[3H]mibolerone [Ligand Id: 3456] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL425863 (Cheque drops, Dihydrolone, Matenon, Mibolerone, Mibolerone ciii, NSC-72260, U-10,997, U-10-997, U-10997)
  • Androgen receptor/Androgen Receptor in Rat [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
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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 Inhibition of [3H]mibolerone binding to cytosolic androgen receptor of rat ventral prostate B 9.12 pKi 0.76 nM Ki J Med Chem (2005) 48: 917-925 [PMID:15715462]
ChEMBL Binding affinity against rat prostate cytosolic Androgen receptor using [3H]mibolerone as radioligand B 9.12 pKi 0.75 nM Ki Bioorg Med Chem Lett (2001) 11: 1045-1047 [PMID:11327585]
ChEMBL Inhibitory constant against rat prostate cytosol androgen receptor using [3H]mibolerone B 9.12 pKi 0.75 nM Ki J Med Chem (2000) 43: 3344-3347 [PMID:10966753]
ChEMBL Inhibition of rat prostate cytosolic androgen receptor B 9.12 pKi 0.75 nM Ki Bioorg Med Chem Lett (2004) 14: 5285-5288 [PMID:15454212]
ChEMBL Inhibitory concentration against recombinant rat androgen receptor expressed in Escherichia coli using [3H]methyltrienolone (R 1881) B 8.78 pIC50 1.66 nM IC50 J Med Chem (2005) 48: 5666-5674 [PMID:16134935]
ChEMBL Displacement of [3H]-MIB from rat prostate cytosolic androgen receptor by liquid scintillation counting method B 9 pIC50 1 nM IC50 Bioorg Med Chem (2017) 25: 1600-1607 [PMID:28174065]

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]