(-)-adrenaline [Ligand Id: 479] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL679 (Adrenaclick, Adrenalin, Adrenaline, Adrenalinum, Adren co, Ana-guard, Ana-Kit, Anapen, Anaphylactic shock drug kit, Asma-vydrin, Asthmahaler, Auvi-q, Bronkaid mist, Brovon, Emerade, Epi e z pen jr, (-)-epinephrine, Epinephrine, Epinephrine (copackaged), Epinephrine hcl, Epinephrine hydrochloride, Epinephrinum, Epipen, Epipen e z pen, Epipen jr, Epipen jr., Eppy, Glauposine, Gppe inh soln, Jext, L-epinephrine hydrochloride, Levo-methylaminoethanolcatechol, Medihaler-epi, Nephridine, NSC-62786, Primatene, Primatene mist, Racepinefrine hydrochloride, (r)-, Racepinefrine, (r)-, (-)-(r)-epinephrine, Riddobron, Riddofan, Rybarvin, Simplene, Soln made to rybarvin for, Susphrine, Sus-Phrine, Sus-phrine sulfite free, Sus-Phrine Sulfite-Free, Sus-phrine sulphite-free, Symjepi, Tonogen, Twinject, Twinject 0.15, Twinject 0.3) |
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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]; J Pharmacol Exp Ther (1995) 272: 134-42 [PMID:7815325]; Br J Pharmacol (1995) 116: 1611-8 [PMID:8564227]; Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529] |
| 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] |
| GtoPdb | - | - | 9.1 | pEC50 | - | - | - | Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529] |
| 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/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368] | ||||||||
| GtoPdb | - | - | 6.5 | pKi | - | - | - |
Mol Pharmacol (1995) 48: 250-8 [PMID:7651358]; Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529] |
| ChEMBL | Agonist activity at human alpha1 beta adrenergic receptor expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium influx by measuring fluorescence intensity by FLIPR assay | F | 7.12 | pEC50 | 75 | nM | EC50 | J Nat Prod (2019) 82: 2986-2993 [PMID:31625751] |
| GtoPdb | - | - | 9.4 | pEC50 | - | - | - | Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529] |
| 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]; Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529] |
| ChEMBL | DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) | B | 6.35 | pIC50 | 449 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| GtoPdb | - | - | 7.7 | pEC50 | - | - | - | Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529] |
| 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]; Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| ChEMBL | DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) | B | 6.13 | pIC50 | 737 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| GtoPdb | inhibition of forskolin stimulated cAMP generation | - | 6.5 | pIC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| GtoPdb | increased cAMP generation | - | 5.5 | pEC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| GtoPdb | GTPγs binding | - | 6.8 | pEC50 | - | - | - | Biochem Pharmacol (1998) 55: 1035-43 [PMID:9605427] |
| GtoPdb | increased ERK1/2 phosphorylation | - | 8 | pEC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| 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]; Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| 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 |
| GtoPdb | inhibition of forskolin stimulated cAMP generation | - | 7.6 | pIC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| GtoPdb | cAMP generation | - | 6.3 | pEC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| GtoPdb | ERK1/2 phosphorylation | - | 7.5 | pEC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| 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]; Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| 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 |
| GtoPdb | inhibition of cAMP production | - | 6.7 | pIC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| GtoPdb | ERK1/2 phosphorylation | - | 7.6 | pEC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| 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/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588] | ||||||||
| GtoPdb | - | - | 6 | pKi | - | - | - |
Proc Natl Acad Sci USA (1988) 85: 9494-8 [PMID:2849109]; Naunyn Schmiedebergs Arch Pharmacol (2004) 369: 151-9 [PMID:14730417]; Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599] |
| ChEMBL | Agonist activity at human beta1 adrenergic receptor expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium influx by measuring fluorescence intensity by FLIPR assay | F | 6.54 | pEC50 | 290 | nM | EC50 | J Nat Prod (2019) 82: 2986-2993 [PMID:31625751] |
| GtoPdb | - | - | 7.6 | pEC50 | - | - | - | Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599] |
| 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 USA (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]; Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599] |
| 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 |
| GtoPdb | - | - | 7.9 | pEC50 | - | - | - | Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599] |
| 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 | - | - | 4.7 | pKi | - | - | - |
Naunyn Schmiedebergs Arch Pharmacol (2004) 369: 151-9 [PMID:14730417]; Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599] |
| GtoPdb | - | - | 6.5 | pEC50 | - | - | - | Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599] |
| 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 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]
