doxazosin [Ligand Id: 7170] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL707 (C02CA04, Cardura, Doxazosin, UK-33274)
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
There should be some charts here, you may need to enable JavaScript!
  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
There should be some charts here, you may need to enable JavaScript!
  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944]
There should be some charts here, you may need to enable JavaScript!
  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
There should be some charts here, you may need to enable JavaScript!
  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
There should be some charts here, you may need to enable JavaScript!
  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
There should be some charts here, you may need to enable JavaScript!
  • β2-adrenoceptor/Beta-2 adrenergic receptor in Human [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • MMP1/Matrix metalloproteinase-1 in Human [ChEMBL: CHEMBL332] [GtoPdb: 1628] [UniProtKB: P03956]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
There should be some charts here, you may need to enable JavaScript!
  • Serotonin 4 (5-HT4) receptor in Guinea pig [ChEMBL: CHEMBL5017] [UniProtKB: O70528]
There should be some charts here, you may need to enable JavaScript!
  • SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
There should be some charts here, you may need to enable JavaScript!
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 In vitro antagonistic activity against alpha-1A receptor in dog prostate. F 7.59 pKd 25.7 nM Kd J. Med. Chem. (2001) 44: 1971-1985 [PMID:11384242]
ChEMBL Binding affinity was tested on human Alpha-1A adrenergic receptor B 8.5 pKi 3.16 nM Ki J. Med. Chem. (1997) 40: 1293-1315 [PMID:9135028]
ChEMBL Binding affinity against Alpha-1A adrenergic receptor from human clone B 8.59 pKi 2.6 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
ChEMBL Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cell membranes after 30 mins B 9.11 pKi 0.78 nM Ki Eur J Med Chem (2017) 136: 259-269 [PMID:28499171]
ChEMBL Displacement of [3H]prazosin from cloned human ADRA1A expressed in CHO cells B 9.27 pKi 0.54 nM Ki J. Med. Chem. (2005) 48: 7750-7763 [PMID:16302814]
ChEMBL Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cells B 9.27 pKi 0.54 nM Ki J. Med. Chem. (2009) 52: 4951-4954 [PMID:19719240]
GtoPdb - - 9.3 pKi 0.54 nM Ki Drug Development Research (1998) 44: 140-162
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens F 8.69 pKd 2.04 nM Kd J. Med. Chem. (2001) 44: 1971-1985 [PMID:11384242]
ChEMBL Antagonist activity at rat alpha1A adrenoceptor assessed as inhibition if norepinephrine-induced contraction of vas deference F 8.69 pKd 2.04 nM Kd J. Med. Chem. (2009) 52: 4951-4954 [PMID:19719240]
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 9.2 pKi 0.63 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 8.81 pIC50 1.55 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Displacement of [3H]-prazosin from rat alpha1A adrenergic receptor after 60 mins by scintillation counting analysis B 9.13 pIC50 0.74 nM IC50 Eur J Med Chem (2018) 143: 1261-1276 [PMID:29128116]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
ChEMBL Binding affinity was tested on human Alpha-1B adrenergic receptor B 9 pKi 1 nM Ki J. Med. Chem. (1997) 40: 1293-1315 [PMID:9135028]
ChEMBL Displacement of [3H]prazosin from cloned human ADRA1B expressed in CHO cells B 9.09 pKi 0.81 nM Ki J. Med. Chem. (2005) 48: 7750-7763 [PMID:16302814]
ChEMBL Displacement of [3H]prazosin from human Alpha-1B adrenoceptor expressed in CHO cells B 9.09 pKi 0.81 nM Ki J. Med. Chem. (2009) 52: 4951-4954 [PMID:19719240]
GtoPdb - - 9.1 pKi 0.81 nM Ki Drug Development Research (1998) 44: 140-162
ChEMBL Binding affinity against Alpha-1B adrenergic receptor from human clone B 9.13 pKi 0.74 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
ChEMBL Displacement of [3H]prazosin from human alpha1B adrenoceptor expressed in CHO cell membranes after 30 mins B 9.2 pKi 0.63 nM Ki Eur J Med Chem (2017) 136: 259-269 [PMID:28499171]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
ChEMBL In vitro antagonistic activity against alpha-1B receptor in rat spleen. F 9.51 pKd 0.31 nM Kd J. Med. Chem. (2001) 44: 1971-1985 [PMID:11384242]
ChEMBL Antagonist activity at rat Alpha-1B adrenoceptor assessed as inhibition if phenylephrine-induced contraction of spleen F 9.51 pKd 0.31 nM Kd J. Med. Chem. (2009) 52: 4951-4954 [PMID:19719240]
ChEMBL DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) B 9.38 pKi 0.42 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) B 9.12 pIC50 0.75 nM IC50 DrugMatrix in vitro pharmacology data
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
ChEMBL Binding affinity was tested on human Alpha-1D adrenergic receptor B 8.4 pKi 3.98 nM Ki J. Med. Chem. (1997) 40: 1293-1315 [PMID:9135028]
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 8.78 pKi 1.66 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Binding affinity against Alpha-1D adrenergic receptor, from human clones. B 8.92 pKi 1.2 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
ChEMBL Displacement of [3H]prazosin from cloned human ADRA1D expressed in CHO cells B 9.09 pKi 0.81 nM Ki J. Med. Chem. (2005) 48: 7750-7763 [PMID:16302814]
ChEMBL Displacement of [3H]prazosin from human Alpha-1D adrenoceptor expressed in CHO cells B 9.09 pKi 0.81 nM Ki J. Med. Chem. (2009) 52: 4951-4954 [PMID:19719240]
GtoPdb - - 9.1 pKi 0.81 nM Ki Drug Development Research (1998) 44: 140-162
ChEMBL Displacement of [3H]prazosin from human alpha1D adrenoceptor expressed in CHO cell membranes after 30 mins B 9.49 pKi 0.32 nM Ki Eur J Med Chem (2017) 136: 259-269 [PMID:28499171]
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 8.47 pIC50 3.38 nM IC50 DrugMatrix in vitro pharmacology data
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944]
ChEMBL Antagonist activity at rat Alpha-1D adrenoceptor assessed as inhibition if norepenephrine-induced contraction of thoracic aorta F 8.97 pKd 1.07 nM Kd J. Med. Chem. (2009) 52: 4951-4954 [PMID:19719240]
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL Binding affinity against Alpha-2A adrenergic receptor, from human clones. B 6.14 pKi 729 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
ChEMBL Binding affinity against Alpha-2B adrenergic receptor from human clones. B 5.3 pKi >5000 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
ChEMBL Binding affinity against Alpha-2C adrenergic receptor from human clones. B 6.55 pKi 280 nM Ki J. Med. Chem. (1995) 38: 3415-3444 [PMID:7658428]
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 5.72 pKi 1889 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177) B 5.56 pIC50 2748 nM IC50 DrugMatrix in vitro pharmacology data
DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
ChEMBL DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) B 6.83 pKi 149 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) B 6.73 pIC50 188 nM IC50 DrugMatrix in vitro pharmacology data
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) B 5.74 pKi 1815.1 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) B 5.65 pIC50 2215.5 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Inhibition of human ERG B 6.23 pIC50 588.84 nM IC50 Eur. J. Med. Chem. (2011) 46: 618-630 [PMID:21185626]
MMP1/Matrix metalloproteinase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL332] [GtoPdb: 1628] [UniProtKB: P03956]
ChEMBL DRUGMATRIX: Peptidase, Matrix Metalloprotease-1 (MMP-1) enzyme inhibition (substrate: Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2) B 5.24 pIC50 5749 nM IC50 DrugMatrix in vitro pharmacology data
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 6.63 pKi 234 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 6.43 pIC50 368 nM IC50 DrugMatrix in vitro pharmacology data
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 6.55 pKi 285 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 6.26 pIC50 544 nM IC50 DrugMatrix in vitro pharmacology data
Serotonin 4 (5-HT4) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5017] [UniProtKB: O70528]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808) B 6.9 pKi 127 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808) B 6.12 pIC50 764 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 5.85 pKi 1428 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) B 5.57 pIC50 2688 nM IC50 DrugMatrix in vitro pharmacology data

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]