glycyrrhizin [Ligand Id: 4688] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL441687 (18.beta.-glycyrrhizic acid, .beta.-glycyrrhizin, E958, Glycyron, Glycyrrhetinic acid, Glycyrrhizate, Glycyrrhizic acid, Glycyrrhizic Acid, Glycyrrhizin, Glycyrrhizinate, Glycyrrhizinic acid, NSC-167409, NSC-234419, Potenlini)
  • hydroxysteroid 11-beta dehydrogenase 1/11-beta-hydroxysteroid dehydrogenase 1 in Human [ChEMBL: CHEMBL4235] [GtoPdb: 2763] [UniProtKB: P28845]
  • hydroxysteroid 11-beta dehydrogenase 1/11-beta-hydroxysteroid dehydrogenase 1 in Mouse [ChEMBL: CHEMBL3910] [GtoPdb: 2763] [UniProtKB: P50172]
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  • hydroxysteroid 11-beta dehydrogenase 2/11-beta-hydroxysteroid dehydrogenase 2 in Human [ChEMBL: CHEMBL3746] [GtoPdb: 3143] [UniProtKB: P80365]
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  • ABCC2/Canalicular multispecific organic anion transporter 1 in Rat [ChEMBL: CHEMBL2073676] [GtoPdb: 780] [UniProtKB: Q63120]
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  • protein tyrosine phosphatase non-receptor type 1/Protein-tyrosine phosphatase 1B in Human [ChEMBL: CHEMBL335] [GtoPdb: 2976] [UniProtKB: P18031]
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  • OATP1B1/Solute carrier organic anion transporter family member 1B1 in Human [ChEMBL: CHEMBL1697668] [GtoPdb: 1220] [UniProtKB: Q9Y6L6]
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  • Solute carrier organic anion transporter family member 1B2 in Rat [ChEMBL: CHEMBL1781861] [UniProtKB: Q9QZX8]
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  • OATP1B3/Solute carrier organic anion transporter family member 1B3 in Human [ChEMBL: CHEMBL1743121] [GtoPdb: 1221] [UniProtKB: Q9NPD5]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
hydroxysteroid 11-beta dehydrogenase 1/11-beta-hydroxysteroid dehydrogenase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4235] [GtoPdb: 2763] [UniProtKB: P28845]
ChEMBL Inhibition of human 11beta-HSD1 expressed in human HEK293 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay B 7.73 pIC50 18.6 nM IC50 J Nat Prod (2011) 74: 2571-2575 [PMID:22148241]
ChEMBL Inhibition of human microsomal 11beta-HSD1 expressed in HEK293 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay B 8 pIC50 10 nM IC50 Bioorg Med Chem Lett (2009) 19: 4455-4458 [PMID:19564108]
ChEMBL Inhibition of human 11beta-HSD1 expressed in HEK293 cells assessed as conversion of [3H]cortisone into [3H]cortisol by scintillation proximity assay B 8.22 pIC50 6 nM IC50 J Nat Prod (2012) 75: 599-604 [PMID:22360639]
ChEMBL Inhibition of human 11beta-HSD1 expressed in HEK293 cells assessed as [3H]cortisol production after 60 mins by SPA B 8 pEC50 10 nM EC50 Bioorg Med Chem Lett (2012) 22: 2748-2752 [PMID:22440625]
hydroxysteroid 11-beta dehydrogenase 1/11-beta-hydroxysteroid dehydrogenase 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3910] [GtoPdb: 2763] [UniProtKB: P50172]
ChEMBL Inhibition of mouse 11beta-HSD1 expressed in human HEK293 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay B 7.53 pIC50 29.5 nM IC50 J Nat Prod (2011) 74: 2571-2575 [PMID:22148241]
ChEMBL Inhibition of mouse liver microsome 11betaHSD1 expressed in HEK293 cells assessed as conversion of [3H]cortisone into [3H]cortisol by scintillation proximity assay B 7.82 pIC50 15 nM IC50 Bioorg Med Chem (2009) 17: 5722-5732 [PMID:19574056]
ChEMBL Inhibition of mouse microsomal 11beta-HSD1 expressed in HEK293 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay B 8.1 pIC50 8 nM IC50 Bioorg Med Chem Lett (2009) 19: 4455-4458 [PMID:19564108]
ChEMBL Inhibition of mouse 11beta-HSD1 expressed in HEK293 cells assessed as conversion of [3H]cortisone into [3H]cortisol by scintillation proximity assay B 8.52 pIC50 3 nM IC50 J Nat Prod (2012) 75: 599-604 [PMID:22360639]
ChEMBL Inhibition of mouse 11beta-HSD1 expressed in HEK293 cells assessed as [3H]cortisol production after 60 mins by SPA B 8.1 pEC50 8 nM EC50 Bioorg Med Chem Lett (2012) 22: 2748-2752 [PMID:22440625]
hydroxysteroid 11-beta dehydrogenase 2/11-beta-hydroxysteroid dehydrogenase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3746] [GtoPdb: 3143] [UniProtKB: P80365]
ChEMBL Inhibition of human microsomal 11beta-HSD2 expressed in HEK293 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay B 9 pIC50 1 nM IC50 Bioorg Med Chem Lett (2009) 19: 4455-4458 [PMID:19564108]
ChEMBL Inhibition of human 11beta-HSD2 expressed in human HEK293 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay B 9.15 pIC50 0.7 nM IC50 J Nat Prod (2011) 74: 2571-2575 [PMID:22148241]
ChEMBL Inhibition of human 11beta-HSD2 expressed in HEK293 cells assessed as conversion of [3H]cortisone into [3H]cortisol by scintillation proximity assay B 9.4 pIC50 0.4 nM IC50 J Nat Prod (2012) 75: 599-604 [PMID:22360639]
ChEMBL Inhibition of human 11beta-HSD2 expressed in HEK293 cells assessed as [3H]cortisol production after 60 mins by SPA B 9 pEC50 1 nM EC50 Bioorg Med Chem Lett (2012) 22: 2748-2752 [PMID:22440625]
Beta-glucuronidase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4814] [UniProtKB: P06760]
ChEMBL Inhibition of rat liver beta-glucuronidase B 4.01 pIC50 97210 nM IC50 Eur J Med Chem (2020) 187: 111921-111921 [PMID:31835168]
Beta-glucuronidase in Escherichia coli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3217380] [UniProtKB: P05804]
ChEMBL Inhibition of Escherichia coli beta-glucuronidase B 4.92 pIC50 12150 nM IC50 Eur J Med Chem (2020) 187: 111921-111921 [PMID:31835168]
ABCC2/Canalicular multispecific organic anion transporter 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073676] [GtoPdb: 780] [UniProtKB: Q63120]
ChEMBL TP_TRANSPORTER: inhibition of SN-38 uptake in bile canalicular membrane vesicles from SD rat F 5.72 pKi 1910 nM Ki Drug Metabol Pharmacokin (2002) 17: 23-33 [PMID:15618649]
ChEMBL TP_TRANSPORTER: inhibition of DNP-SG uptake in bile canalicular membrane vesicles from SD rat F 6.08 pKi 840 nM Ki Drug Metabol Pharmacokin (2002) 17: 23-33 [PMID:15618649]
High mobility group protein B1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2311236] [UniProtKB: P09429]
ChEMBL Binding affinity to recombinant HMGB1 B box region (90 to 175 residues) (unknown origin) expressed Escherichia coli after 5 mins by fluorescence-based assay B 4.06 pKd 87000 nM Kd J Med Chem (2018) 61: 5093-5107 [PMID:29268019]
protein tyrosine phosphatase non-receptor type 1/Protein-tyrosine phosphatase 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL335] [GtoPdb: 2976] [UniProtKB: P18031]
ChEMBL Inhibition of human recombinant PTP1B B 4 pIC50 >100000 nM IC50 Bioorg Med Chem Lett (2006) 16: 3273-3276 [PMID:16580200]
OATP1B1/Solute carrier organic anion transporter family member 1B1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1697668] [GtoPdb: 1220] [UniProtKB: Q9Y6L6]
ChEMBL TP_TRANSPORTER: inhibition of E1S uptake in Xenopus laevis oocytes F 4.8 pKi 15900 nM Ki Hepatol Res (2003) 26: 343-347 [PMID:12963436]
Solute carrier organic anion transporter family member 1B2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1781861] [UniProtKB: Q9QZX8]
ChEMBL TP_TRANSPORTER: inhibition of E1S uptake in Xenopus laevis oocytes F 5.21 pKi 6100 nM Ki Hepatol Res (2003) 26: 343-347 [PMID:12963436]
OATP1B3/Solute carrier organic anion transporter family member 1B3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743121] [GtoPdb: 1221] [UniProtKB: Q9NPD5]
ChEMBL TP_TRANSPORTER: inhibition of BSP uptake in Xenopus laevis oocytes F 4.9 pKi 12500 nM Ki Hepatol Res (2003) 26: 343-347 [PMID:12963436]

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]