ChEMBL ligand: CHEMBL1393 (Abbolactone, Aldactone, Carospir, Diatensec, Gx spironol, Laractone, NSC-150399, SC-9420, Spiretic, Spiroctan 100, Spiroctan 25, Spiroctan 50, Spironolactone, Spironolactone ceva, Spironolactonum, Spirospare 100, Spirospare 25, Verospirone)
Androgen receptor/Androgen Receptor in Human [ChEMBL: CHEMBL1871] [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!
CYP2C19/Cytochrome P450 2C19 in Human [ChEMBL: CHEMBL3622] [GtoPdb: 1328] [UniProtKB: P33261] 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!
Mineralocorticoid receptor in Human [ChEMBL: CHEMBL1994] [GtoPdb: 626] [UniProtKB: P08235] There should be some charts here, you may need to enable JavaScript!
Multidrug and toxin extrusion/Multidrug and toxin extrusion protein 1 in Human [ChEMBL: CHEMBL1743126] [GtoPdb: 1216] [UniProtKB: Q96FL8] There should be some charts here, you may need to enable JavaScript!
ABCB1/P-glycoprotein 1 in Human [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183] There should be some charts here, you may need to enable JavaScript!
Plasmodium falciparum [ChEMBL: CHEMBL364] There should be some charts here, you may need to enable JavaScript!
Progesterone receptor in Human [ChEMBL: CHEMBL208] [GtoPdb: 627] [UniProtKB: P06401] Progesterone receptor in Bovine [ChEMBL: CHEMBL1909044] [UniProtKB: Q690N0] 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/Androgen Receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275]
ChEMBL	Binding affinity to human androgen receptor	B	7.4	pKi	39.4	nM	Ki	J Med Chem (2007) 50: 6443-6445 [PMID:18038968]
ChEMBL	Antagonist activity at androgen receptor (unknown origin) by NH Pro assay	B	6.17	pIC50	670	nM	IC50	Bioorg Med Chem Lett (2013) 23: 4388-4392 [PMID:23777778]
ChEMBL	Antagonist activity at human androgen receptor expressed in CHOK1 cells assessed as inhibition of D(-)-norgestrel-induced protein interaction with steroid receptor co-activator peptide after 24 hrs by beta-galactosidase reporter gene assay	B	6.17	pIC50	670	nM	IC50	ACS Med Chem Lett (2015) 6: 461-465 [PMID:25941555]
ChEMBL	Antagonist activity at androgen receptor	F	6.28	pIC50	523	nM	IC50	J Med Chem (2010) 53: 5979-6002 [PMID:20672822]
ChEMBL	Displacement of [3H]testosterone from AR	B	6.92	pIC50	120	nM	IC50	J Med Chem (2011) 54: 8616-8631 [PMID:22074142]
ChEMBL	Displacement of [3H]testosterone from androgen receptor (unknown origin) expressed in 293 cells after 16 hrs by scintillation counting	B	6.92	pIC50	120	nM	IC50	Bioorg Med Chem (2014) 22: 5428-5445 [PMID:25187277]
ChEMBL	Agonist activity at androgen receptor (unknown origin) by NH Pro assay	B	4.7	pEC50	>20000	nM	EC50	Bioorg Med Chem Lett (2013) 23: 4388-4392 [PMID:23777778]
Androgen receptor/Androgen Receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
ChEMBL	DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone)	B	7.04	pKi	90.6	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Inhibitory concentration against recombinant rat androgen receptor expressed in Escherichia coli using [3H]methyltrienolone (R 1881)	B	6.17	pIC50	676.08	nM	IC50	J Med Chem (2005) 48: 5666-5674 [PMID:16134935]
ChEMBL	DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone)	B	6.87	pIC50	135.9	nM	IC50	DrugMatrix in vitro pharmacology data
CYP2C19/Cytochrome P450 2C19 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3622] [GtoPdb: 1328] [UniProtKB: P33261]
ChEMBL	DRUGMATRIX: CYP450, 2C19 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)	B	5.52	pIC50	3000	nM	IC50	DrugMatrix in vitro pharmacology data
Estrogen receptor-α/Estrogen receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372]
ChEMBL	Binding affinity to human estrogen receptor	B	5.96	pKi	>1100	nM	Ki	J Med Chem (2007) 50: 6443-6445 [PMID:18038968]
ChEMBL	Antagonist activity at estrogen receptor alpha (unknown origin) by NH Pro assay	B	4.7	pIC50	>20000	nM	IC50	Bioorg Med Chem Lett (2013) 23: 4388-4392 [PMID:23777778]
ChEMBL	Antagonist activity at estrogen receptor	F	5.24	pIC50	5702	nM	IC50	J Med Chem (2010) 53: 5979-6002 [PMID:20672822]
ChEMBL	Agonist activity at estrogen receptor alpha (unknown origin) by NH Pro assay	B	4.7	pEC50	>20000	nM	EC50	Bioorg Med Chem Lett (2013) 23: 4388-4392 [PMID:23777778]
Estrogen receptor-β/Estrogen receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731]
ChEMBL	Antagonist activity at estrogen receptor beta (unknown origin) by NH Pro assay	B	4.7	pIC50	>20000	nM	IC50	Bioorg Med Chem Lett (2013) 23: 4388-4392 [PMID:23777778]
ChEMBL	Antagonist activity at human estrogen receptor beta assessed as inhibition of agonist-induced protein interaction with steroid receptor co-activator peptide by cell-based reporter gene assay	B	4.7	pIC50	>20000	nM	IC50	ACS Med Chem Lett (2015) 6: 461-465 [PMID:25941555]
ChEMBL	Agonist activity at estrogen receptor beta (unknown origin) by NH Pro assay	B	5.48	pEC50	3300	nM	EC50	Bioorg Med Chem Lett (2013) 23: 4388-4392 [PMID:23777778]
Glucocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150]
ChEMBL	DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone)	B	6.06	pKi	864.8	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Binding affinity to human glucocorticoid receptor	B	7.49	pKi	32.6	nM	Ki	J Med Chem (2007) 50: 6443-6445 [PMID:18038968]
ChEMBL	Antagonist activity at glucocorticoid receptor	F	5.16	pIC50	6920	nM	IC50	J Med Chem (2010) 53: 5979-6002 [PMID:20672822]
ChEMBL	Antagonist activity at glucocorticoid receptor (unknown origin) by NH Pro assay	B	5.39	pIC50	4100	nM	IC50	Bioorg Med Chem Lett (2013) 23: 4388-4392 [PMID:23777778]
ChEMBL	DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone)	B	5.72	pIC50	1902.5	nM	IC50	DrugMatrix in vitro pharmacology data
ChEMBL	Displacement of [3H]dexomethasone from GR	B	5.85	pIC50	1400	nM	IC50	J Med Chem (2011) 54: 8616-8631 [PMID:22074142]
ChEMBL	Agonist activity at glucocorticoid receptor (unknown origin) by NH Pro assay	B	4.7	pEC50	>20000	nM	EC50	Bioorg Med Chem Lett (2013) 23: 4388-4392 [PMID:23777778]
Mineralocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1994] [GtoPdb: 626] [UniProtKB: P08235]
ChEMBL	Displacement of [3H]-aldosterone to human mineralocorticoid receptor LBD by radiometric binding assay	B	8.3	pKi	5.01	nM	Ki	J Med Chem (2019) 62: 1385-1406 [PMID:30596500]
GtoPdb	-	-	8.63	pKi	2.32	nM	Ki	J Med Chem (2007) 50: 6443-5 [PMID:18038968]
ChEMBL	Binding affinity to human mineralocorticoid receptor	B	8.63	pKi	2.32	nM	Ki	J Med Chem (2007) 50: 6443-6445 [PMID:18038968]
ChEMBL	Antagonist activity at human mineralocorticoid receptor expressed in COS1 cells after 1 day by luciferase reporter gene assay	B	7.22	pIC50	60	nM	IC50	Bioorg Med Chem (2014) 22: 5428-5445 [PMID:25187277]
ChEMBL	Antagonist activity at human MR transfected in human COS1 cells after 1 day by luciferase reporter gene assay	F	7.22	pIC50	60	nM	IC50	J Med Chem (2011) 54: 8616-8631 [PMID:22074142]
ChEMBL	Antagonist activity at gal4-fused human mineralocorticoid receptor LBD expressed in UAS-MR-bla HEK293 cells by luciferase reporter gene assay	B	7.3	pIC50	50.12	nM	IC50	J Med Chem (2019) 62: 1385-1406 [PMID:30596500]
ChEMBL	Displacement of [3H]aldosterone from human mineralocorticoid receptor expressed in 293 cells after 16 hrs by scintillation counting	B	7.31	pIC50	49	nM	IC50	Bioorg Med Chem (2014) 22: 5428-5445 [PMID:25187277]
ChEMBL	Displacement of [3H]aldosterone from cytosolic human MR expressed in HEK293 cells after 16 hrs by scintillation counting	B	7.31	pIC50	49	nM	IC50	J Med Chem (2011) 54: 8616-8631 [PMID:22074142]
ChEMBL	Antagonist activity at Gal4-tagged mineralocorticoid receptor expressed in human Huh7 cells by luciferase reporter gene assay	F	7.89	pIC50	13	nM	IC50	J Med Chem (2010) 53: 5979-6002 [PMID:20672822]
ChEMBL	Antagonist activity at human full-length MCR assessed as inhibition of receptor binding to co-activator peptide by PathHunter assay	B	7.96	pIC50	11	nM	IC50	Bioorg Med Chem Lett (2016) 26: 2866-2869 [PMID:27161805]
ChEMBL	Antagonist activity at human mineralocorticoid receptor assessed as inhibition of binding to coactivator peptide by NH Pro assay	B	7.96	pIC50	11	nM	IC50	Bioorg Med Chem Lett (2013) 23: 4388-4392 [PMID:23777778]
ChEMBL	Antagonist activity at mineralocorticoid receptor (unknown origin) by PathHunter assay	B	7.96	pIC50	11	nM	IC50	Bioorg Med Chem Lett (2014) 24: 1681-1684 [PMID:24630411]
ChEMBL	Antagonist activity at mineralocorticoid receptor ligand binding domain expressed in african green monkey COS7 cells co-transfected with Gal4-LBD by luciferase reporter gene assay	B	8.8	pIC50	1.6	nM	IC50	J Nat Prod (2009) 72: 1944-1948 [PMID:19863083]
Multidrug and toxin extrusion/Multidrug and toxin extrusion protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743126] [GtoPdb: 1216] [UniProtKB: Q96FL8]
ChEMBL	Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay	B	4.73	pIC50	18600	nM	IC50	J Med Chem (2013) 56: 781-795 [PMID:23241029]
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL	TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells	F	4.63	pIC50	23600	nM	IC50	Chem Res Toxicol (2001) 14: 1596-1603 [PMID:11743742]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL	Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay	F	4.9	pIC50	12589.25	nM	IC50	Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL	Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay	F	4.9	pIC50	12589.25	nM	IC50	Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL	Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay	F	5	pIC50	10000	nM	IC50	Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL	Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay	F	5	pIC50	10000	nM	IC50	Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL	Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay	F	5	pIC50	10000	nM	IC50	Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
Progesterone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL208] [GtoPdb: 627] [UniProtKB: P06401]
ChEMBL	Binding affinity to human progesterone receptor	B	6.4	pKi	399.7	nM	Ki	J Med Chem (2007) 50: 6443-6445 [PMID:18038968]
ChEMBL	Antagonist activity at progesterone receptor	F	5	pIC50	>10000	nM	IC50	J Med Chem (2010) 53: 5979-6002 [PMID:20672822]
ChEMBL	Antagonist activity at progesterone receptor beta (unknown origin) by NH Pro assay	B	5.4	pIC50	4000	nM	IC50	Bioorg Med Chem Lett (2013) 23: 4388-4392 [PMID:23777778]
ChEMBL	Displacement of [3H]-Dexamethasone from glucocorticoid receptor (unknown origin) expressed in 293 cells after 16 hrs by scintillation counting	B	5.85	pIC50	1400	nM	IC50	Bioorg Med Chem (2014) 22: 5428-5445 [PMID:25187277]
ChEMBL	Displacement of [3H]progesterone from PR	B	6.19	pIC50	650	nM	IC50	J Med Chem (2011) 54: 8616-8631 [PMID:22074142]
ChEMBL	Displacement of [[3H]-Progesterone from progesterone receptor (unknown origin) expressed in 293 cells after 16 hrs by scintillation counting	B	6.19	pIC50	650	nM	IC50	Bioorg Med Chem (2014) 22: 5428-5445 [PMID:25187277]
ChEMBL	Agonist activity at progesterone receptor beta (unknown origin) by NH Pro assay	B	4.7	pEC50	>20000	nM	EC50	Bioorg Med Chem Lett (2013) 23: 4388-4392 [PMID:23777778]
Progesterone receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1909044] [UniProtKB: Q690N0]
ChEMBL	DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020)	B	6.66	pKi	217.2	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020)	B	5.78	pIC50	1665.4	nM	IC50	DrugMatrix in vitro pharmacology data

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]