Found 27 hits Enz. Inhib. hit(s) with Target = 'Beta-1 adrenergic receptor' and Ligand = 'BDBM25761' Target/Host (Institution) | Ligand | Target/Host Links | Ligand Links | Trg + Lig Links | Ki nM | ΔG° kJ/mole | IC50 nM | Kd nM | EC50/IC50 nM | koff s-1 | kon M-1s-1 | pH | Temp °C |
Beta-1 adrenergic receptor
(Homo sapiens (Human)) | BDBM25761
(Anapriline | Avlocardyl | CHEMBL27 | PROPANOLOL(-)...)Show InChI InChI=1S/C16H21NO2/c1-12(2)17-10-14(18)11-19-16-9-5-7-13-6-3-4-8-15(13)16/h3-9,12,14,17-18H,10-11H2,1-2H3 | PDB
Reactome pathway KEGG
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| DrugBank Article PubMed
| 0.0200 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Janssen Research Foundation
Curated by PDSP Ki Database
| |
Psychopharmacology (Berl) 124: 57-73 (1996)
Article DOI: 10.1007/bf02245606 BindingDB Entry DOI: 10.7270/Q2610XV6 |
More data for this Ligand-Target Pair | |
Beta-1 adrenergic receptor
(Rattus norvegicus (Rat)) | BDBM25761
(Anapriline | Avlocardyl | CHEMBL27 | PROPANOLOL(-)...)Show InChI InChI=1S/C16H21NO2/c1-12(2)17-10-14(18)11-19-16-9-5-7-13-6-3-4-8-15(13)16/h3-9,12,14,17-18H,10-11H2,1-2H3 | PDB
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| Article PubMed
| 0.690 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Niigata College of Pharmacy
Curated by PDSP Ki Database
| |
Jpn J Pharmacol 52: 195-200 (1990)
Article DOI: 10.1254/jjp.52.195 BindingDB Entry DOI: 10.7270/Q2H41PXD |
More data for this Ligand-Target Pair | |
Beta-1 adrenergic receptor
(Homo sapiens (Human)) | BDBM25761
(Anapriline | Avlocardyl | CHEMBL27 | PROPANOLOL(-)...)Show InChI InChI=1S/C16H21NO2/c1-12(2)17-10-14(18)11-19-16-9-5-7-13-6-3-4-8-15(13)16/h3-9,12,14,17-18H,10-11H2,1-2H3 | PDB
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| DrugBank Article PubMed
| 1.40 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Friedrich-Alexander Universit£t Erlangen-N£rnberg
Curated by ChEMBL
| Assay Description Displacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T cell membranes |
Bioorg Med Chem 27: 2959-2971 (2019)
Article DOI: 10.1016/j.bmc.2019.05.034 BindingDB Entry DOI: 10.7270/Q2FB56CD |
More data for this Ligand-Target Pair | |
Beta-1 adrenergic receptor
(Homo sapiens (Human)) | BDBM25761
(Anapriline | Avlocardyl | CHEMBL27 | PROPANOLOL(-)...)Show InChI InChI=1S/C16H21NO2/c1-12(2)17-10-14(18)11-19-16-9-5-7-13-6-3-4-8-15(13)16/h3-9,12,14,17-18H,10-11H2,1-2H3 | PDB
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| DrugBank Article PubMed
| 1.80 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Universität Würzburg
Curated by PDSP Ki Database
| |
Naunyn Schmiedebergs Arch Pharmacol 369: 151-9 (2004)
Article DOI: 10.1007/s00210-003-0860-y BindingDB Entry DOI: 10.7270/Q2PZ57C6 |
More data for this Ligand-Target Pair | |
Beta-1 adrenergic receptor
(Homo sapiens (Human)) | BDBM25761
(Anapriline | Avlocardyl | CHEMBL27 | PROPANOLOL(-)...)Show InChI InChI=1S/C16H21NO2/c1-12(2)17-10-14(18)11-19-16-9-5-7-13-6-3-4-8-15(13)16/h3-9,12,14,17-18H,10-11H2,1-2H3 | PDB
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| 2.30 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Università di Perugia
Curated by ChEMBL
| Assay Description Inhibition of [3H]-Dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes. |
J Med Chem 36: 157-61 (1993)
BindingDB Entry DOI: 10.7270/Q2ZK5FQV |
More data for this Ligand-Target Pair | |
Beta-1 adrenergic receptor
(Mus musculus) | BDBM25761
(Anapriline | Avlocardyl | CHEMBL27 | PROPANOLOL(-)...)Show InChI InChI=1S/C16H21NO2/c1-12(2)17-10-14(18)11-19-16-9-5-7-13-6-3-4-8-15(13)16/h3-9,12,14,17-18H,10-11H2,1-2H3 | PDB
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| Article PubMed
| 2.40 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Friedrich-Alexander Universit£t Erlangen-N£rnberg
Curated by ChEMBL
| Assay Description Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranes |
Bioorg Med Chem 27: 2959-2971 (2019)
Article DOI: 10.1016/j.bmc.2019.05.034 BindingDB Entry DOI: 10.7270/Q2FB56CD |
More data for this Ligand-Target Pair | |
Beta-1 adrenergic receptor
(Homo sapiens (Human)) | BDBM25761
(Anapriline | Avlocardyl | CHEMBL27 | PROPANOLOL(-)...)Show InChI InChI=1S/C16H21NO2/c1-12(2)17-10-14(18)11-19-16-9-5-7-13-6-3-4-8-15(13)16/h3-9,12,14,17-18H,10-11H2,1-2H3 | PDB
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| 2.69 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Ohio State University
Curated by PDSP Ki Database
| |
J Pharmacol Exp Ther 270: 665-74 (1994)
BindingDB Entry DOI: 10.7270/Q2RN36CJ |
More data for this Ligand-Target Pair | |
Beta-1 adrenergic receptor
(Rattus norvegicus (Rat)) | BDBM25761
(Anapriline | Avlocardyl | CHEMBL27 | PROPANOLOL(-)...)Show InChI InChI=1S/C16H21NO2/c1-12(2)17-10-14(18)11-19-16-9-5-7-13-6-3-4-8-15(13)16/h3-9,12,14,17-18H,10-11H2,1-2H3 | PDB
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| | 3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
The Medical University of Warsaw
| Assay Description Radioligand receptor binding studies were conducted in the rat brain. |
Medicinal Chemistry Research 17: 507-514 (2008)
BindingDB Entry DOI: 10.7270/Q2Z036S7 |
More data for this Ligand-Target Pair | |
Beta-1 adrenergic receptor
(GUINEA PIG) | BDBM25761
(Anapriline | Avlocardyl | CHEMBL27 | PROPANOLOL(-)...)Show InChI InChI=1S/C16H21NO2/c1-12(2)17-10-14(18)11-19-16-9-5-7-13-6-3-4-8-15(13)16/h3-9,12,14,17-18H,10-11H2,1-2H3 | PDB
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| 5.24 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Ohio State University
Curated by PDSP Ki Database
| |
J Pharmacol Exp Ther 270: 665-74 (1994)
BindingDB Entry DOI: 10.7270/Q2RN36CJ |
More data for this Ligand-Target Pair | |
Beta-1 adrenergic receptor
(Rattus norvegicus (Rat)) | BDBM25761
(Anapriline | Avlocardyl | CHEMBL27 | PROPANOLOL(-)...)Show InChI InChI=1S/C16H21NO2/c1-12(2)17-10-14(18)11-19-16-9-5-7-13-6-3-4-8-15(13)16/h3-9,12,14,17-18H,10-11H2,1-2H3 | PDB
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| Article PubMed
| 7 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Jagiellonian University Medical College
Curated by ChEMBL
| Assay Description Displacement of [3H]CGP-12177 from beta1 adrenergic receptor in rat brain cerebral cortex after 60 mins by microbeta scintillation counting method |
Bioorg Med Chem Lett 26: 5315-5321 (2016)
Article DOI: 10.1016/j.bmcl.2016.09.037 BindingDB Entry DOI: 10.7270/Q24J0H3X |
More data for this Ligand-Target Pair | |
Beta-1 adrenergic receptor
(Homo sapiens (Human)) | BDBM25761
(Anapriline | Avlocardyl | CHEMBL27 | PROPANOLOL(-)...)Show InChI InChI=1S/C16H21NO2/c1-12(2)17-10-14(18)11-19-16-9-5-7-13-6-3-4-8-15(13)16/h3-9,12,14,17-18H,10-11H2,1-2H3 | PDB
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| 12 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
University of Florence
Curated by ChEMBL
| Assay Description Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation counting |
J Med Chem 61: 5380-5394 (2018)
Article DOI: 10.1021/acs.jmedchem.8b00625 BindingDB Entry DOI: 10.7270/Q2XS5XX3 |
More data for this Ligand-Target Pair | |
Beta-1 adrenergic receptor
(Rattus norvegicus (Rat)) | BDBM25761
(Anapriline | Avlocardyl | CHEMBL27 | PROPANOLOL(-)...)Show InChI InChI=1S/C16H21NO2/c1-12(2)17-10-14(18)11-19-16-9-5-7-13-6-3-4-8-15(13)16/h3-9,12,14,17-18H,10-11H2,1-2H3 | PDB
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| Article PubMed
| 15 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Jagiellonian University Medical College
Curated by ChEMBL
| Assay Description Displacement of [3H]-CGP-12177 from beta1-adrenergic receptor in rat brain cortex after 1 hr by Microbeta scintillation counting method |
Eur J Med Chem 147: 102-114 (2018)
Article DOI: 10.1016/j.ejmech.2018.01.093 BindingDB Entry DOI: 10.7270/Q29P346S |
More data for this Ligand-Target Pair | |
Beta-1 adrenergic receptor
(Rattus norvegicus (Rat)) | BDBM25761
(Anapriline | Avlocardyl | CHEMBL27 | PROPANOLOL(-)...)Show InChI InChI=1S/C16H21NO2/c1-12(2)17-10-14(18)11-19-16-9-5-7-13-6-3-4-8-15(13)16/h3-9,12,14,17-18H,10-11H2,1-2H3 | PDB
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| Article PubMed
| 81.3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Niigata College of Pharmacy
Curated by PDSP Ki Database
| |
Jpn J Pharmacol 52: 195-200 (1990)
Article DOI: 10.1254/jjp.52.195 BindingDB Entry DOI: 10.7270/Q2H41PXD |
More data for this Ligand-Target Pair | |
Beta-1 adrenergic receptor
(Rattus norvegicus (Rat)) | BDBM25761
(Anapriline | Avlocardyl | CHEMBL27 | PROPANOLOL(-)...)Show InChI InChI=1S/C16H21NO2/c1-12(2)17-10-14(18)11-19-16-9-5-7-13-6-3-4-8-15(13)16/h3-9,12,14,17-18H,10-11H2,1-2H3 | PDB
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| Article PubMed
| 9.70E+3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Jagiellonian University Medical College
Curated by ChEMBL
| Assay Description Displacement of [3H]CGP12177 from beta1 adrenergic receptor in rat cerebral cortex by liquid scintillation counting |
Bioorg Med Chem 17: 1345-52 (2009)
Article DOI: 10.1016/j.bmc.2008.12.031 BindingDB Entry DOI: 10.7270/Q2KP8213 |
More data for this Ligand-Target Pair | |
Beta-1 adrenergic receptor
(Homo sapiens (Human)) | BDBM25761
(Anapriline | Avlocardyl | CHEMBL27 | PROPANOLOL(-)...)Show InChI InChI=1S/C16H21NO2/c1-12(2)17-10-14(18)11-19-16-9-5-7-13-6-3-4-8-15(13)16/h3-9,12,14,17-18H,10-11H2,1-2H3 | PDB
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| n/a | n/a | 18 | n/a | n/a | n/a | n/a | n/a | n/a |
Berlex Laboratories
Curated by ChEMBL
| Assay Description Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogs |
J Med Chem 33: 2883-91 (1990)
BindingDB Entry DOI: 10.7270/Q2416XN5 |
More data for this Ligand-Target Pair | |
Beta-1 adrenergic receptor
(GUINEA PIG) | BDBM25761
(Anapriline | Avlocardyl | CHEMBL27 | PROPANOLOL(-)...)Show InChI InChI=1S/C16H21NO2/c1-12(2)17-10-14(18)11-19-16-9-5-7-13-6-3-4-8-15(13)16/h3-9,12,14,17-18H,10-11H2,1-2H3 | PDB
UniProtKB/TrEMBL
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| PubMed
| n/a | n/a | 35 | n/a | n/a | n/a | n/a | n/a | n/a |
Universit£ di Pisa
Curated by ChEMBL
| Assay Description Inhibitory activity against beta-1 adrenergic receptor in guinea pig atria is determined |
J Med Chem 36: 3077-86 (1993)
BindingDB Entry DOI: 10.7270/Q2PG1SB1 |
More data for this Ligand-Target Pair | |
Beta-1 adrenergic receptor
(Homo sapiens (Human)) | BDBM25761
(Anapriline | Avlocardyl | CHEMBL27 | PROPANOLOL(-)...)Show InChI InChI=1S/C16H21NO2/c1-12(2)17-10-14(18)11-19-16-9-5-7-13-6-3-4-8-15(13)16/h3-9,12,14,17-18H,10-11H2,1-2H3 | PDB
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| DrugBank Article PubMed
| n/a | n/a | 251 | n/a | n/a | n/a | n/a | n/a | n/a |
Janssen Pharmaceutica N.V.
Curated by ChEMBL
| Assay Description Antagonist activity at human beta1 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assay |
J Med Chem 58: 9287-95 (2015)
Article DOI: 10.1021/acs.jmedchem.5b01088 BindingDB Entry DOI: 10.7270/Q21C20VP |
More data for this Ligand-Target Pair | |
Beta-1 adrenergic receptor
(GUINEA PIG) | BDBM25761
(Anapriline | Avlocardyl | CHEMBL27 | PROPANOLOL(-)...)Show InChI InChI=1S/C16H21NO2/c1-12(2)17-10-14(18)11-19-16-9-5-7-13-6-3-4-8-15(13)16/h3-9,12,14,17-18H,10-11H2,1-2H3 | PDB
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| n/a | n/a | n/a | 2.40 | n/a | n/a | n/a | n/a | n/a |
TBA
Curated by ChEMBL
| Assay Description Beta-1 adrenergic receptor blocking activity in atria of guinea pig. |
J Med Chem 27: 1291-4 (1984)
BindingDB Entry DOI: 10.7270/Q23779W0 |
More data for this Ligand-Target Pair | |
Beta-1 adrenergic receptor
(Homo sapiens (Human)) | BDBM25761
(Anapriline | Avlocardyl | CHEMBL27 | PROPANOLOL(-)...)Show InChI InChI=1S/C16H21NO2/c1-12(2)17-10-14(18)11-19-16-9-5-7-13-6-3-4-8-15(13)16/h3-9,12,14,17-18H,10-11H2,1-2H3 | PDB
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| DrugBank Article PubMed
| n/a | n/a | n/a | 200 | n/a | n/a | n/a | n/a | n/a |
University of Nottingham
Curated by ChEMBL
| Assay Description Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluoresce... |
J Med Chem 54: 6874-87 (2011)
Article DOI: 10.1021/jm2008562 BindingDB Entry DOI: 10.7270/Q29S1SBQ |
More data for this Ligand-Target Pair | |
Beta-1 adrenergic receptor
(GUINEA PIG) | BDBM25761
(Anapriline | Avlocardyl | CHEMBL27 | PROPANOLOL(-)...)Show InChI InChI=1S/C16H21NO2/c1-12(2)17-10-14(18)11-19-16-9-5-7-13-6-3-4-8-15(13)16/h3-9,12,14,17-18H,10-11H2,1-2H3 | PDB
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| PubMed
| n/a | n/a | n/a | 8.70 | n/a | n/a | n/a | n/a | n/a |
TBA
Curated by ChEMBL
| Assay Description Antagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atria |
J Med Chem 24: 994-8 (1982)
BindingDB Entry DOI: 10.7270/Q2JH3ND4 |
More data for this Ligand-Target Pair | |
Beta-1 adrenergic receptor
(GUINEA PIG) | BDBM25761
(Anapriline | Avlocardyl | CHEMBL27 | PROPANOLOL(-)...)Show InChI InChI=1S/C16H21NO2/c1-12(2)17-10-14(18)11-19-16-9-5-7-13-6-3-4-8-15(13)16/h3-9,12,14,17-18H,10-11H2,1-2H3 | PDB
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| PubMed
| n/a | n/a | n/a | 2.40 | n/a | n/a | n/a | n/a | n/a |
TBA
Curated by ChEMBL
| Assay Description Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pig |
J Med Chem 23: 620-4 (1980)
BindingDB Entry DOI: 10.7270/Q2Q52QT2 |
More data for this Ligand-Target Pair | |
Beta-1 adrenergic receptor
(Homo sapiens (Human)) | BDBM25761
(Anapriline | Avlocardyl | CHEMBL27 | PROPANOLOL(-)...)Show InChI InChI=1S/C16H21NO2/c1-12(2)17-10-14(18)11-19-16-9-5-7-13-6-3-4-8-15(13)16/h3-9,12,14,17-18H,10-11H2,1-2H3 | PDB
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| DrugBank Article PubMed
| n/a | n/a | n/a | 6.90 | n/a | n/a | n/a | 7.4 | 37 |
University of Nottingham
| Assay Description The whole cell-binding studies were undertaken in CHO cell lines stably expressing each beta-adrenoceptor subtype. Nonspecific binding was determined... |
Br J Pharmacol 144: 317-22 (2005)
Article DOI: 10.1038/sj.bjp.0706048 BindingDB Entry DOI: 10.7270/Q28C9TKV |
More data for this Ligand-Target Pair | |
Beta-1 adrenergic receptor
(Homo sapiens (Human)) | BDBM25761
(Anapriline | Avlocardyl | CHEMBL27 | PROPANOLOL(-)...)Show InChI InChI=1S/C16H21NO2/c1-12(2)17-10-14(18)11-19-16-9-5-7-13-6-3-4-8-15(13)16/h3-9,12,14,17-18H,10-11H2,1-2H3 | PDB
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| DrugBank Article PubMed
| n/a | n/a | n/a | 6 | n/a | n/a | n/a | n/a | n/a |
University of Nottingham
Curated by ChEMBL
| Assay Description Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cells |
J Med Chem 54: 6874-87 (2011)
Article DOI: 10.1021/jm2008562 BindingDB Entry DOI: 10.7270/Q29S1SBQ |
More data for this Ligand-Target Pair | |
Beta-1 adrenergic receptor
(Homo sapiens (Human)) | BDBM25761
(Anapriline | Avlocardyl | CHEMBL27 | PROPANOLOL(-)...)Show InChI InChI=1S/C16H21NO2/c1-12(2)17-10-14(18)11-19-16-9-5-7-13-6-3-4-8-15(13)16/h3-9,12,14,17-18H,10-11H2,1-2H3 | PDB
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| DrugBank Article PubMed
| n/a | n/a | n/a | 1.80 | n/a | n/a | n/a | n/a | n/a |
University of Nottingham
Curated by ChEMBL
| Assay Description Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluoresce... |
J Med Chem 54: 6874-87 (2011)
Article DOI: 10.1021/jm2008562 BindingDB Entry DOI: 10.7270/Q29S1SBQ |
More data for this Ligand-Target Pair | |
Beta-1 adrenergic receptor
(GUINEA PIG) | BDBM25761
(Anapriline | Avlocardyl | CHEMBL27 | PROPANOLOL(-)...)Show InChI InChI=1S/C16H21NO2/c1-12(2)17-10-14(18)11-19-16-9-5-7-13-6-3-4-8-15(13)16/h3-9,12,14,17-18H,10-11H2,1-2H3 | PDB
UniProtKB/TrEMBL
GoogleScholar AffyNet
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CHEMBL DrugBank MCE KEGG PC cid PC sid PDB UniChem
Patents
Similars
| PubMed
| n/a | n/a | n/a | 1.70 | n/a | n/a | n/a | n/a | n/a |
TBA
Curated by ChEMBL
| Assay Description In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea p... |
J Med Chem 26: 950-7 (1983)
BindingDB Entry DOI: 10.7270/Q2GH9K4C |
More data for this Ligand-Target Pair | |
Beta-1 adrenergic receptor
(GUINEA PIG) | BDBM25761
(Anapriline | Avlocardyl | CHEMBL27 | PROPANOLOL(-)...)Show InChI InChI=1S/C16H21NO2/c1-12(2)17-10-14(18)11-19-16-9-5-7-13-6-3-4-8-15(13)16/h3-9,12,14,17-18H,10-11H2,1-2H3 | PDB
UniProtKB/TrEMBL
GoogleScholar AffyNet
| Purchase
CHEMBL DrugBank MCE KEGG PC cid PC sid PDB UniChem
Patents
Similars
| PubMed
| n/a | n/a | n/a | 3.10 | n/a | n/a | n/a | n/a | n/a |
TBA
Curated by ChEMBL
| Assay Description Compound was evaluated for competitive antagonism of beta-1 adrenergic receptor in guinea pig atria measured as pA2 (-log KB) |
J Med Chem 27: 857-61 (1984)
BindingDB Entry DOI: 10.7270/Q22B906S |
More data for this Ligand-Target Pair | |
Beta-1 adrenergic receptor
(GUINEA PIG) | BDBM25761
(Anapriline | Avlocardyl | CHEMBL27 | PROPANOLOL(-)...)Show InChI InChI=1S/C16H21NO2/c1-12(2)17-10-14(18)11-19-16-9-5-7-13-6-3-4-8-15(13)16/h3-9,12,14,17-18H,10-11H2,1-2H3 | PDB
UniProtKB/TrEMBL
GoogleScholar AffyNet
| Purchase
CHEMBL DrugBank MCE KEGG PC cid PC sid PDB UniChem
Patents
Similars
| PubMed
| n/a | n/a | n/a | 2 | n/a | n/a | n/a | n/a | n/a |
TBA
Curated by ChEMBL
| Assay Description Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparation |
J Med Chem 25: 1408-12 (1983)
BindingDB Entry DOI: 10.7270/Q2S183PB |
More data for this Ligand-Target Pair | |