(-)-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 | - | - | - |
Mol Pharmacol (1995) 48: 250-8 [PMID:7651358]; Br J Pharmacol (1999) 127: 962-8 [PMID:10433504]; J Pharmacol Exp Ther (1995) 272: 134-42 [PMID:7815325]; Mol Pharmacol (2011) 79: 298-307 [PMID:20978120]; Br J Pharmacol (1995) 116: 1611-8 [PMID:8564227]; Br J Pharmacol (2017) 174: 2318-2333 [PMID:28444738]; Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529] |
| 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 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]
