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 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]