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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 |
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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] |
GtoPdb | - | - | 10 | pIC50 | - | - | - |
Eur J Pharmacol (1993) 247: 145-54 [PMID:8282004]; FEBS Lett (1999) 464: 9-13 [PMID:10611474] |
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 human MR expressed in CHO-K1 cells by PathHunter assay | B | 9.22 | pEC50 | 0.6 | nM | EC50 | J Med Chem (2022) 65: 9974-10000 [PMID:35797110] |
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] | ||||||||
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 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]