(-)-adrenaline [Ligand Id: 479] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL679 (Anapen, Ana-Guard, Ana-Kit, Sus-phrine sulfite free, Adrenalin, Epipen, Anaphylactic Shock Drug Kit, Riddobron, Symjepi, Epinephrine HCl, Epi E Z Pen Jr, Sus-Phrine Sulfite-Free, Bronkaid Mist, Epinephrine, Adrenaline, Gppe Inh Soln, Simplene, Riddofan, Adren Co, Epipen E Z Pen, Primatene, Epipen Jr, Medihaler-epi, Rybarvin, Epipen Jr., Twinject 0.15, Eppy, Asthmahaler, Levo-Methylaminoethanolcatechol, Asma-Vydrin, Soln Made To Rybarvin For, Auvi-Q, Emerade, Twinject 0.3, Primatene Mist, Twinject, Brovon, NSC-62786, Sus-Phrine, Jext, Adrenaclick) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348] | ||||||||
| ChEMBL | Binding affinity against alpha-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of [3H]- WB-4101 | B | 5.7 | pKi | 2000 | nM | Ki | J. Med. Chem. (1988) 31: 1972-1977 [PMID:2845082] |
| GtoPdb | - | - | 6.5 | pKi | - | - | - |
Mol. Pharmacol. (1995) 48: 250-8 [PMID:7651358]; Br. J. Pharmacol. (1995) 116: 1611-8 [PMID:8564227] |
| ChEMBL | Agonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortex | F | 6.4 | pEC50 | 400 | nM | EC50 | J. Med. Chem. (1988) 31: 1972-1977 [PMID:2845082] |
| α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140] | ||||||||
| ChEMBL | DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) | B | 6.6 | pKi | 254 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) | B | 6.2 | pIC50 | 628 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| α1B-adrenoceptor in Human [GtoPdb: 23] [UniProtKB: P35368] | ||||||||
| GtoPdb | - | - | 6.5 | pKi | - | - | - | Mol. Pharmacol. (1995) 48: 250-8 [PMID:7651358] |
| α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823] | ||||||||
| ChEMBL | DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) | B | 6.01 | pKi | 977 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) | B | 5.75 | pIC50 | 1766 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100] | ||||||||
| ChEMBL | DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) | B | 6.66 | pKi | 221 | nM | Ki | DrugMatrix in vitro pharmacology data |
| GtoPdb | - | - | 7.2 | pKi | - | - | - |
Mol. Pharmacol. (1995) 48: 250-8 [PMID:7651358]; Br. J. Pharmacol. (1995) 116: 1611-8 [PMID:8564227] |
| ChEMBL | DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) | B | 6.35 | pIC50 | 449 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| α1D-adrenoceptor in Rat [GtoPdb: 24] [UniProtKB: P23944] | ||||||||
| GtoPdb | - | - | 6.3 | pKi | - | - | - | Mol. Pharmacol. (1994) 46: 929-36 [PMID:7969082] |
| α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
| ChEMBL | DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) | B | 6.56 | pKi | 276 | nM | Ki | DrugMatrix in vitro pharmacology data |
| GtoPdb | - | - | 7.4 | pKi | - | - | - |
Biochim. Biophys. Acta (1998) 1448: 135-46 [PMID:9824686]; Biochem. Pharmacol. (1998) 55: 1035-43 [PMID:9605427] |
| ChEMBL | DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) | B | 6.13 | pIC50 | 737 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089] | ||||||||
| GtoPdb | - | - | 5.2 | pKi | - | - | - | Biochem. Pharmacol. (1998) 55: 1035-43 [PMID:9605427] |
| ChEMBL | DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) | B | 6.4 | pKi | 397 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) | B | 6.06 | pIC50 | 869 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] | ||||||||
| GtoPdb | - | - | 5.8 | pKi | - | - | - | Biochem. Pharmacol. (1998) 55: 1035-43 [PMID:9605427] |
| ChEMBL | DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) | B | 6.45 | pKi | 356 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) | B | 5.61 | pIC50 | 2449 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Arachidonate 15-lipoxygenase in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4358] [UniProtKB: P12530] | ||||||||
| ChEMBL | DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid) | B | 5.48 | pIC50 | 3279 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| β1-adrenoceptor in Human [GtoPdb: 28] [UniProtKB: P08588] | ||||||||
| GtoPdb | - | - | 6 | pKi | - | - | - |
Proc. Natl. Acad. Sci. U.S.A. (1988) 85: 9494-8 [PMID:2849109]; Naunyn Schmiedebergs Arch. Pharmacol. (2004) 369: 151-9 [PMID:14730417] |
| β1-adrenoceptor/Beta-1 adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3252] [GtoPdb: 28] [UniProtKB: P18090] | ||||||||
| ChEMBL | Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranes | B | 5.68 | pKi | 2100 | nM | Ki | J. Med. Chem. (2000) 43: 1611-1619 [PMID:10780918] |
| ChEMBL | Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes | B | 5.92 | pKi | 1200 | nM | Ki | J. Med. Chem. (1993) 36: 3947-3955 [PMID:8254623] |
| ChEMBL | Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranes | B | 5.96 | pKi | 1100 | nM | Ki | J. Med. Chem. (2000) 43: 1611-1619 [PMID:10780918] |
| Beta-1 adrenergic receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5471] [UniProtKB: B0FL73] | ||||||||
| ChEMBL | Binding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenolol | B | 5.52 | pKi | 3000 | nM | Ki | J. Med. Chem. (1988) 31: 1972-1977 [PMID:2845082] |
| ChEMBL | Effective dose required to stimulate contractions in isolated guinea pig atrium. | F | 6.36 | pEC50 | 436 | nM | EC50 | J. Med. Chem. (1995) 38: 3681-3716 [PMID:7562902] |
| ChEMBL | Agonistic potency at beta-1 adrenergic receptor for the percent maximal increase in contraction rate of isolated guinea pig atria | F | 6.59 | pEC50 | 260 | nM | EC50 | J. Med. Chem. (1988) 31: 1972-1977 [PMID:2845082] |
| ChEMBL | Effective dose required to stimulate contractions in isolated guinea pig atrium. | F | 7.82 | pEC50 | 15 | nM | EC50 | J. Med. Chem. (1995) 38: 3681-3716 [PMID:7562902] |
| β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550] | ||||||||
| ChEMBL | Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM | B | 6.2 | pKd | 630.96 | nM | Kd | Bioorg. Med. Chem. Lett. (2013) 23: 5376-5381 [PMID:23954364] |
| ChEMBL | Binding affinity to human adrenergic beta2 receptor | B | 6.2 | pKd | 630 | nM | Kd | Eur. J. Med. Chem. (2009) 44: 2840-2846 [PMID:19168263] |
| GtoPdb | - | - | 6.2 | pKi | - | - | - |
Proc. Natl. Acad. Sci. U.S.A. (1988) 85: 9494-8 [PMID:2849109]; J. Biol. Chem. (1997) 272: 23871-9 [PMID:9295336]; Naunyn Schmiedebergs Arch. Pharmacol. (2004) 369: 151-9 [PMID:14730417] |
| ChEMBL | Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells | B | 6.44 | pKi | 360 | nM | Ki | Bioorg. Med. Chem. (2016) 24: 2641-2653 [PMID:27132867] |
| ChEMBL | DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177) | B | 6.71 | pKi | 196 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177) | B | 6.55 | pIC50 | 284 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Beta-2 adrenergic receptor in Dog (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2289] [UniProtKB: P54833] | ||||||||
| ChEMBL | Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes | B | 5.96 | pKi | 1100 | nM | Ki | J. Med. Chem. (2000) 43: 1611-1619 [PMID:10780918] |
| ChEMBL | Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes | B | 6.18 | pKi | 660 | nM | Ki | J. Med. Chem. (2000) 43: 1611-1619 [PMID:10780918] |
| β2-adrenoceptor/Beta-2 adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3754] [GtoPdb: 29] [UniProtKB: P10608] | ||||||||
| ChEMBL | Binding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranes | B | 6.14 | pKi | 720 | nM | Ki | J. Med. Chem. (1993) 36: 3947-3955 [PMID:8254623] |
| Beta-2 adrenergic receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5414] [UniProtKB: Q8K4Z4] | ||||||||
| ChEMBL | Effective dose for relaxation of guinea pig trachea. | F | 6.36 | pEC50 | 436 | nM | EC50 | J. Med. Chem. (1995) 38: 3681-3716 [PMID:7562902] |
| ChEMBL | Effective dose for relaxation of guinea pig trachea. | F | 7.82 | pEC50 | 15 | nM | EC50 | J. Med. Chem. (1995) 38: 3681-3716 [PMID:7562902] |
| β3-adrenoceptor/Beta-3 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945] | ||||||||
| GtoPdb | - | - | 3.9 | pKi | - | - | - | Naunyn Schmiedebergs Arch. Pharmacol. (2004) 369: 151-9 [PMID:14730417] |
| ChEMBL | Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assay | F | 7.31 | pEC50 | 49 | nM | EC50 | Bioorg. Med. Chem. (2008) 16: 2473-2488 [PMID:18083578] |
| ChEMBL | Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method | F | 7.51 | pEC50 | 31 | nM | EC50 | Bioorg. Med. Chem. (2008) 16: 2473-2488 [PMID:18083578] |
| D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728] | ||||||||
| ChEMBL | Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells | B | 4.26 | pKd | 55000 | nM | Kd | J. Med. Chem. (1996) 39: 850-859 [PMID:8632409] |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Displacement of [3H]spiperone from human D2S receptor expressed in CHO cells | B | 6.04 | pKi | 910 | nM | Ki | Bioorg. Med. Chem. (2016) 24: 2641-2653 [PMID:27132867] |
ChEMBL data shown on this page come from version 26:
Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]
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