mibolerone [Ligand Id: 2859] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL425863 (Cheque drops, Dihydrolone, Matenon, Mibolerone, Mibolerone ciii, NSC-72260, U-10,997, U-10-997, U-10997)
  • Androgen receptor in Human [GtoPdb: 628] [UniProtKB: P10275]
  • Androgen receptor/Androgen Receptor in Rat [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Androgen receptor in Human [GtoPdb: 628] [UniProtKB: P10275]
GtoPdb - - 8.96 pIC50 1.1 nM IC50 J Clin Endocrinol Metab (2000) 85: 2253-9 [PMID:10852459]
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]
GtoPdb - - 8.8 pIC50 - - - Chem Res Toxicol (2003) 16: 1338-58 [PMID:14565775]
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]