guanabenz [Ligand Id: 5443] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1331786
  • α2A-adrenoceptor in Human [GtoPdb: 25] [UniProtKB: P08913]
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  • α2B-adrenoceptor in Human [GtoPdb: 26] [UniProtKB: P18089]
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  • α2C-adrenoceptor in Human [GtoPdb: 27] [UniProtKB: P18825]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
α2A-adrenoceptor in Human [GtoPdb: 25] [UniProtKB: P08913]
GtoPdb - - 7.7 pKi - - - Biochem Pharmacol (1998) 55: 1035-43 [PMID:9605427];
Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495]
GtoPdb - - 7.4 pIC50 41 nM IC50 National Toxicology Program: Dept of Health and Human Services.. DrugMatrix;
Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495]
GtoPdb inhibition of forskolin stimulated cAMP generation - 8.4 pIC50 - - - National Toxicology Program: Dept of Health and Human Services.. DrugMatrix;
Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495]
GtoPdb GTPγs binding - 8.3 pEC50 - - - Biochem Pharmacol (1998) 55: 1035-43 [PMID:9605427]
GtoPdb increased ERK1/2 phosphorylation - 9.1 pEC50 - - - Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495]
α2B-adrenoceptor in Human [GtoPdb: 26] [UniProtKB: P18089]
GtoPdb - - 6 pKi - - - Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495]
GtoPdb inhibition of forskolin stimulated cAMP generation - 9 pIC50 - - - Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495]
GtoPdb cAMP generation - 7.9 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 in Human [GtoPdb: 27] [UniProtKB: P18825]
GtoPdb - - 6.4 pKd - - - Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495]
GtoPdb inhibition of cAMP production - 7.9 pIC50 1106 nM IC50 National Toxicology Program: Dept of Health and Human Services.. DrugMatrix;
Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495];
Brain Res Bull (2014) 107: 89-101 [PMID:25080296]
GtoPdb 5.14 =value for β-arrestin recruitment and internalization - 6.57 pEC50 - - - Brain Res Bull (2014) 107: 89-101 [PMID:25080296]
GtoPdb ERK1/2 phosphorylation - 8.4 pEC50 - - - Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495]

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]