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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 |
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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 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]