timolol [Ligand Id: 565] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL499 (Betim, Betimol, Blocadren, Glaucol, Glau-opt, Istalol, Nyogel, Timolol, Timolol anhydrous, Timolol hemihydrate, Timoptic, Timoptic-XE, Tiopex) |
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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 | Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation counting | B | 8.27 | pKi | 5.37 | nM | Ki | J Med Chem (2018) 61: 5380-5394 [PMID:29851481] |
| ChEMBL | DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) | B | 8.82 | pKi | 1.5 | nM | Ki | DrugMatrix in vitro pharmacology data |
| GtoPdb | - | - | 9 | pKi | - | - | - |
Naunyn Schmiedebergs Arch Pharmacol (2004) 369: 525-32 [PMID:15060759]; Br J Pharmacol (2005) 144: 317-22 [PMID:15655528]; Mol Pharmacol (2003) 64: 1357-69 [PMID:14645666] |
| ChEMBL | DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) | B | 8.58 | pIC50 | 2.6 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| β1-adrenoceptor/Beta-1 adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3252] [GtoPdb: 28] [UniProtKB: P18090] | ||||||||
| ChEMBL | Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells | F | 6.2 | pKi | 630.96 | nM | Ki | J Med Chem (2006) 49: 3467-3477 [PMID:16759089] |
| ChEMBL | Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells | F | 7.5 | pKi | 31.62 | nM | Ki | J Med Chem (2006) 49: 3467-3477 [PMID:16759089] |
| ChEMBL | Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells | F | 7.8 | pKi | 15.85 | nM | Ki | J Med Chem (2006) 49: 3467-3477 [PMID:16759089] |
| ChEMBL | Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells | F | 8.1 | pKi | 7.94 | nM | Ki | J Med Chem (2006) 49: 3467-3477 [PMID:16759089] |
| ChEMBL | Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells | F | 8.5 | pKi | 3.16 | nM | Ki | J Med Chem (2006) 49: 3467-3477 [PMID:16759089] |
| Beta-1 adrenergic receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5471] [UniProtKB: B0FL73] | ||||||||
| ChEMBL | Compound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig atria | F | 9.44 | pKd | 0.36 | nM | Kd | J Med Chem (1982) 25: 931-936 [PMID:6126588] |
| 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 | 9.44 | pKd | 0.36 | 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 | 9.44 | pKd | 0.36 | nM | Kd | J Med Chem (1986) 29: 1065-1080 [PMID:2872332] |
| β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550] | ||||||||
| ChEMBL | Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting | B | 9.68 | pKi | 0.21 | nM | Ki | J Med Chem (2018) 61: 5380-5394 [PMID:29851481] |
| ChEMBL | DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177) | B | 9.7 | pKi | 0.2 | nM | Ki | DrugMatrix in vitro pharmacology data |
| GtoPdb | - | - | 9.7 | pKi | - | - | - | Br J Pharmacol (2005) 144: 317-22 [PMID:15655528] |
| ChEMBL | DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177) | B | 9.53 | pIC50 | 0.29 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Beta-2 adrenergic receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5414] [UniProtKB: Q8K4Z4] | ||||||||
| ChEMBL | Beta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chains | F | 9.62 | pKd | 0.24 | nM | Kd | J Med Chem (1982) 25: 931-936 [PMID:6126588] |
| 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 | 9.62 | pKd | 0.24 | nM | Kd | J Med Chem (1983) 26: 950-957 [PMID:6134834] |
| ChEMBL | In vitro inhibitory activity against beta-2 adrenoceptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea | B | 9.78 | pKd | 0.17 | nM | Kd | J Med Chem (1986) 29: 1065-1080 [PMID:2872332] |
| β3-adrenoceptor/Beta-3 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945] | ||||||||
| ChEMBL | DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol) | B | 6.47 | pKi | 339 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol) | B | 6.34 | pIC50 | 452 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) | B | 5.81 | pKi | 1550 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | Binding affinity of a compound to rat brain 5-hydroxytryptamine 1A (serotonin) receptor assayed by radiolabeled [3H]-8-OH-DPAT ligand displacement | B | 6.21 | pKi | 616.6 | nM | Ki | J Med Chem (1996) 39: 126-134 [PMID:8568799] |
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) | B | 5.57 | pIC50 | 2712 | nM | IC50 | DrugMatrix in vitro pharmacology data |
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]
