ChEMBL ligand: CHEMBL386630 (Androderm, Androgel, Androgel 1%, Android-t, Androlan, Andropatch, Axiron, Delatestryl, Fortesta, Homosterone, Intrinsa, Livensa, Natesto, NSC-9700, Striant, Striant sr, Testiculosterone, Testim, TESTIM, Testim 1%, Testoderm, Testoderm tts, Testogel, Testopatch, Testopel, Testoral, Testosterone, Testosterone ciii, Tostran, Virosterone, Vogelxo)
3-beta-hydroxysteroid-delta(8),delta(7)-isomerase in Human [ChEMBL: CHEMBL4931] [UniProtKB: Q15125] There should be some charts here, you may need to enable JavaScript!
synuclein alpha/Alpha-synuclein in Human [ChEMBL: CHEMBL6152] [GtoPdb: 3285] [UniProtKB: P37840] There should be some charts here, you may need to enable JavaScript!
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] There should be some charts here, you may need to enable JavaScript!
C-8 sterol isomerase in Saccharomyces cerevisiae S288c [ChEMBL: CHEMBL3224] [UniProtKB: P32352] There should be some charts here, you may need to enable JavaScript!
Constitutive androstane receptor in Mouse [ChEMBL: CHEMBL3069] [UniProtKB: O35627] There should be some charts here, you may need to enable JavaScript!
Corticosteroid binding globulin in Human [ChEMBL: CHEMBL2421] [UniProtKB: P08185] There should be some charts here, you may need to enable JavaScript!
CYP19A1/Cytochrome P450 19A1 in Human [ChEMBL: CHEMBL1978] [GtoPdb: 1362] [UniProtKB: P11511] There should be some charts here, you may need to enable JavaScript!
CYP51A1/Cytochrome P450 51 in Human [ChEMBL: CHEMBL3849] [GtoPdb: 1374] [UniProtKB: Q16850] There should be some charts here, you may need to enable JavaScript!
Estrogen receptor-α/Estrogen receptor alpha in Human [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372] There should be some charts here, you may need to enable JavaScript!
Estrogen receptor-β/Estrogen receptor beta in Human [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731] There should be some charts here, you may need to enable JavaScript!
Glucocorticoid receptor in Human [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150] There should be some charts here, you may need to enable JavaScript!
GPBA receptor/G-protein coupled bile acid receptor 1 in Human [ChEMBL: CHEMBL5409] [GtoPdb: 37] [UniProtKB: Q8TDU6] There should be some charts here, you may need to enable JavaScript!
Progesterone receptor in Bovine [ChEMBL: CHEMBL1909044] [UniProtKB: Q690N0] There should be some charts here, you may need to enable JavaScript!
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] There should be some charts here, you may need to enable JavaScript!
Solute carrier organic anion transporter family member 1A1 in Rat [ChEMBL: CHEMBL1781859] [UniProtKB: P46720] There should be some charts here, you may need to enable JavaScript!
Testis-specific androgen-binding protein in Human [ChEMBL: CHEMBL3305] [UniProtKB: P04278] There should be some charts here, you may need to enable JavaScript!
Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936] 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
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/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/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	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 34:

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]