ||||||||
| GtoPdb | - | - | 6.8 | pKi | - | - | - |
Eur J Pharmacol (1999) 367: 431-5 [PMID:10079020]; Br J Pharmacol (2005) 144: 317-22 [PMID:15655528] |
| β1-adrenoceptor/Beta-1 adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3252] [GtoPdb: 28] [UniProtKB: P18090] | ||||||||
| ChEMBL | Apparent dissociation constant towards beta-1 adrenergic receptor in rat heart membranes using (2-6)x10E-9M of [3AH]-DHA in the presence or absence of 10e-5 M (+/-) propranolol. | B | 6.21 | pKd | 0 | M | KD' | J Med Chem (1987) 30: 722-726 [PMID:3031293] |
| ChEMBL | Antagonist activity at beta1 adrenergic receptor in isolated rat atria | B | 6.47 | pKd | 338.84 | nM | Kd | J Med Chem (1978) 21: 982-984 [PMID:31488] |
| 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 | 5.08 | pKd | 8317.64 | nM | Kd | J Med Chem (1987) 30: 1003-1011 [PMID:2884312] |
| ChEMBL | Antagonist activity against beta-1 adrenergic receptor in isolated guinea pig atria | F | 5.78 | pKd | 1659.59 | nM | Kd | J Med Chem (1987) 30: 616-622 [PMID:2882026] |
| ChEMBL | Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria | F | 5.78 | pKd | 1659.59 | nM | Kd | J Med Chem (1985) 28: 153-160 [PMID:2857200] |
| ChEMBL | Activity at beta-1 adrenergic receptor | B | 6 | pKd | 1000 | nM | Kd | J Med Chem (1992) 35: 4676-4682 [PMID:1361581] |
| ChEMBL | Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparation | B | 6.6 | pKd | 251.19 | nM | Kd | J Med Chem (1982) 25: 1408-1412 [PMID:6130154] |
| ChEMBL | Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 mins | B | 6.67 | pKd | 213.8 | nM | Kd | J Med Chem (1978) 21: 1081-1084 [PMID:31474] |
| ChEMBL | Antagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atria | F | 6.76 | pKd | 173.78 | nM | Kd | J Med Chem (1981) 24: 994-998 [PMID:6120237] |
| 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 | 6.98 | pKd | 104.71 | nM | Kd | J Med Chem (1983) 26: 950-957 [PMID:6134834] |
| Beta-2 adrenergic receptor in Dog (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2289] [UniProtKB: P54833] | ||||||||
| ChEMBL | Cardioselectivity for the beta-2 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria | F | 6.73 | pKd | 186.21 | nM | Kd | J Med Chem (1987) 30: 1003-1011 [PMID:2884312] |
| 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 | 4.69 | pKd | 20417 | nM | Kd | J Med Chem (1985) 28: 1328-1334 [PMID:2993621] |
| ChEMBL | Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA) | B | 4.99 | pKd | 4.99 | - | -Log KD | J Med Chem (1985) 28: 1328-1334 [PMID:2993621] |
| β2-adrenoceptor/Beta-2 adrenergic receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3707] [GtoPdb: 29] [UniProtKB: P18762] | ||||||||
| ChEMBL | Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2). | B | 4.87 | pKi | 13500 | nM | Ki | J Med Chem (1990) 33: 216-223 [PMID:1967313] |
| β2-adrenoceptor/Beta-2 adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3754] [GtoPdb: 29] [UniProtKB: P10608] | ||||||||
| ChEMBL | Apparent dissociation constant towards beta-2 adrenergic receptor in rat lung membranes using (2-6)x10E-9M of [3AH]-DHA in the presence or absence of 10e-5 M (+/-) propranolol. | B | 5.44 | pKd | 0 | M | KD' | J Med Chem (1987) 30: 722-726 [PMID:3031293] |
| Beta-2 adrenergic receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5414] [UniProtKB: Q8K4Z4] | ||||||||
| ChEMBL | Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips | F | 4.5 | pKd | 31622.78 | nM | Kd | J Med Chem (1985) 28: 153-160 [PMID:2857200] |
| ChEMBL | Antagonist activity against beta-2 adrenergic receptor in isolated guinea pig trachea | F | 4.5 | pKd | 31622.78 | nM | Kd | J Med Chem (1987) 30: 616-622 [PMID:2882026] |
| ChEMBL | Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins | B | 5.2 | pKd | 6309.57 | nM | Kd | J Med Chem (1978) 21: 1081-1084 [PMID:31474] |
| 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 | 5.35 | pKd | 4466.84 | nM | Kd | J Med Chem (1983) 26: 950-957 [PMID:6134834] |
| ChEMBL | Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparation | B | 5.8 | pKd | 1584.89 | nM | Kd | J Med Chem (1982) 25: 1408-1412 [PMID:6130154] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
