idazoxan [Ligand Id: 12575] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL10316 (Dl-idazoxan, Idazoxan, NSC-759867, Racemic idazoxan, RX-781094) |
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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 | Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement. | B | 5.54 | pIC50 | 2884.03 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 71-74 [PMID:10636247] |
| Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130] | ||||||||
| ChEMBL | Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand | B | 6.3 | pKi | 500 | nM | Ki | J Med Chem (1983) 26: 1696-1701 [PMID:6139479] |
| α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
| GtoPdb | - | - | 7.2 | pKi | - | - | - | Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877] |
| ChEMBL | Displacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cells | B | 8.1 | pKi | 8 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 1616-1621 [PMID:17257841] |
| ChEMBL | Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2A receptor expressed in CHO cells | B | 8.15 | pKi | 7.08 | nM | Ki | J Med Chem (2008) 51: 4289-4299 [PMID:18578476] |
| ChEMBL | Displacement of [3H]RX821002 from human alpha2A adrenergic receptor expressed in CHO cells after 30 mins by scintillation counting | B | 8.15 | pKi | 7.08 | nM | Ki | Bioorg Med Chem (2012) 20: 2259-2265 [PMID:22370341] |
| ChEMBL | Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement. | B | 8.08 | pIC50 | 8.32 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 71-74 [PMID:10636247] |
| Alpha-2a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4744] [UniProtKB: Q28838] | ||||||||
| ChEMBL | Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand | B | 8.82 | pKi | 1.5 | nM | Ki | J Med Chem (1983) 26: 1696-1701 [PMID:6139479] |
| α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089] | ||||||||
| GtoPdb | - | - | 6.4 | pKi | - | - | - | Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877] |
| ChEMBL | Displacement of [3H]MK912 from adrenergic alpha-2B receptor expressed in COS7 cells | B | 7 | pKi | 100 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 1616-1621 [PMID:17257841] |
| ChEMBL | Displacement of [3H]RS79948-197 from human recombinant adrenergic alpha2B receptor expressed in CHO cells | B | 7.64 | pKi | 22.91 | nM | Ki | J Med Chem (2008) 51: 4289-4299 [PMID:18578476] |
| ChEMBL | Displacement of [3H]RX821002 from human alpha2B adrenergic receptor expressed in CHO cells after 30 mins by scintillation counting | B | 7.64 | pKi | 22.91 | nM | Ki | Bioorg Med Chem (2012) 20: 2259-2265 [PMID:22370341] |
| ChEMBL | Binding affinity at human Alpha-2B adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement. | B | 7.71 | pIC50 | 19.5 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 71-74 [PMID:10636247] |
| α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] | ||||||||
| GtoPdb | - | - | 7.2 | pKi | - | - | - | Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877] |
| ChEMBL | Displacement of [3H]MK912 from adrenergic Alpha-2C receptor in HepG2 cells | B | 7.72 | pKi | 19 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 1616-1621 [PMID:17257841] |
| ChEMBL | Displacement of [3H]RS79948-197 from human recombinant adrenergic Alpha-2C receptor expressed in CHO cells | B | 7.75 | pKi | 17.78 | nM | Ki | J Med Chem (2008) 51: 4289-4299 [PMID:18578476] |
| ChEMBL | Displacement of [3H]RX821002 from human Alpha-2C adrenergic receptor expressed in CHO cells after 30 mins by scintillation counting | B | 7.75 | pKi | 17.78 | nM | Ki | Bioorg Med Chem (2012) 20: 2259-2265 [PMID:22370341] |
| ChEMBL | Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement. | B | 7.27 | pIC50 | 53.7 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 71-74 [PMID:10636247] |
| D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
| ChEMBL | In vitro inhibition of specific binding of [3H]-YM 09151-2 to Dopamine receptor D2 site in rat striatal tissue. | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2000) 43: 3653-3664 [PMID:11020279] |
| Monoamine oxidase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1951] [GtoPdb: 2489] [UniProtKB: P21397] | ||||||||
| ChEMBL | Activity Assay: Inhibitory activity of compounds was evaluated by a homogeneous luminescent method, the MAO-Glo Assay (Promega), measuring the monoamine oxidase activity (MAOs) from recombinant source (microsomes from baculovirus infected insect cells, Sigma). Experiments were performed according to the Supplier's procedure, incubating human recombinant MAO-A or MAO-B with a luminogenic substrate, a derivative of beetle luciferin ((4S)-4,5-dihydro-2-(6-hydroxybenzothiazolyl)-4-thiazolecarboxylic acid). MAOs converts this luciferin derivative to methyl ester luciferin and only compounds that interfere with the ability of the enzyme to use the pro-luminescent substrate will cause changes in the resulting luminescent signal. | B | 6 | pIC50 | 1000 | nM | IC50 | US-8633208-B2. 6-1H-imidazo-quinazoline and quinolines derivatives, new MAO inhibitors and imidazoline receptor ligands (2014) |
| Monoamine oxidase B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2039] [GtoPdb: 2490] [UniProtKB: P27338] | ||||||||
| ChEMBL | Activity Assay: Inhibitory activity of compounds was evaluated by a homogeneous luminescent method, the MAO-Glo Assay (Promega), measuring the monoamine oxidase activity (MAOs) from recombinant source (microsomes from baculovirus infected insect cells, Sigma). Experiments were performed according to the Supplier's procedure, incubating human recombinant MAO-A or MAO-B with a luminogenic substrate, a derivative of beetle luciferin ((4S)-4,5-dihydro-2-(6-hydroxybenzothiazolyl)-4-thiazolecarboxylic acid). MAOs converts this luciferin derivative to methyl ester luciferin and only compounds that interfere with the ability of the enzyme to use the pro-luminescent substrate will cause changes in the resulting luminescent signal. | B | 6 | pIC50 | 1000 | nM | IC50 | US-8633208-B2. 6-1H-imidazo-quinazoline and quinolines derivatives, new MAO inhibitors and imidazoline receptor ligands (2014) |
| 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 | 5.9 | pKi | 1256.03 | 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 | 5.9 | pKi | 1255 | nM | Ki | Bioorg Med Chem (2008) 16: 7134-7140 [PMID:18621536] |
| ChEMBL | Binding affinity for imidazoline receptor I-1 | B | 6.52 | pKi | 300 | nM | Ki | J Med Chem (1995) 38: 3681-3716 [PMID:7562902] |
| ChEMBL | Binding affinity for imidazoline receptor I-2 in rabbit kidney homogenate (relative to [3H]-Idazoxan radioligand) | B | 8.1 | pKi | 7.94 | nM | Ki | J Med Chem (2000) 43: 1109-1122 [PMID:10737743] |
| Nischarin in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5221] [UniProtKB: Q4G017] | ||||||||
| ChEMBL | Displacement of [125I]PIC from Imidazoline-1 receptor in rat PC12 cell membrane by gamma counting method | B | 5.9 | pKi | 1258.93 | nM | Ki | Bioorg Med Chem (2016) 24: 3174-3183 [PMID:27265687] |
| NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] | ||||||||
| ChEMBL | Inhibitory activity against norepinephrine (NE) uptake in rat whole brain synaptosome preparation | F | 4.7 | pIC50 | >20000 | nM | IC50 | J Med Chem (1996) 39: 570-581 [PMID:8558529] |
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]
