propranolol [Ligand Id: 564] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL27 (AY-64043-, Betalong, .beta.-propranolol, Dl-propranolol, Euprovasin, Inderal, Inderide-40/25, Inderide-80/25, Propranolol, Proprasylyt, Reducor)
  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
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  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
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  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
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  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
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  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
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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]
  • 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 in Rat [GtoPdb: 30] [UniProtKB: P26255]
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  • Sodium/bile acid and sulphated solute cotransporter 1/Bile acid transporter in Human [ChEMBL: CHEMBL5287] [GtoPdb: 959] [UniProtKB: Q14973]
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  • CCK1 receptor/Cholecystokinin A receptor in Human [ChEMBL: CHEMBL1901] [GtoPdb: 76] [UniProtKB: P32238]
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  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
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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]
  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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  • D3 receptor/Dopamine D3 receptor in Rat [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
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  • ETA receptor/Endothelin receptor ET-A in Human [ChEMBL: CHEMBL252] [GtoPdb: 219] [UniProtKB: P25101]
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  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
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  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
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  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
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  • M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
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  • Plasmodium falciparum (isolate K1 / Thailand) in Plasmodium falciparum K1 [ChEMBL: CHEMBL612856]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
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  • SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
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  • Nav1.5/Sodium channel protein type V alpha subunit in Human [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
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  • Organic cation transporter 1/Solute carrier family 22 member 1 in Human [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
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  • AT1 receptor/Type-1 angiotensin II receptor in Human [ChEMBL: CHEMBL227] [GtoPdb: 34] [UniProtKB: P30556]
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  • V1A receptor/Vasopressin V1a receptor in Human [ChEMBL: CHEMBL1889] [GtoPdb: 366] [UniProtKB: P37288]
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  • Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig [ChEMBL: CHEMBL2366456] [UniProtKB: O35505]
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  • Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL Antagonist activity at human wild-type A2A receptor expressed in CHO-K1 cells assessed as NECA-induced cAMP by HTRF assay F 5.3 pIC50 >5011.87 nM IC50 J. Med. Chem. (2015) 58: 9287-9295 [PMID:26565745]
ChEMBL Agonist activity at human wild-type A2A receptor expressed in CHO-K1 cells assessed as cAMP level by HTRF assay F 5.3 pEC50 >5011.87 nM EC50 J. Med. Chem. (2015) 58: 9287-9295 [PMID:26565745]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL Antagonist activity at human wild-type A3 receptor expressed in CHO-K1 cells assessed as IB MECA-induced cAMP by HTRF assay F 5.3 pIC50 >5011.87 nM IC50 J. Med. Chem. (2015) 58: 9287-9295 [PMID:26565745]
ChEMBL Agonist activity at human wild-type A3 receptor expressed in CHO-K1 cells assessed as cAMP level by HTRF assay F 5.3 pEC50 >5011.87 nM EC50 J. Med. Chem. (2015) 58: 9287-9295 [PMID:26565745]
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
ChEMBL Antagonist activity at human wild-type alpha 1A receptor expressed in CHO cells assessed as EP-induced calcium by HTRF assay F 5.3 pIC50 >5011.87 nM IC50 J. Med. Chem. (2015) 58: 9287-9295 [PMID:26565745]
ChEMBL Agonist activity at human wild-type alpha 1A receptor expressed in CHO cells assessed as calcium level by HTRF assay F 5.3 pEC50 >5011.87 nM EC50 J. Med. Chem. (2015) 58: 9287-9295 [PMID:26565745]
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL Antagonist activity at human wild-type alpha 2A receptor expressed in CHO-K1 cells assessed as epinephrine-induced cAMP by HTRF assay F 5.3 pIC50 >5011.87 nM IC50 J. Med. Chem. (2015) 58: 9287-9295 [PMID:26565745]
ChEMBL Agonist activity at human wild-type alpha 2A receptor expressed in CHO-K1 cells assessed as cAMP level by HTRF assay F 5.3 pEC50 >5011.87 nM EC50 J. Med. Chem. (2015) 58: 9287-9295 [PMID:26565745]
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
ChEMBL Antagonist activity at human wild-type alpha 2C receptor expressed in CHO-K1 cells assessed as epinephrine-induced cAMP by HTRF assay F 5.3 pIC50 >5011.87 nM IC50 J. Med. Chem. (2015) 58: 9287-9295 [PMID:26565745]
ChEMBL Agonist activity at human wild-type alpha 2C receptor expressed in CHO-K1 cells assessed as cAMP level by HTRF assay F 5.3 pEC50 >5011.87 nM EC50 J. Med. Chem. (2015) 58: 9287-9295 [PMID:26565745]
β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
ChEMBL Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis F 6.7 pKd 199.53 nM Kd J. Med. Chem. (2011) 54: 6874-6887 [PMID:21870877]
ChEMBL Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cells B 8.22 pKd 6.03 nM Kd J. Med. Chem. (2011) 54: 6874-6887 [PMID:21870877]
ChEMBL Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis F 8.74 pKd 1.82 nM Kd J. Med. Chem. (2011) 54: 6874-6887 [PMID:21870877]
ChEMBL Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation counting B 7.93 pKi 11.75 nM Ki J Med Chem (2018) 61: 5380-5394 [PMID:29851481]
ChEMBL Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes. B 8.64 pKi 2.3 nM Ki J. Med. Chem. (1993) 36: 157-161 [PMID:8093626]
ChEMBL DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) B 8.83 pKi 1.47 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Displacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T cell membranes B 8.85 pKi 1.4 nM Ki Bioorg Med Chem (2019) 27: 2959-2971 [PMID:31151791]
ChEMBL Antagonist activity at human beta1 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assay F 6.6 pIC50 251.19 nM IC50 J. Med. Chem. (2015) 58: 9287-9295 [PMID:26565745]
ChEMBL Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogs B 7.74 pIC50 18 nM IC50 J. Med. Chem. (1990) 33: 2883-2891 [PMID:1976812]
ChEMBL DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) B 8.59 pIC50 2.54 nM IC50 DrugMatrix in vitro pharmacology data
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 adrenoceptor expressed in HEK293T cell membranes B 8.62 pKi 2.4 nM Ki Bioorg Med Chem (2019) 27: 2959-2971 [PMID:31151791]
β1-adrenoceptor/Beta-1 adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3252] [GtoPdb: 28] [UniProtKB: P18090]
ChEMBL Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for S-enantiomer) F 5.58 pKd 2630.27 nM Kd J. Med. Chem. (1998) 41: 1613-1618 [PMID:9572886]
ChEMBL Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria F 8.36 pKd 4.37 nM Kd J. Med. Chem. (1987) 30: 1003-1011 [PMID:2884312]
ChEMBL Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria F 8.36 pKd 4.37 nM Kd