[3H]aldosterone [Ligand Id: 3452] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL273453 (Aldosterone, NSC-73856) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Androgen receptor/Androgen Receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207] | ||||||||
| ChEMBL | Inhibitory concentration against recombinant rat androgen receptor expressed in Escherichia coli using [3H]methyltrienolone (R 1881) | B | 4.37 | pIC50 | >42657.95 | nM | IC50 | J Med Chem (2005) 48: 5666-5674 [PMID:16134935] |
| Corticosteroid binding globulin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2421] [UniProtKB: P08185] | ||||||||
| ChEMBL | Binding affinity to human CBG receptor (corticosteroid-binding globulins) | B | 6.28 | pKi | 524.81 | nM | Ki | J Med Chem (2004) 47: 2732-2742 [PMID:15139751] |
| Mineralocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1994] [GtoPdb: 626] [UniProtKB: P08235] | ||||||||
| ChEMBL | Binding affinity to MR (unknown origin) | B | 9.3 | pKd | 0.5 | nM | Kd | J Med Chem (2017) 60: 2629-2650 [PMID:28051871] |
| ChEMBL | Antagonist activity at mineralocorticoid receptor-LBD in human U2OS cells transfected with Gal4-DBD assessed as inhibition of transactivation activity after 18 hrs by luciferase reporter gene assay | F | 8.03 | pIC50 | 9.27 | nM | IC50 | J Med Chem (2010) 53: 6947-6953 [PMID:20812681] |
| ChEMBL | Agonist activity at GAL4 DNA-binding domain fused MR (unknown origin) ligand binding domain expressed in UAS-bla H cells assessed as beta-lactamase transcriptional activation by FRET-based GeneBLAzer assay | B | 9.52 | pIC50 | 0.3 | nM | IC50 | Eur J Med Chem (2018) 157: 791-804 [PMID:30144697] |
| ChEMBL | Agonist activity at mineralocorticoid receptor ligand binding domain expressed in african green monkey COS7 cells co-transfected with Gal4-LBD by luciferase reporter gene assay | B | 8.42 | pEC50 | 3.8 | nM | EC50 | J Nat Prod (2009) 72: 1944-1948 [PMID:19863083] |
| ChEMBL | Agonist activity at MR (unknown origin) by Alpha Screen assay | B | 8.89 | pEC50 | 1.3 | nM | EC50 | Medchemcomm (2019) 10: 1412-1419 [PMID:31673308] |
| ChEMBL | Agonist activity at mineralocorticoid receptor-LBD in human U2OS cells transfected with Gal4-DBD assessed as increase of transactivation activity after 18 hrs by luciferase reporter gene assay | F | 9.47 | pEC50 | 0.34 | nM | EC50 | J Med Chem (2010) 53: 6947-6953 [PMID:20812681] |
| ChEMBL | Agonist activity at human MCR expressed in HEK293 cells by luciferase reporter gene assay | B | 9.74 | pEC50 | 0.18 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 5265-5267 [PMID:25305688] |
| Mineralocorticoid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3507] [GtoPdb: 626] [UniProtKB: P22199] | ||||||||
| GtoPdb | - | - | 9.52 | pKd | 0.3 | nM | Kd |
Am J Physiol (1984) 246: F227-33 [PMID:6320679]; Mol Cell Endocrinol (2005) 243: 35-42 [PMID:16188378] |
| ChEMBL | Displacement of [3H]aldosterone from Sprague-Dawley rat MR by liquid scintillation counting | B | 7.37 | pIC50 | 43 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1744-1747 [PMID:21349712] |
| ChEMBL | Displacement of [3H]Aldo from mineralocorticoid receptor in Sprague-Dawley rat kidney after 2 hrs by liquid scintillation counting | B | 7.37 | pIC50 | 43 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6310-6313 [PMID:21944856] |
| Testis-specific androgen-binding protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3305] [UniProtKB: P04278] | ||||||||
| ChEMBL | Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | B | 5.32 | pKd | 4786.3 | nM | Kd | J Med Chem (2008) 51: 2047-2056 [PMID:18330978] |
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]
