isoprenaline [Ligand Id: 536] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL434 (A-21, Aleudrin, Aludrine, Asiprenol, Asmalar, Assiprenol, Bellasthman, Isonorin, Isoprenaline, Isopropydrin, Isoproterenol, Isoproterenol dl-form, Isorenin, Isupren, Neodrenal, Neo-epinine, Novodrin, NSC-33791, NSC-9975, Proternol, Respifral, Saventrine, Vapo-n-iso)
  • Arachidonate 15-lipoxygenase in Rabbit [ChEMBL: CHEMBL4358] [UniProtKB: P12530]
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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 Mouse [ChEMBL: CHEMBL3440] [GtoPdb: 28] [UniProtKB: P34971]
  • 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]
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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]
  • Beta-2 adrenergic receptor in Bovine [ChEMBL: CHEMBL3373] [UniProtKB: Q28044]
  • 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]
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  • β3-adrenoceptor/Beta-3 adrenergic receptor in Human [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945]
  • β3-adrenoceptor in Mouse [GtoPdb: 30] [UniProtKB: P25962]
  • β3-adrenoceptor/Beta-3 adrenergic receptor in Rat [ChEMBL: CHEMBL4031] [GtoPdb: 30] [UniProtKB: P26255]
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  • D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Arachidonate 15-lipoxygenase in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4358] [UniProtKB: P12530]
ChEMBL DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid) B 5.75 pIC50 1770 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]
ChEMBL Binding Affinity against human Beta-1 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligand B 5.8 pKi 1584.89 nM Ki J. Med. Chem. (1999) 42: 2287-2294 [PMID:10377236]
ChEMBL DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) B 6.71 pKi 193 nM Ki DrugMatrix in vitro pharmacology data
GtoPdb - - 7 pKi - - - Eur J Pharmacol (1996) 315: 363-7 [PMID:8982677];
Proc Natl Acad Sci USA (1988) 85: 9494-8 [PMID:2849109]
ChEMBL DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) B 6.48 pIC50 333 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol F 6 pEC50 1000 nM EC50 Bioorg. Med. Chem. (2009) 17: 5510-5519 [PMID:19581100]
ChEMBL Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation F 7 pEC50 100 nM EC50 Bioorg. Med. Chem. (2009) 17: 3283-3294 [PMID:19362005]
ChEMBL Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay F 7.92 pEC50 12 nM EC50 Eur. J. Med. Chem. (2009) 44: 2533-2543 [PMID:19232786]
ChEMBL Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay F 7.92 pEC50 12 nM EC50 Bioorg. Med. Chem. (2009) 17: 5510-5519 [PMID:19581100]
ChEMBL Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulation F 8.1 pEC50 7.94 nM EC50 Bioorg. Med. Chem. (2011) 19: 4192-4201 [PMID:21696967]
ChEMBL Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay F 8.1 pEC50 7.94 nM EC50 J. Med. Chem. (2009) 52: 2280-2288 [PMID:19317397]
ChEMBL Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins F 8.1 pEC50 7.94 nM EC50 J. Med. Chem. (2010) 53: 4522-4530 [PMID:20462258]
ChEMBL Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulation F 8.1 pEC50 7.94 nM EC50 Bioorg. Med. Chem. (2011) 19: 6026-6032 [PMID:21925889]
ChEMBL Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay F 8.5 pEC50 3.16 nM EC50 Eur J Med Chem (2018) 152: 424-435 [PMID:29751236]
ChEMBL Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay F 8.5 pEC50 3.16 nM EC50 Bioorg Med Chem (2019) 27: 2306-2314 [PMID:30392952]
ChEMBL Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation F 8.9 pEC50 1.26 nM EC50 Eur J Med Chem (2021) 224: 113697-113697 [PMID:34273662]
ChEMBL Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP production F 9 pEC50 1 nM EC50 J. Med. Chem. (2006) 49: 2758-2771 [PMID:16640337]
ChEMBL Activity against human beta 1 adrenergic receptor (AR), expressed in CHO cells. F 9 pEC50 1 nM EC50 J. Med. Chem. (2002) 45: 567-583 [PMID:11806709]
ChEMBL Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay F 9.08 pEC50 0.84 nM EC50 J. Med. Chem. (2009) 52: 3063-3072 [PMID:19366244]
ChEMBL Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation F 10.08 pEC50 0.08 nM EC50 J. Med. Chem. (2008) 51: 4804-4822 [PMID:18651730]
ChEMBL Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor F 10.08 pEC50 0.08 nM EC50 Bioorg. Med. Chem. Lett. (2005) 15: 251-254 [PMID:15603933]
ChEMBL Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA F 10.08 pEC50 0.08 nM EC50 J. Med. Chem. (2008) 51: 1925-1944 [PMID:18307290]
ChEMBL Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay F 10.08 pEC50 0.08 nM EC50 J. Med. Chem. (2008) 51: 4002-4020 [PMID:18553954]
ChEMBL Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation F 10.08 pEC50 0.08 nM EC50 Bioorg. Med. Chem. Lett. (2008) 18: 5037-5040 [PMID:18752946]
β1-adrenoceptor/Beta-1 adrenergic receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3440] [GtoPdb: 28] [UniProtKB: P34971]
ChEMBL Displacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cells B 6.66 pKi 220 nM Ki Bioorg. Med. Chem. (2016) 24: 2641-2653 [PMID:27132867]
β1-adrenoceptor/Beta-1 adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3252] [GtoPdb: 28] [UniProtKB: P18090]
ChEMBL Compound was evaluated for the inhibition of binding of [3H]dihydroalprenolol from beta-1 adrenergic receptor of rat cerebral cortical membranes B 6.17 pKi 670 nM Ki J. Med. Chem. (1991) 34: 1063-1068 [PMID:1672155]
ChEMBL Tested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligand B 7.1 pKi 80 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 7.1 pKi 80 nM Ki J. Med. Chem. (1992) 35: 1009-1018 [PMID:1313109]
ChEMBL Compound was evaluated for its binding affinity towards beta-1 adrenergic receptor in rat heart membrane by displacing [125I]- iodocyanopindolol B 6.22 pIC50 600 nM IC50 J. Med. Chem. (1992) 35: 3081-3084 [PMID:1354264]
ChEMBL In vitro beta-adrenergic activity against beta-1 adrenergic receptor by the inhibition of insulin stimulated [14C]- glucose incorporation into glycogen in isolated rat soleus muscle F 8.28 pIC50 5.3 nM IC50 J. Med. Chem. (1992) 35: 3081-3084 [PMID:1354264]
Beta-1 adrenergic receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5471] [UniProtKB: B0FL73]
ChEMBL Agonistic activity (beta-1 adrenergic receptor) for the percent maximal increase in contraction rate of isolated guinea pig atria F 8.22 pEC50 6 nM EC50 J. Med. Chem. (1991) 34: 1063-1068 [PMID:1672155]
β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
ChEMBL Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting B 6.13 pKd 740 nM Kd J Med Chem (2016) 59: 5780-5789 [PMID:27239696]
ChEMBL Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM B 6.6 pKd 251.19 nM Kd Bioorg. Med. Chem. Lett. (2013) 23: 5376-5381 [PMID:23954364]
ChEMBL Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting B 6.89 pKd 130 nM Kd J Med Chem (2016) 59: 5780-5789 [PMID:27239696]
ChEMBL Binding affinity to human adrenergic beta2 receptor B 7.3 pKd 50 nM Kd Eur. J. Med. Chem. (2009) 44: 2840-2846 [PMID:19168263]
ChEMBL Binding Affinity against human beta-2 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligand B 6.17 pKi 676.08 nM Ki J. Med. Chem. (1999) 42: 2287-2294 [PMID:10377236]
GtoPdb - - 6.4 pKi - - - Eur J Pharmacol (1996) 315: 363-7 [PMID:8982677]
ChEMBL Displacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis B 6.72 pKi 192 nM Ki Bioorg. Med. Chem. (2014) 22: 234-246 [PMID:24326276]
ChEMBL DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177) B 6.77 pKi 169 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells B 7.34 pKi 46 nM Ki Bioorg. Med. Chem. (2016) 24: 2641-2653 [PMID:27132867]
ChEMBL Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis B 8.61 pKi 2.44 nM Ki Bioorg. Med. Chem. (2014) 22: 234-246 [PMID:24326276]
ChEMBL DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177) B 6.61 pIC50 246 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol F 6 pEC50 1000 nM EC50 Bioorg. Med. Chem. (2009) 17: 5510-5519 [PMID:19581100]
ChEMBL Agonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assay B 6.92 pEC50 120 nM EC50 Bioorg. Med. Chem. (2016) 24: 2641-2653 [PMID:27132867]
ChEMBL Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol F 7.06 pEC50 87 nM EC50 Bioorg. Med. Chem. (2016) 24: 2641-2653 [PMID:27132867]
ChEMBL Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation F 7.4 pEC50 39.81 nM EC50 Bioorg. Med. Chem. (2011) 19: 6026-6032 [PMID:21925889]
ChEMBL Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins F 7.4 pEC50 39.81 nM EC50 J. Med. Chem. (2010) 53: 4522-4530 [PMID:20462258]
ChEMBL Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr F 7.4 pEC50 39.81 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 4027-4031 [PMID:21652207]
ChEMBL Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation F 7.4 pEC50 39.81 nM EC50 Bioorg. Med. Chem. (2011) 19: 4192-4201 [PMID:21696967]
ChEMBL Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay F 7.4 pEC50 39.81 nM EC50 J. Med. Chem. (2009) 52: 2280-2288 [PMID:19317397]
ChEMBL Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay F 8.52 pEC50 3 nM EC50 Eur. J. Med. Chem. (2009) 44: 2533-2543 [PMID:19232786]