(-)-noradrenaline [Ligand Id: 505] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1437 (Levarterenol, Levophed, Nor adrenalin, (-)-noradrenaline, Norepinephrine, NSC-757246, R-norepinephrine) |
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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 | 5.82 | pKi | 1500 | nM | Ki | J Med Chem (1988) 31: 1972-1977 [PMID:2845082] |
| GtoPdb | - | - | 6.4 | pKi | - | - | - |
Br J Pharmacol (2017) 174: 2318-2333 [PMID:28444738]; Mol Pharmacol (2011) 79: 298-307 [PMID:20978120]; Br J Pharmacol (1995) 116: 1611-8 [PMID:8564227]; Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529]; J Pharmacol Exp Ther (1995) 272: 134-42 [PMID:7815325]; Mol Pharmacol (1995) 48: 250-8 [PMID:7651358]; Br J Pharmacol (1999) 127: 962-8 [PMID:10433504] |
| ChEMBL | In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate | F | 5.66 | pEC50 | 2187.76 | nM | EC50 | J Med Chem (1996) 39: 4116-4119 [PMID:8831777] |
| ChEMBL | Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay | F | 8.04 | pEC50 | 9.1 | nM | EC50 | J Med Chem (2015) 58: 6048-6057 [PMID:26125514] |
| GtoPdb | - | - | 8.6 | pEC50 | - | - | - |
Mol Pharmacol (2011) 79: 298-307 [PMID:20978120]; Br J Pharmacol (2017) 174: 2318-2333 [PMID:28444738]; Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529] |
| Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130] | ||||||||
| ChEMBL | Binding affinity towards bovine clonal Alpha-1A adrenergic receptor | B | 6.35 | pKi | 446.68 | nM | Ki | J Med Chem (1996) 39: 4116-4119 [PMID:8831777] |
| α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140] | ||||||||
| ChEMBL | Binding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glands | B | 6.55 | pKi | 281.84 | nM | Ki | J Med Chem (1996) 39: 4116-4119 [PMID:8831777] |
| ChEMBL | In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens | F | 5.93 | pEC50 | 1174.9 | nM | EC50 | J Med Chem (1996) 39: 4116-4119 [PMID:8831777] |
| α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368] | ||||||||
| ChEMBL | Displacement of [3H]prazosin from human adrenergic Alpha-1B receptor expressed in CHO cell membrane | B | 4.69 | pKi | 20400 | nM | Ki | Bioorg Med Chem (2009) 17: 7987-7992 [PMID:19857969] |
| GtoPdb | - | - | 6.2 | pKi | - | - | - |
Mol Pharmacol (1995) 48: 250-8 [PMID:7651358]; Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529] |
| GtoPdb | - | - | 9.2 | pEC50 | - | - | - | Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529] |
| Alpha-1b adrenergic receptor in Hamster (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3122] [UniProtKB: P18841] | ||||||||
| ChEMBL | Binding affinity towards hamster clonal Alpha-1B adrenergic receptor | B | 6.58 | pKi | 263.03 | nM | Ki | J Med Chem (1996) 39: 4116-4119 [PMID:8831777] |
| α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823] | ||||||||
| ChEMBL | In vitro agonist potency towards Alpha-1B adrenergic receptor in rat spleen | F | 4.99 | pEC50 | 10232.93 | nM | EC50 | J Med Chem (1996) 39: 4116-4119 [PMID:8831777] |
| α1D-adrenoceptor in Human [GtoPdb: 24] [UniProtKB: P25100] | ||||||||
| GtoPdb | - | - | 7.4 | 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] |
| GtoPdb | - | - | 7.8 | pEC50 | - | - | - | Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529] |
| α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944] | ||||||||
| GtoPdb | - | - | 6.3 | pKi | - | - | - | Mol Pharmacol (1994) 46: 929-36 [PMID:7969082] |
| ChEMBL | Binding affinity towards rat clonal Alpha-1D adrenergic receptor | B | 7.65 | pKi | 22.39 | nM | Ki | J Med Chem (1996) 39: 4116-4119 [PMID:8831777] |
| ChEMBL | In vitro agonist potency towards Alpha-1D adrenergic receptor in rat aorta | F | 7.92 | pEC50 | 12.02 | nM | EC50 | J Med Chem (1996) 39: 4116-4119 [PMID:8831777] |
| α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
| ChEMBL | Binding affinity for human Alpha-2A adrenergic receptor | B | 7.18 | pKi | 66 | nM | Ki | J Med Chem (1996) 39: 1193-1195 [PMID:8632424] |
| 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] |
| GtoPdb | inhibition of forskolin stimulated cAMP generation | - | 6.6 | pIC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| GtoPdb | increased cAMP generation | - | 5.3 | pEC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| ChEMBL | Agonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry | F | 6.43 | pEC50 | 371.54 | nM | EC50 | J Med Chem (2009) 52: 7319-7322 [PMID:19886609] |
| ChEMBL | Agonistic potency at human adrenergic alpha-2A receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulation | F | 6.43 | pEC50 | 371.54 | nM | EC50 | J Med Chem (2007) 50: 3964-3968 [PMID:17630725] |
| ChEMBL | Agonist activity at human recombinant adrenergic alpha2A receptor expressed in CHO cells assessed as stimulation of extracellular acidification | F | 6.43 | pEC50 | 371.54 | nM | EC50 | J Med Chem (2008) 51: 4289-4299 [PMID:18578476] |
| ChEMBL | Agonist activity at human adrenergic alpha-2A receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry | F | 6.43 | pEC50 | 371.54 | nM | EC50 | J Med Chem (2004) 47: 6160-6173 [PMID:15566287] |
| GtoPdb | GTPγs binding | - | 6.7 | pEC50 | - | - | - | Biochem Pharmacol (1998) 55: 1035-43 [PMID:9605427] |
| ChEMBL | Agonist activity at human alpha2A adrenoceptor expressed in CHO-K1 cells after 30 mins by [35S]GTPgammaS binding assay | F | 6.89 | pEC50 | 128.82 | nM | EC50 | Eur J Med Chem (2014) 87: 386-397 [PMID:25282262] |
| ChEMBL | Agonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation counting | F | 6.93 | pEC50 | 118 | nM | EC50 | Bioorg Med Chem (2012) 20: 108-116 [PMID:22172308] |
| ChEMBL | Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting | F | 6.96 | pEC50 | 110 | nM | EC50 | Bioorg Med Chem (2011) 19: 321-329 [PMID:21129985] |
| GtoPdb | increased ERK1/2 phosphorylation | - | 7.7 | pEC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| α2A-adrenoceptor/Alpha-2a adrenergic receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4075] [GtoPdb: 25] [UniProtKB: Q01338] | ||||||||
| ChEMBL | Binding affinity to mouse alpha-2A receptor expressed in COS7 cells | B | 5.24 | pKi | 5800 | nM | Ki | US-20050059664-A1. Novel methods for identifying improved, non-sedating alpha-2 agonists (2005) |
| α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089] | ||||||||
| GtoPdb | - | - | 6 | 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] |
| GtoPdb | inhibition of forskolin stimulated cAMP generation | - | 7.8 | pIC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| GtoPdb | cAMP generation | - | 6.9 | pEC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| ChEMBL | Agonist activity at human adrenergic alpha-2B receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry | F | 7.21 | pEC50 | 61.66 | nM | EC50 | J Med Chem (2004) 47: 6160-6173 [PMID:15566287] |
| ChEMBL | Agonistic potency at human adrenergic alpha-2B receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulation | F | 7.21 | pEC50 | 61.66 | nM | EC50 | J Med Chem (2007) 50: 3964-3968 [PMID:17630725] |
| ChEMBL | Agonist activity at human recombinant adrenergic alpha2B receptor expressed in CHO cells | F | 7.21 | pEC50 | 61.66 | nM | EC50 | J Med Chem (2008) 51: 4289-4299 [PMID:18578476] |
| GtoPdb | ERK1/2 phosphorylation | - | 7.8 | pEC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| α2B-adrenoceptor/Alpha-2b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL266] [GtoPdb: 26] [UniProtKB: P19328] | ||||||||
| ChEMBL | Binding affinity for rat Alpha-2B adrenergic receptor | B | 7.11 | pKi | 78 | nM | Ki | J Med Chem (1996) 39: 1193-1195 [PMID:8632424] |
| α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] | ||||||||
| GtoPdb | - | - | 6.8 | 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]; Brain Res Bull (2014) 107: 89-101 [PMID:25080296] |
| ChEMBL | Binding affinity for human Alpha-2C adrenergic receptor | B | 7.2 | pKi | 63 | nM | Ki | J Med Chem (1996) 39: 1193-1195 [PMID:8632424] |
| GtoPdb | inhibition of cAMP production | - | 8.6 | pIC50 | - | - | - |
Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495]; Brain Res Bull (2014) 107: 89-101 [PMID:25080296] |
| ChEMBL | Agonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry | F | 6.1 | pEC50 | 794.33 | nM | EC50 | J Med Chem (2004) 47: 6160-6173 [PMID:15566287] |
| ChEMBL | Agonistic potency at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulation | F | 6.1 | pEC50 | 794.33 | nM | EC50 | J Med Chem (2007) 50: 3964-3968 [PMID:17630725] |
| ChEMBL | Agonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidification | F | 6.1 | pEC50 | 794.33 | nM | EC50 | J Med Chem (2008) 51: 4289-4299 [PMID:18578476] |
| ChEMBL | Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry | F | 6.1 | pEC50 | 794.33 | nM | EC50 | J Med Chem (2009) 52: 7319-7322 [PMID:19886609] |
| GtoPdb | 6.02 = value for β-arrestin recruitment and internalization | - | 6.6 | pEC50 | - | - | - | Brain Res Bull (2014) 107: 89-101 [PMID:25080296] |
| GtoPdb | ERK1/2 phosphorylation | - | 7.7 | pEC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| α2C-adrenoceptor/Alpha-2c adrenergic receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4826] [GtoPdb: 27] [UniProtKB: Q01337] | ||||||||
| ChEMBL | Binding affinity to mouse alpha-2C receptor expressed in COS7 cells | B | 6.19 | pKi | 650 | nM | Ki | US-20050059664-A1. Novel methods for identifying improved, non-sedating alpha-2 agonists (2005) |
| β1-adrenoceptor in Human [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] |
| GtoPdb | - | - | 7.9 | 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 | 4.59 | pKi | 26000 | nM | Ki | J Med Chem (2000) 43: 1611-1619 [PMID:10780918] |
| ChEMBL | Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranes | B | 5.57 | pKi | 2700 | 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 | 5.8 | pKi | 1600 | 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 | 5.89 | pKi | 1300 | nM | Ki | J Med Chem (2000) 43: 1611-1619 [PMID:10780918] |
| ChEMBL | Tested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligand | B | 6.9 | pKi | 126 | nM | Ki | J Med Chem (1993) 36: 3077-3086 [PMID:8230093] |
| ChEMBL | Compound was evaluated for beta adrenergic binding affinity towards Beta-1 adrenergic receptor of rat brain | B | 6.9 | pKi | 126 | nM | Ki | J Med Chem (1992) 35: 1009-1018 [PMID:1313109] |
| 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 | 6.4 | pKi | 400 | nM | Ki | J Med Chem (1988) 31: 1972-1977 [PMID:2845082] |
| ChEMBL | Effective dose required to stimulate contractions in isolated guinea pig atrium. | F | 5 | pEC50 | 10000 | 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 | 6.46 | pEC50 | 350 | nM | EC50 | J Med Chem (1988) 31: 1972-1977 [PMID:2845082] |
| ChEMBL | Effective concentration for Beta-1 adrenergic receptor mediated inhibition of neurotransmission in field-stimulated reserpine pretreated guinea pig ileum. | F | 7.52 | pEC50 | 30 | 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 | 5.4 | pKd | 3981.07 | nM | Kd | Bioorg Med Chem Lett (2013) 23: 5376-5381 [PMID:23954364] |
| ChEMBL | Binding affinity to human adrenergic beta2 receptor | B | 5.4 | pKd | 3980 | nM | Kd | Eur J Med Chem (2009) 44: 2840-2846 [PMID:19168263] |
| ChEMBL | Displacement of [3H]prazosin from human adrenergic beta2 receptor expressed in CHO cell membrane | B | 4.01 | pKi | 96700 | nM | Ki | Bioorg Med Chem (2009) 17: 7987-7992 [PMID:19857969] |
| GtoPdb | - | - | 5.4 | 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 | Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells | B | 5.48 | pKi | 3300 | nM | Ki | Bioorg Med Chem (2016) 24: 2641-2653 [PMID:27132867] |
| GtoPdb | - | - | 6.4 | 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 | 4.57 | pKi | 27000 | 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 | 4.96 | pKi | 11000 | 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 | 5.3 | pKi | 5000 | nM | Ki | J Med Chem (2000) 43: 1611-1619 [PMID:10780918] |
| Beta-2 adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3373] [UniProtKB: Q28044] | ||||||||
| ChEMBL | Tested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligand | B | 5.22 | pKi | 6000 | nM | Ki | J Med Chem (1993) 36: 3077-3086 [PMID:8230093] |
| ChEMBL | Compound was evaluated for beta adrenergic binding affinity towards beta-2 receptor of bovine lung | B | 5.22 | pKi | 6000 | nM | Ki | J Med Chem (1992) 35: 1009-1018 [PMID:1313109] |
| 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 | 5.38 | pKi | 4200 | 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 | Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea. | F | 4.52 | pEC50 | 30000 | nM | EC50 | J Med Chem (1995) 38: 3681-3716 [PMID:7562902] |
| ChEMBL | Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea. | F | 6.67 | pEC50 | 213 | 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 | - | - | 6.3 | pKi | - | - | - |
Annu Rev Pharmacol Toxicol (1997) 37: 421-50 [PMID:9131260]; Naunyn Schmiedebergs Arch Pharmacol (2004) 369: 151-9 [PMID:14730417]; Eur J Pharmacol (2004) 484: 323-31 [PMID:14744619] |
| GtoPdb | - | - | 7.2 | 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 | 8.2 | pEC50 | 6.3 | 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 | 8.26 | pEC50 | 5.5 | nM | EC50 | Bioorg Med Chem (2008) 16: 2473-2488 [PMID:18083578] |
| β3-adrenoceptor in Mouse [GtoPdb: 30] [UniProtKB: P25962] | ||||||||
| GtoPdb | - | - | 3.8 | pKi | - | - | - | Eur J Pharmacol (2004) 484: 323-31 [PMID:14744619] |
| β3-adrenoceptor/Beta-3 adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4031] [GtoPdb: 30] [UniProtKB: P26255] | ||||||||
| GtoPdb | - | - | 4.2 | pKi | - | - | - | Eur J Pharmacol (2004) 484: 323-31 [PMID:14744619] |
| ChEMBL | Activity for beta 3-adrenoceptor was assessed from effect on stimulation of lipolysis in rat adipocytes. | F | 4 | pEC50 | 100000 | nM | EC50 | J Med Chem (1995) 38: 3681-3716 [PMID:7562902] |
| ChEMBL | Effective dose for contraction of reserpine-pretreated rat vas deferens | F | 5.8 | pEC50 | 1580 | nM | EC50 | J Med Chem (1995) 38: 3681-3716 [PMID:7562902] |
| 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 | 4.3 | pKd | 50000 | 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 | 5.89 | pKi | 1300 | nM | Ki | Bioorg Med Chem (2016) 24: 2641-2653 [PMID:27132867] |
| Nischarin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3923] [UniProtKB: Q9Y2I1] | ||||||||
| ChEMBL | Displacement of [3H]-clonidine from bovine imidazoline receptor I-1 | B | 4 | pKi | >100000 | nM | Ki | J Med Chem (1996) 39: 1193-1195 [PMID:8632424] |
| Vesicular acetylcholine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2125] [GtoPdb: 1013] [UniProtKB: Q62666] | ||||||||
| ChEMBL | Displacement of [125I]O-iodo-trans-decalinvesamicol from VAChT in Sprague-Dawley rat cerebral membrane after 1 hr by gamma counting | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem (2012) 20: 4936-4941 [PMID:22831799] |
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]
