phentolamine [Ligand Id: 502] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL597 (Fentolamina, Phentolamin, Phentolamine) |
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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 | Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor | B | 7.49 | pKd | 32.36 | nM | Kd | J Med Chem (1984) 27: 495-503 [PMID:6142954] |
| ChEMBL | Displacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method | B | 7.92 | pKi | 12 | nM | Ki | Bioorg Med Chem Lett (2018) 28: 2039-2049 [PMID:29730027] |
| ChEMBL | Binding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cells | B | 8.39 | pKi | 4.12 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4691-4695 [PMID:16153828] |
| GtoPdb | - | - | 8.6 | pKi | - | - | - |
Mol Pharmacol (1995) 48: 250-8 [PMID:7651358]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144] |
| ChEMBL | Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis | B | 9.22 | pKi | 0.6 | nM | Ki | ACS Med Chem Lett (2015) 6: 502-506 [PMID:26005522] |
| ChEMBL | Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis | B | 8.96 | pIC50 | 1.1 | nM | IC50 | ACS Med Chem Lett (2015) 6: 502-506 [PMID:26005522] |
| Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130] | ||||||||
| ChEMBL | Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells | B | 8.17 | pKi | 6.8 | nM | Ki | J Med Chem (2003) 46: 265-283 [PMID:12519065] |
| ChEMBL | In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor | B | 9.1 | pKi | 0.79 | nM | Ki | J Med Chem (1997) 40: 2674-2687 [PMID:9276013] |
| Alpha-1a adrenergic receptor in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3637] [UniProtKB: O02824] | ||||||||
| ChEMBL | Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay | F | 8.2 | pKd | 6.31 | nM | Kd | J Med Chem (1997) 40: 2674-2687 [PMID:9276013] |
| α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140] | ||||||||
| GtoPdb | - | - | 8.1 | pKi | - | - | - | J Biol Chem (2001) 276: 25366-71 [PMID:11331292] |
| ChEMBL | DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) | B | 8.33 | pKi | 4.66 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) | B | 7.96 | pIC50 | 11 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368] | ||||||||
| ChEMBL | Binding affinity towards human alpha-1B adrenergic receptor expressed in Chinese Hamster ovary (CHO) cells | B | 7.32 | pKi | 47.4 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4691-4695 [PMID:16153828] |
| GtoPdb | - | - | 7.5 | pKi | - | - | - |
Mol Pharmacol (1995) 48: 250-8 [PMID:7651358]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144] |
| ChEMBL | Displacement of [3H]-Prazosin from human alpha-1B adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis | B | 8.32 | pKi | 4.8 | nM | Ki | ACS Med Chem Lett (2015) 6: 502-506 [PMID:26005522] |
| ChEMBL | Displacement of [3H]-Prazosin from human alpha-1B adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis | B | 7.97 | pIC50 | 10.8 | nM | IC50 | ACS Med Chem Lett (2015) 6: 502-506 [PMID:26005522] |
| Alpha-1b adrenergic receptor in Hamster (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3122] [UniProtKB: P18841] | ||||||||
| ChEMBL | Displacement of [3H]prazosin (0.5 nM) from hamster Alpha-1B adrenergic receptor expressed in rat-1 cells | B | 6.66 | pKi | 220 | nM | Ki | J Med Chem (2003) 46: 265-283 [PMID:12519065] |
| α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823] | ||||||||
| ChEMBL | DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) | B | 7.35 | pKi | 45 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) | B | 7.09 | pIC50 | 82 | 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 towards human alpha-1D adrenergic receptor expressed in Chinese Hamster ovary (CHO) cells | B | 7.71 | pKi | 19.4 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4691-4695 [PMID:16153828] |
| ChEMBL | DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) | B | 7.96 | pKi | 11 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | Displacement of [3H]-Prazosin from human alpha-1D adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis | B | 8.12 | pKi | 7.6 | nM | Ki | ACS Med Chem Lett (2015) 6: 502-506 [PMID:26005522] |
| GtoPdb | - | - | 8.2 | pKi | - | - | - |
Mol Pharmacol (1995) 48: 250-8 [PMID:7651358]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144] |
| ChEMBL | DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) | B | 7.66 | pIC50 | 22 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| ChEMBL | Displacement of [3H]-Prazosin from human alpha-1D adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis | B | 7.9 | pIC50 | 12.5 | nM | IC50 | ACS Med Chem Lett (2015) 6: 502-506 [PMID:26005522] |
| α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944] | ||||||||
| ChEMBL | Displacement of [3H]prazosin (0.3 nM) from rat Alpha-1D adrenergic receptor expressed in CHO cells | B | 7.35 | pKi | 45 | nM | Ki | J Med Chem (2003) 46: 265-283 [PMID:12519065] |
| α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
| ChEMBL | Binding affinity towards human alpha-2A adrenergic receptor expressed in Chinese Hamster ovary (CHO) cells | B | 7.25 | pKi | 55.9 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4691-4695 [PMID:16153828] |
| GtoPdb | - | - | 8.4 | pKi | - | - | - |
Mol Pharmacol (1992) 42: 1-5 [PMID:1353247]; Eur J Pharmacol (1994) 252: 43-9 [PMID:7908642]; Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877] |
| ChEMBL | The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones. | B | 8.59 | pKi | 2.6 | nM | Ki | J Med Chem (1995) 38: 3415-3444 [PMID:7658428] |
| ChEMBL | DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) | B | 8.65 | pKi | 2.25 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | Displacement of [3H]RX781094 from alpha2 adrenergic receptor | B | 8.77 | pKi | 1.7 | nM | Ki | J Nat Prod (1993) 56: 441-455 [PMID:8496700] |
| ChEMBL | DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) | B | 8.22 | pIC50 | 6 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| GtoPdb | increased cAMP generation | - | 7.1 | pEC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| Alpha-2a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4744] [UniProtKB: Q28838] | ||||||||
| ChEMBL | Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligand | B | 8.68 | pKi | 2.1 | nM | Ki | J Med Chem (1983) 26: 1769-1772 [PMID:6139481] |
| ChEMBL | Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand | B | 9.03 | pKi | 0.93 | nM | Ki | J Med Chem (1983) 26: 1769-1772 [PMID:6139481] |
| α2A-adrenoceptor/Alpha-2a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL327] [GtoPdb: 25] [UniProtKB: P22909] | ||||||||
| ChEMBL | The compound was tested for binding affinity against alpha-2D adrenergic receptor, from rat clones. | B | 8.33 | pKi | 4.7 | 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 towards human alpha-2B adrenergic receptor expressed in Chinese Hamster ovary (CHO) cells | B | 7.32 | pKi | 48 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4691-4695 [PMID:16153828] |
| ChEMBL | DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) | B | 8.08 | pKi | 8.23 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | Binding affinity against Alpha-2B adrenergic receptor from human clones. | B | 8.12 | pKi | 7.6 | nM | Ki | J Med Chem (1995) 38: 3415-3444 [PMID:7658428] |
| GtoPdb | - | - | 8.2 | pKi | - | - | - |
Mol Pharmacol (1992) 42: 1-5 [PMID:1353247]; Eur J Pharmacol (1994) 252: 43-9 [PMID:7908642]; Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877] |
| ChEMBL | DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) | B | 7.74 | pIC50 | 18 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] | ||||||||
| ChEMBL | Binding affinity towards human alpha-2C adrenergic receptor expressed in Chinese Hamster ovary (CHO) cells | B | 7.1 | pKi | 80.3 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4691-4695 [PMID:16153828] |
| ChEMBL | DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) | B | 7.8 | pKi | 16 | nM | Ki | DrugMatrix in vitro pharmacology data |
| GtoPdb | - | - | 7.9 | pKi | - | - | - |
Mol Pharmacol (1992) 42: 1-5 [PMID:1353247]; Eur J Pharmacol (1994) 252: 43-9 [PMID:7908642]; Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877] |
| ChEMBL | Binding affinity against Alpha-2C adrenergic receptor from human clones. | B | 8.08 | pKi | 8.4 | nM | Ki | J Med Chem (1995) 38: 3415-3444 [PMID:7658428] |
| ChEMBL | DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) | B | 6.96 | pIC50 | 110 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| CYP2D6/Cytochrome P450 2D6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL289] [GtoPdb: 1329] [UniProtKB: P10635] | ||||||||
| ChEMBL | DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) | B | 5 | pIC50 | 10000 | 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 | 4.78 | pKi | 16448 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) | B | 4.7 | pIC50 | 20076.3 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| H1 receptor/Histamine H1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390] | ||||||||
| ChEMBL | Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting | B | 4.9 | pIC50 | 12589.25 | nM | IC50 | J Med Chem (2012) 55: 7054-7060 [PMID:22793499] |
| Nischarin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3923] [UniProtKB: Q9Y2I1] | ||||||||
| ChEMBL | Displacement of [125I]PIC from human imidazoline receptor 1 in human platelets analyzed under norepinephrine mask of alpha 2AR | B | 7.94 | pKi | 11.4 | nM | Ki | Bioorg Med Chem (2008) 16: 7134-7140 [PMID:18621536] |
| ChEMBL | Displacement of [125I]PIC from human imidazoline receptor 1 in human platelets analyzed under norepinephrine mask of alpha 2AR | B | 7.94 | pKi | 11.4 | nM | Ki | Bioorg Med Chem (2008) 16: 7134-7140 [PMID:18621536] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) | B | 6.99 | pKi | 103 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) | B | 6.44 | pIC50 | 359 | 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 | 5.62 | pKi | 2422 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 5.42 | pIC50 | 3807 | 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 | 6.68 | pKi | 207 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) | B | 6.4 | pIC50 | 396 | 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 | The compound was tested for affinity towards sigma-3 receptor | B | 6.26 | pIC50 | 549.54 | nM | IC50 | J Med Chem (1994) 37: 4109-4117 [PMID:7990111] |
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]
