testosterone [Ligand Id: 2858] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL386630 (Androgel, Testopatch, Axiron, Testoderm tts, Testosterone, Fortesta, Testim 1%, NSC-9700, Vogelxo, Natesto, Testopel, Andropatch, Intrinsa, Striant SR, Testogel, Tostran, Testosterone ciii, Striant, Testoderm, Androderm, Testim, Androgel 1%, Delatestryl, Testoral)
  • 3-beta-hydroxysteroid-delta(8),delta(7)-isomerase in Human [ChEMBL: CHEMBL4931] [UniProtKB: Q15125]
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  • Androgen receptor/Androgen Receptor in Human [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275]
  • Androgen receptor/Androgen Receptor in Mouse [ChEMBL: CHEMBL3056] [GtoPdb: 628] [UniProtKB: P19091]
  • Androgen receptor/Androgen Receptor in Rat [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
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  • C-8 sterol isomerase in Saccharomyces cerevisiae S288c [ChEMBL: CHEMBL3224] [UniProtKB: P32352]
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  • Constitutive androstane receptor in Mouse [ChEMBL: CHEMBL3069] [UniProtKB: O35627]
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  • Corticosteroid binding globulin in Human [ChEMBL: CHEMBL2421] [UniProtKB: P08185]
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  • Estrogen receptor-α/Estrogen receptor alpha in Human [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372]
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  • Estrogen receptor-β/Estrogen receptor beta in Human [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731]
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  • GPBA receptor/G-protein coupled bile acid receptor 1 in Human [ChEMBL: CHEMBL5409] [GtoPdb: 37] [UniProtKB: Q8TDU6]
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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
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  • Solute carrier organic anion transporter family member 1A1 in Rat [ChEMBL: CHEMBL1781859] [UniProtKB: P46720]
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  • Testis-specific androgen-binding protein in Human [ChEMBL: CHEMBL3305] [UniProtKB: P04278]
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  • Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
3-beta-hydroxysteroid-delta(8),delta(7)-isomerase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4931] [UniProtKB: Q15125]
ChEMBL Affinity for human EMP expressed in ERG2 deficient strain of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine as radioligand B 4 pKi >100000 nM Ki J. Med. Chem. (2005) 48: 4754-4764 [PMID:16033255]
Androgen receptor/Androgen Receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275]
ChEMBL Displacement of fluorescent-tagged R1881 from androgen receptor after 4 hrs by fluorometric assay B 7.54 pKi 29 nM Ki ACS Med. Chem. Lett. (2011) 2: 124-129 [PMID:24900290]
ChEMBL Binding affinity to androgen receptor by fluorescence binding assay B 7.52 pIC50 30 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 7516-7520 [PMID:21036041]
ChEMBL Displacement of [3H]R1881 from wild type human androgen receptor expressed in COS-1 cells co-transfected with pSG5 after 15 mins by scintillation assay B 8.34 pIC50 4.57 nM IC50 J. Med. Chem. (2012) 55: 6316-6327 [PMID:22746350]
ChEMBL Displacement of [3H]R1881 from pSG5-tagged human androgen receptor expressed in COS1 cells assessed as relative binding inhibition B 8.37 pIC50 4.27 nM IC50 J. Med. Chem. (2015) 58: 1569-1574 [PMID:25646649]
ChEMBL Antagonist activity against pSG5-tagged human androgen receptor expressed in COS1 cells assessed as reduction in receptor-mediated transcriptional activity by AR-regulated rat probasin promoter fragment driven firefly luciferase reporter assay B 8.38 pIC50 4.17 nM IC50 J. Med. Chem. (2015) 58: 1569-1574 [PMID:25646649]
ChEMBL Inhibition of human androgen receptor expressed in Escherichia coli B 8.41 pIC50 3.9 nM IC50 J. Med. Chem. (2004) 47: 4985-4988 [PMID:15456242]
ChEMBL Binding affinity at AR B 8.57 pIC50 2.7 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 6295-6298 [PMID:17890084]
ChEMBL Binding affinity to androgen receptor B 8.57 pIC50 2.7 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 2944-2948 [PMID:17448656]
ChEMBL Inhibitory activity against AR B 8.57 pIC50 2.7 nM IC50 Bioorg. Med. Chem. Lett. (2006) 16: 834-838 [PMID:16309907]
ChEMBL Agonist activity at androgen receptor in human MDA-KB2 cells transfected with MMTV linked luciferase assessed as transcriptional activation by luciferase reporter gene assay F 8.5 pEC50 3.16 nM EC50 J. Med. Chem. (2009) 52: 7186-7191 [PMID:19856921]
Androgen receptor/Androgen Receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3056] [GtoPdb: 628] [UniProtKB: P19091]
ChEMBL Agonist activity at androgen receptor in mouse NIH3T3 cells transiently transfected with beta-galactosidase reporter gene assessed as cellular transformation by R-SAT assay F 8.7 pEC50 2 nM EC50 J. Med. Chem. (2009) 52: 7186-7191 [PMID:19856921]
Androgen receptor/Androgen Receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
ChEMBL Binding affinity against rat prostate cytosolic Androgen receptor using [3H]mibolerone as radioligand B 8.31 pKi 4.9 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 1045-1047 [PMID:11327585]
ChEMBL Inhibition of rat prostate cytosolic androgen receptor B 8.31 pKi 4.9 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 5285-5288 [PMID:15454212]
ChEMBL Displacement of [3H]Mibolerone from rat recombinant androgen receptor expressed in Escherichia coli after 4 hrs B 8.37 pKi 4.3 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone) B 8.39 pKi 4.11 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Inhibition of [3H]mibolerone binding to cytosolic androgen receptor of rat ventral prostate B 8.85 pKi 1.41 nM Ki J. Med. Chem. (2005) 48: 917-925 [PMID:15715462]
ChEMBL Inhibitory constant against rat prostate cytosol androgen receptor using [3H]mibolerone B 8.85 pKi 1.4 nM Ki J. Med. Chem. (2000) 43: 3344-3347 [PMID:10966753]
ChEMBL Inhibitory concentration against recombinant rat androgen receptor expressed in Escherichia coli using [3H]methyltrienolone (R 1881) B 5.51 pIC50 3090.3 nM IC50 J. Med. Chem. (2005) 48: 5666-5674 [PMID:16134935]
GtoPdb - - 7.8 pIC50 - - - Chem. Res. Toxicol. (2003) 16: 1338-58 [PMID:14565775]
ChEMBL Displacement of [3H]Mibolerone from rat recombinant androgen receptor expressed in Escherichia coli after 4 hrs B 8.19 pIC50 6.5 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone) B 8.21 pIC50 6.17 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL In vitro antagonist activity against rat prostatic androgen receptor (AR) F 8.49 pIC50 3.2 nM IC50 J. Med. Chem. (1986) 29: 2298-2315 [PMID:3783591]
C-8 sterol isomerase in Saccharomyces cerevisiae S288c (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3224] [UniProtKB: P32352]
ChEMBL Affinity for ERG2 of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine radioligand B 5.11 pKi 7760 nM Ki J. Med. Chem. (2005) 48: 4754-4764 [PMID:16033255]
Constitutive androstane receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3069] [UniProtKB: O35627]
ChEMBL Inhibitory concentration against mammalian m-constitutive androstane receptor (mCAR) activity B 4.52 pIC50 30000 nM IC50 J. Med. Chem. (2003) 46: 4687-4695 [PMID:14561088]
Corticosteroid binding globulin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2421] [UniProtKB: P08185]
ChEMBL In silico binding affinity to human corticosteriod binding globulin B 5.72 pKd 5.72 - -Log Kdiss J. Med. Chem. (1997) 40: 3161-3172 [PMID:9379435]
ChEMBL Binding affinity to human CBG receptor (corticosteroid-binding globulins) B 6.72 pKi 190.55 nM Ki J. Med. Chem. (2004) 47: 2732-2742 [PMID:15139751]
CYP19A1/Cytochrome P450 19A1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1978] [GtoPdb: 1362] [UniProtKB: P11511]
ChEMBL Inhibition of human placental aromatase Cytochrome P450 19A1 B 6.22 pKi 600 nM Ki J. Med. Chem. (1983) 26: 50-54 [PMID:6827528]
CYP51A1/Cytochrome P450 51 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3849] [GtoPdb: 1374] [UniProtKB: Q16850]
ChEMBL Inhibition of human CYP51 expressed in Topp 3 cells by lanosterol demethylase assay B 4.3 pIC50 50000 nM IC50 Drug Metab. Dispos. (2007) 35: 493-500 [PMID:17194716]
Estrogen receptor-α/Estrogen receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372]
ChEMBL Binding affinity to human ERalpha B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2006) 16: 834-838 [PMID:16309907]
ChEMBL Binding affinity to human recombinant ERalpha by scintillation proximity assay B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 2944-2948 [PMID:17448656]
Estrogen receptor-β/Estrogen receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731]
ChEMBL Binding affinity to human ERbeta B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2006) 16: 834-838 [PMID:16309907]
ChEMBL Binding affinity to human recombinant ERbeta by scintillation proximity assay B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 2944-2948 [PMID:17448656]
ChEMBL Binding affinity at human recombinant ERbeta B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 6295-6298 [PMID:17890084]
Glucocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150]
ChEMBL DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone) B 5.84 pKi 1457 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone) B 5.49 pIC50 3206 nM IC50 DrugMatrix in vitro pharmacology data
GPBA receptor/G-protein coupled bile acid receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5409] [GtoPdb: 37] [UniProtKB: Q8TDU6]
ChEMBL Agonist activity at human TGR5 expressed in CHO cells by luciferase assay F 4.74 pEC50 18300 nM EC50 J. Med. Chem. (2008) 51: 1831-1841 [PMID:18307294]
Progesterone receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1909044] [UniProtKB: Q690N0]
ChEMBL DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) B 6.6 pKi 252 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) B 5.71 pIC50 1935 nM IC50 DrugMatrix in vitro pharmacology data
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL Affinity for sigma receptor type 1 of guinea pig using [3H]ifenprodil or (+)-[3H]pentazocine radioligand B 5.92 pKi 1200 nM Ki J. Med. Chem. (2005) 48: 4754-4764 [PMID:16033255]
Solute carrier organic anion transporter family member 1A1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1781859] [UniProtKB: P46720]
ChEMBL TP_TRANSPORTER: inhibition of E217betaG uptake in Oatp1-expressing HeLa cells F 5.27 pKi 5400 nM Ki Am. J. Physiol. (1996) 270: F326-F331 [PMID:8779894]
Testis-specific androgen-binding protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3305] [UniProtKB: P04278]
ChEMBL Binding affinity towards human testosterone binding globulin. B 8.2 pKd 8.2 - -Log Kdiss J. Med. Chem. (1997) 40: 3161-3172 [PMID:9379435]
ChEMBL Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin B 9.2 pKd 0.63 nM Kd J. Med. Chem. (2008) 51: 2047-2056 [PMID:18330978]
ChEMBL Displacement of [3H]DHT from human SHBG B 7.85 pIC50 14 nM IC50 J. Med. Chem. (2006) 49: 7466-7478 [PMID:17149875]
Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936]
ChEMBL Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit F 7.42 pIC50 38.4 nM IC50 Journal of Applied Toxicology (2012) 32: 858-866 [PMID:22761000]
ChEMBL Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit F 7.47 pIC50 34 nM IC50 Journal of Applied Toxicology (2012) 32: 858-866 [PMID:22761000]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]