guanfacine [Ligand Id: 522] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL862 (Guanfacine, Intuniv, NSC-759121, Tenex) |
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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 Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140] | ||||||||
| ChEMBL | DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) | B | 6.26 | pKi | 546 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) | B | 5.87 | pIC50 | 1348 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
| GtoPdb | - | - | 7.3 | pKi | - | - | - |
Biochem Pharmacol (1998) 55: 1035-43 [PMID:9605427]; Br J Pharmacol (1997) 121: 1721-9 [PMID:9283709]; Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| ChEMBL | DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) | B | 7.3 | pKi | 50 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) | B | 6.87 | pIC50 | 134 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| GtoPdb | inhibition of forskolin stimulated cAMP generation | - | 8 | pIC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| GtoPdb | increased cAMP generation | - | 6.5 | pEC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| GtoPdb | GTPγs binding | - | 7.3 | pEC50 | - | - | - | Biochem Pharmacol (1998) 55: 1035-43 [PMID:9605427] |
| GtoPdb | increased ERK1/2 phosphorylation | - | 9 | pEC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089] | ||||||||
| GtoPdb | - | - | 6.5 | pKi | - | - | - |
Biochem Pharmacol (1998) 55: 1035-43 [PMID:9605427]; Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| ChEMBL | DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) | B | 6.94 | pKi | 114 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) | B | 6.6 | pIC50 | 249 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| GtoPdb | inhibition of forskolin stimulated cAMP generation | - | 8.7 | pIC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| GtoPdb | cAMP generation | - | 7.6 | pEC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| GtoPdb | ERK1/2 phosphorylation | - | 8.5 | pEC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] | ||||||||
| ChEMBL | DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) | B | 6.03 | pKi | 937 | nM | Ki | DrugMatrix in vitro pharmacology data |
| GtoPdb | - | - | 6.2 | pKi | - | - | - |
Biochem Pharmacol (1998) 55: 1035-43 [PMID:9605427]; Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| ChEMBL | DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) | B | 5.19 | pIC50 | 6447 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| GtoPdb | inhibition of cAMP production | - | 7.2 | pIC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| GtoPdb | ERK1/2 phosphorylation | - | 8 | pEC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| 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 | 7.72 | pKi | 19.01 | 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 | 6.06 | pKi | 861 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) | B | 5.52 | pIC50 | 3014 | 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 | 5.87 | pKi | 1335 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 5.68 | pIC50 | 2098 | 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 | 6.12 | pKi | 761 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) | B | 5.84 | pIC50 | 1453 | 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]
