[3H]methyltrienolone [Ligand Id: 3457] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL166444 (Methyltrienolone, Metribolone, NSC-92858, R 1881, R-1881) |
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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 Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275] | ||||||||
| ChEMBL | Dissociation constant for [3H]R-1881 binding to human androgen receptor at 310K | B | 8.71 | pKd | 1.95 | nM | Kd | J Med Chem (2005) 48: 2026-2035 [PMID:15771445] |
| ChEMBL | Dissociation constant for [3H]R-1881 binding to human androgen receptor at 308 K | B | 8.82 | pKd | 1.51 | nM | Kd | J Med Chem (2005) 48: 2026-2035 [PMID:15771445] |
| ChEMBL | Dissociation constant for [3H]R-1881 binding to human androgen receptor at 303 K | B | 8.92 | pKd | 1.21 | nM | Kd | J Med Chem (2005) 48: 2026-2035 [PMID:15771445] |
| ChEMBL | Dissociation constant for [3H]R-1881 binding to human androgen receptor at 298 K | B | 9 | pKd | 0.99 | nM | Kd | J Med Chem (2005) 48: 2026-2035 [PMID:15771445] |
| ChEMBL | Dissociation constant value of the radiolabeled compound against the androgen receptor 293 K | B | 9.13 | pKd | 0.74 | nM | Kd | J Med Chem (2005) 48: 2026-2035 [PMID:15771445] |
| ChEMBL | Dissociation constant for [3H]R-1881 binding to human androgen receptor at 288 K | B | 9.17 | pKd | 0.68 | nM | Kd | J Med Chem (2005) 48: 2026-2035 [PMID:15771445] |
| ChEMBL | Dissociation constant for [3H]R-1881 binding to human androgen receptor at 273 K | B | 9.21 | pKd | 0.61 | nM | Kd | J Med Chem (2005) 48: 2026-2035 [PMID:15771445] |
| ChEMBL | Binding affinity to androgen receptor | B | 9.22 | pKd | 0.6 | nM | Kd | J Med Chem (2010) 53: 3349-3360 [PMID:20355713] |
| ChEMBL | Dissociation constant for [3H]R-1881 binding to human androgen receptor at 283 K | B | 9.25 | pKd | 0.56 | nM | Kd | J Med Chem (2005) 48: 2026-2035 [PMID:15771445] |
| ChEMBL | Dissociation constant for [3H]R-1881 binding to human androgen receptor at 278 K | B | 9.28 | pKd | 0.52 | nM | Kd | J Med Chem (2005) 48: 2026-2035 [PMID:15771445] |
| ChEMBL | Displacement of [3H]-methyltrienolone from androgen receptor (unknown origin) expressed in HEK293 cell lysate incubated overnight by microbeta scintillation counting method | B | 9.4 | pKi | 0.4 | nM | Ki | J Med Chem (2016) 59: 750-755 [PMID:26683992] |
| ChEMBL | Binding affinity to androgen receptor by fluorescence binding assay | B | 8.15 | pIC50 | 7 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 7516-7520 [PMID:21036041] |
| ChEMBL | Competitive displacement of [3H]R1881 from human AR-LBD expressed in LNCaP cells incubated for 24 hrs by scintillation counting method based radioligand competitive binding assay | B | 8.34 | pIC50 | 4.6 | nM | IC50 | Eur J Med Chem (2019) 171: 265-281 [PMID:30925341] |
| ChEMBL | Agonist activity at GAL4 DNA-binding domain fused androgen receptor (unknown origin) ligand binding domain expressed in UAS-bla GripTite 293 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 human androgen receptor expressed in mouse C2C12 cells cotransfected with GRE/ARE reporter plasmid assessed as receptor transactivation after 48 hrs by luciferase reporter gene assay | B | 10.89 | pEC50 | 0.01 | nM | EC50 | J Med Chem (2016) 59: 750-755 [PMID:26683992] |
| 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 | 8.51 | pIC50 | 3.09 | nM | IC50 | J Med Chem (2005) 48: 5666-5674 [PMID:16134935] |
| ChEMBL | Inhibition of rat AR-mediated reporter gene expression in COS7 cells | B | 8.82 | pIC50 | 1.5 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 3233-3237 [PMID:16603353] |
| Glucocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150] | ||||||||
| ChEMBL | Displacement of [3H]-dexamethasone from glucocorticoid receptor (unknown origin) expressed in HEK293 cell lysate incubated overnight by microbeta scintillation counting method | B | 8.02 | pKi | 9.65 | nM | Ki | J Med Chem (2016) 59: 750-755 [PMID:26683992] |
| Mineralocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1994] [GtoPdb: 626] [UniProtKB: P08235] | ||||||||
| ChEMBL | Displacement of [3H]-aldosterone from mineralocorticoid receptor (unknown origin) expressed in HEK293 cell lysate incubated overnight by microbeta scintillation counting method | B | 9.27 | pKi | 0.54 | nM | Ki | J Med Chem (2016) 59: 750-755 [PMID:26683992] |
| Progesterone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL208] [GtoPdb: 627] [UniProtKB: P06401] | ||||||||
| ChEMBL | Displacement of [3H]-methyltrienolone from progesterone receptor (unknown origin) expressed in HEK293 cell lysate incubated overnight by microbeta scintillation counting method | B | 9.31 | pKi | 0.49 | nM | Ki | J Med Chem (2016) 59: 750-755 [PMID:26683992] |
| Testis-specific androgen-binding protein in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4932] [UniProtKB: P08689] | ||||||||
| ChEMBL | Inhibition of rat androgen binding protein (rABP) (n=9) | B | 8.43 | pIC50 | 3.7 | nM | IC50 | J Med Chem (1990) 33: 129-132 [PMID:2296011] |
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]
