(+)-propranolol [Ligand Id: 7596] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL275742 (Dexpropranolol, Propranolol, (r)-)
  • β1-adrenoceptor/Beta-1 adrenergic receptor in Human [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
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  • β2-adrenoceptor/Beta-2 adrenergic receptor in Human [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
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  • TLX/Nuclear receptor subfamily 2 group E member 1 in Human [ChEMBL: CHEMBL1961788] [GtoPdb: 615] [UniProtKB: Q9Y466]
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  • 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 Rat [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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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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  • Sodium/bile acid and sulphated solute cotransporter 1 in Human [GtoPdb: 959] [UniProtKB: Q14973]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
ChEMBL DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) B 6.67 pKi 214 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) B 6.43 pIC50 370 nM IC50 DrugMatrix in vitro pharmacology data
β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
ChEMBL DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177) B 7.28 pKi 52 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177) B 7.12 pIC50 76 nM IC50 DrugMatrix in vitro pharmacology data
TLX/Nuclear receptor subfamily 2 group E member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1961788] [GtoPdb: 615] [UniProtKB: Q9Y466]
ChEMBL Agonist activity at in human TLX LBD expressed in human HEK293T cells coexpressing Gal4-VP 16 assessed as increase in reporter activity measured after 14 hrs by luciferase reporter gene assay relative to control B 4.4 pEC50 40000 nM EC50 J Med Chem (2021) 64: 8727-8738 [PMID:34115934]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) B 5.55 pKi 2789 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Inhibitory activity against 5-hydroxytryptamine 1A receptor of rat hippocampal tissue using [3H]OH-DPAT as radioligand. B 5.77 pKi 1700 nM Ki J Med Chem (1989) 32: 859-863 [PMID:2539480]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) B 5.31 pIC50 4880 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Binding affinity towards 5-hydroxytryptamine 1A receptor in rat frontal cortex using [3H]8-OH-DPAT as a radioligand B 6.77 pIC50 169.82 nM IC50 J Med Chem (1988) 31: 1087-1093 [PMID:3373482]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
ChEMBL Binding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligand B 6.31 pIC50 489.78 nM IC50 J Med Chem (1988) 31: 1087-1093 [PMID:3373482]
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 6.55 pKi 279 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 6.36 pIC50 438 nM IC50 DrugMatrix in vitro pharmacology data
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) B 6.49 pKi 325 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) B 6.21 pIC50 612 nM IC50 DrugMatrix in vitro pharmacology data
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) B 5.78 pKi 1670 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) B 5.4 pIC50 3974 nM IC50 DrugMatrix in vitro pharmacology data
Sodium/bile acid and sulphated solute cotransporter 1 in Human [GtoPdb: 959] [UniProtKB: Q14973]
GtoPdb - - 5.26 pIC50 5500 nM IC50 J Pharmacol Exp Ther (1999) 291: 1204-9 [PMID:10565843]

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]