(-)-adrenaline [Ligand Id: 479] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL679 (Anapen, Epi e z pen jr, Primatene mist, Ana-Kit, Auvi-q, Sus-phrine sulfite free, Epipen, Riddobron, Symjepi, Sus-Phrine Sulfite-Free, Epinephrine, Adrenaline, Simplene, Riddofan, Primatene, Ana-guard, Epinephrine (copackaged), Epipen e z pen, Medihaler-epi, Epipen jr, Levo-methylaminoethanolcatechol, Rybarvin, Twinject 0.15, Bronkaid mist, Eppy, Gppe inh soln, Asma-vydrin, Asthmahaler, Anaphylactic shock drug kit, Epinephrine hydrochloride, Emerade, Epipen jr., Twinject 0.3, Twinject, Soln made to rybarvin for, Brovon, Adren co, NSC-62786, Sus-Phrine, Adrenaclick, Jext, Adrenalin)
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
  • 6.6
1 CHEMBL679_lig_chart_1 Alpha-1a adrenergic receptor HumanRat
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  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
  • 6.01
2 CHEMBL679_lig_chart_2 Alpha-1b adrenergic receptor HumanRat
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  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
  • α1D-adrenoceptor in Rat [GtoPdb: 24] [UniProtKB: P23944]
  • 6.3
3 CHEMBL679_lig_chart_3 Alpha-1d adrenergic receptor HumanRat
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  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
  • 6.98
4 CHEMBL679_lig_chart_4 Alpha-2a adrenergic receptor Human
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  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
  • 5.8
5 CHEMBL679_lig_chart_5 Alpha-2b adrenergic receptor Human
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  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
  • 6.12
6 CHEMBL679_lig_chart_6 Alpha-2c adrenergic receptor Human
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  • Arachidonate 15-lipoxygenase in Rabbit [ChEMBL: CHEMBL4358] [UniProtKB: P12530]
  • This target only has 0 pki data point
  • 0
7 CHEMBL679_lig_chart_7 Arachidonate 15-lipoxygenase Rabbit
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  • β1-adrenoceptor/Beta-1 adrenergic receptor in Human [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
  • β1-adrenoceptor/Beta-1 adrenergic receptor in Rat [ChEMBL: CHEMBL3252] [GtoPdb: 28] [UniProtKB: P18090]
  • Beta-1 adrenergic receptor in Guinea pig [ChEMBL: CHEMBL5471] [UniProtKB: B0FL73]
  • 5.52
8 CHEMBL679_lig_chart_8 Beta-1 adrenergic receptor HumanRatGuinea pig
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  • β2-adrenoceptor/Beta-2 adrenergic receptor in Human [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
  • Beta-2 adrenergic receptor in Dog [ChEMBL: CHEMBL2289] [UniProtKB: P54833]
  • β2-adrenoceptor/Beta-2 adrenergic receptor in Rat [ChEMBL: CHEMBL3754] [GtoPdb: 29] [UniProtKB: P10608]
  • Beta-2 adrenergic receptor in Guinea pig [ChEMBL: CHEMBL5414] [UniProtKB: Q8K4Z4]
  • 0
9 CHEMBL679_lig_chart_9 Beta-2 adrenergic receptor HumanDogRatGuinea pig
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  • β3-adrenoceptor/Beta-3 adrenergic receptor in Human [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945]
  • This target only has 1 pki data point
  • 3.9
10 CHEMBL679_lig_chart_10 Beta-3 adrenergic receptor Human
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  • D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
  • This target only has 0 pki data point
  • 0
11 CHEMBL679_lig_chart_11 Dopamine D1 receptor Human
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • This target only has 1 pki data point
  • 6.04
12 CHEMBL679_lig_chart_12 Dopamine D2 receptor Human
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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/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]
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 B 7.12 pEC50 75 nM EC50 J Nat Prod (2019) 82: 2986-2993 [PMID:31625751]
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 B 7.12 pEC50 75 nM EC50 J Nat Prod (2019) 82: 2986-2993 [PMID:31625751]
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/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]
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 B 6.54 pEC50 290 nM EC50 J Nat Prod (2019) 82: 2986-2993 [PMID:31625751]
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 B 6.54 pEC50 290 nM EC50 J Nat Prod (2019) 82: 2986-2993 [PMID:31625751]
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]
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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]