guanfacine [Ligand Id: 522] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL862 (Guanfacina, Guanfacine, Intuniv, NSC-759121, Tenex)
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
Created with Highcharts 10.3.3ValuesChart context menuAlpha-1a adrenergic receptorpKd RatpKi RatpIC50 RatpEC50 Rat01234567Highcharts.com
  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
Created with Highcharts 10.3.3ValuesChart context menuAlpha-2a adrenergic receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human0246810Highcharts.com
  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
Created with Highcharts 10.3.3ValuesChart context menuAlpha-2b adrenergic receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human0246810Highcharts.com
  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
Created with Highcharts 10.3.3ValuesChart context menuAlpha-2c adrenergic receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human0246810Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuNischarinpKd HumanpKi HumanpIC50 HumanpEC50 Human0246810Highcharts.com
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
Created with Highcharts 10.3.3ValuesChart context menuSerotonin 2a (5-HT2a) receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human01234567Highcharts.com
  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
Created with Highcharts 10.3.3ValuesChart context menuSerotonin 2b (5-HT2b) receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human01234567Highcharts.com
  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
Created with Highcharts 10.3.3ValuesChart context menuSerotonin 2c (5-HT2c) receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human01234567Highcharts.com
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 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]