guanfacine [Ligand Id: 522] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL862 (Guanfacina, Guanfacine, Intuniv, NSC-759121) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 5-HT2A receptor/5-hydroxytryptamine receptor 2A 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/5-hydroxytryptamine receptor 2B 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/5-hydroxytryptamine receptor 2C 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 |
| α1A-adrenoceptor/Alpha-1A adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348] | ||||||||
| ChEMBL | Binding affinity to human alpha1A-adrenoceptor | B | 5.33 | pKi | 4677.35 | nM | Ki | J Med Chem (2024) 67: 11435-11449 [PMID:38889119] |
| 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 |
| α1D-adrenoceptor/Alpha-1D adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100] | ||||||||
| ChEMBL | Binding affinity to human alpha1D-adrenoceptor | B | 4.93 | pKi | 11748.98 | nM | Ki | J Med Chem (2024) 67: 11435-11449 [PMID:38889119] |
| 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] |
| ChEMBL | Agonist activity at human alpha2A-adrenoceptor expressed in HEK293 cells assessed as forskolin-stimulated intracellular cAMP accumulation incubated for 15 mins by Scintillation proximity assay | F | 7.28 | pEC50 | 52.48 | nM | EC50 | J Med Chem (2024) 67: 11435-11449 [PMID:38889119] |
| 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] |
| ChEMBL | Agonist activity at human alpha2B-adrenoceptor expressed in HEK293 cells assessed as forskolin-stimulated intracellular cAMP accumulation incubated for 15 mins by Scintillation proximity assay | F | 6.54 | pEC50 | 288.4 | nM | EC50 | J Med Chem (2024) 67: 11435-11449 [PMID:38889119] |
| 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] |
| ChEMBL | Agonist activity at human alpha2C-adrenoceptor expressed in HEK293 cells assessed as forskolin-stimulated intracellular cAMP accumulation incubated for 15 mins by Scintillation proximity assay | F | 6.22 | pEC50 | 602.56 | nM | EC50 | J Med Chem (2024) 67: 11435-11449 [PMID:38889119] |
| 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] |
ChEMBL data shown on this page come from version 36:
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]
