doxazosin [Ligand Id: 7170] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL707 (C02CA04, Cardura, Doxazosin, UK-33274) |
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| 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; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144]; J Pharmacol Exp Ther (2019) 371: 106-112 [PMID:31285236] |
| 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; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144] |
| 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; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144] |
| 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
