testosterone [Ligand Id: 2858] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL386630 (Androderm, Androgel, Androgel 1%, Android-t, Androlan, Andropatch, Axiron, Fortesta, Homosterone, Intrinsa, Livensa, Natesto, NSC-9700, Striant, Striant sr, Testiculosterone, Testim, TESTIM, Testim 1%, Testoderm, Testoderm tts, Testogel, Testopatch, Testopel, Testoral, Testosterona, Testosterone, Testosterone ciii, Tostran, Virosterone, Vogelxo) |
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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] |
| synuclein alpha/Alpha-synuclein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6152] [GtoPdb: 3285] [UniProtKB: P37840] | ||||||||
| ChEMBL | Inhibition of alpha-synuclein aggregation (unknown origin) incubated for 8 days by thioflavin S based fluorescence assay | B | 4.01 | pIC50 | 96800 | nM | IC50 | Eur J Med Chem (2019) 167: 10-36 [PMID:30743095] |
| Androgen receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275] | ||||||||
| ChEMBL | Binding affinity to human Androgen receptor | B | 9.4 | pKd | 0.4 | nM | Kd | J Med Chem (2022) 65: 8772-8797 [PMID:35786895] |
| 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] |
| ChEMBL | Modulation of Androgen receptor (unknown origin) | B | 8.72 | pEC50 | 1.9 | nM | EC50 | Eur J Med Chem (2022) 230: 114119-114119 [PMID:35063736] |
| Androgen receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3056] [GtoPdb: 628] [UniProtKB: P19091] | ||||||||
| ChEMBL | Androgen Receptor Assay: Androgen binding is measured using the hydroxylapatite (HAP) assay. In brief, the radioactive steroid [3H]R1881 solubilized in ethanol is diluted with buffer B (10 mM Tris-HCl, 1.5 mM EDTA disodium salt, 10 mM α-monothioglycerol, pH 7.4). Aliquots of the cell or prostate cytosol preparation (0.1 ml) are then incubated with 5 nM [3H]R1881 (0.1 ml, ¿100 000 cpm) in the presence or absence of the indicated concentrations of unlabeled compounds (0.1 ml, prepared in buffer B containing 30% ethanol) for 16-18 h at 0-4° C. Triamcinolone acetonide (TAC; 100 nM) is added to mask progesterone receptors. Unbound steroids are separated by incubation for 40 min at 0-4° C. with 0.3 ml HAP prepared in buffer P (50 mM Tris-HCl, 10 mM KH2PO4, pH 7.4). After incubation with HAP and 10 min of centrifugation at 1000×g, the pellet is washed 3 times with 1 ml of buffer P. Thereafter, the radioactivity is extracted from the pellet by incubation at room temperature for 60 min with 1 ml of ethanol. After centrifugation, the supernatant is decanted into a scintillation vial and the pellet is extracted again with ethanol. After the addition of scintillation liquid, the radioactivity is measured in a liquid scintillation counter. | B | 7.96 | pIC50 | 11 | nM | IC50 | US-9682960-B2. Non-steroidal antiandrogens and selective androgen receptor modulators with a pyridyl moiety (2017) |
| 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 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] |
| CYP19A1/Aromatase 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] |
| C-8 sterol isomerase ERG2 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] |
| 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] |
| Estrogen receptor-α/Estrogen receptor 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] |
| CYP51A1/Lanosterol 14-alpha demethylase 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] |
| Nuclear receptor subfamily 1 group I member 3 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] |
| 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 |
| Sex hormone-binding globulin 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] |
| sigma non-opioid intracellular receptor 1/Sigma non-opioid intracellular receptor 1 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] |
| Cav1.2/Voltage-dependent L-type calcium channel subunit alpha-1C 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 | J Appl Toxicol (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 | J Appl Toxicol (2012) 32: 858-866 [PMID:22761000] |
ChEMBL data shown on this page come from version 36:
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]
