practolol [Ligand Id: 555] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL6995 (AY-21,011, AY-21011, Dalzic, Eraldin, I.C.I. 50,172, I.C.I.-50,172, ICI-50172, Practolol) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| 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 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]
