ChEMBL ligand: CHEMBL166444 (Methyltrienolone, Metribolone, NSC-92858, R 1881, R-1881)
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!
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!
Progesterone receptor in Human [ChEMBL: CHEMBL208] [GtoPdb: 627] [UniProtKB: P06401] There should be some charts here, you may need to enable JavaScript!
Testis-specific androgen-binding protein in Rat [ChEMBL: CHEMBL4932] [UniProtKB: P08689] 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	Dissociation constant for [3H]R-1881 binding to human androgen receptor at 310K	B	8.71	pKd	1.95	nM	Kd	J. Med. Chem. (2005) 48: 2026-2035 [PMID:15771445]
ChEMBL	Dissociation constant for [3H]R-1881 binding to human androgen receptor at 308 K	B	8.82	pKd	1.51	nM	Kd	J. Med. Chem. (2005) 48: 2026-2035 [PMID:15771445]
ChEMBL	Dissociation constant for [3H]R-1881 binding to human androgen receptor at 303 K	B	8.92	pKd	1.21	nM	Kd	J. Med. Chem. (2005) 48: 2026-2035 [PMID:15771445]
ChEMBL	Dissociation constant for [3H]R-1881 binding to human androgen receptor at 298 K	B	9	pKd	0.99	nM	Kd	J. Med. Chem. (2005) 48: 2026-2035 [PMID:15771445]
ChEMBL	Dissociation constant value of the radiolabeled compound against the androgen receptor 293 K	B	9.13	pKd	0.74	nM	Kd	J. Med. Chem. (2005) 48: 2026-2035 [PMID:15771445]
ChEMBL	Dissociation constant for [3H]R-1881 binding to human androgen receptor at 288 K	B	9.17	pKd	0.68	nM	Kd	J. Med. Chem. (2005) 48: 2026-2035 [PMID:15771445]
ChEMBL	Dissociation constant for [3H]R-1881 binding to human androgen receptor at 273 K	B	9.21	pKd	0.61	nM	Kd	J. Med. Chem. (2005) 48: 2026-2035 [PMID:15771445]
ChEMBL	Binding affinity to androgen receptor	B	9.22	pKd	0.6	nM	Kd	J. Med. Chem. (2010) 53: 3349-3360 [PMID:20355713]
ChEMBL	Dissociation constant for [3H]R-1881 binding to human androgen receptor at 283 K	B	9.25	pKd	0.56	nM	Kd	J. Med. Chem. (2005) 48: 2026-2035 [PMID:15771445]
ChEMBL	Dissociation constant for [3H]R-1881 binding to human androgen receptor at 278 K	B	9.28	pKd	0.52	nM	Kd	J. Med. Chem. (2005) 48: 2026-2035 [PMID:15771445]
ChEMBL	Displacement of [3H]-methyltrienolone from androgen receptor (unknown origin) expressed in HEK293 cell lysate incubated overnight by microbeta scintillation counting method	B	9.4	pKi	0.4	nM	Ki	J. Med. Chem. (2016) 59: 750-755 [PMID:26683992]
ChEMBL	Binding affinity to androgen receptor by fluorescence binding assay	B	8.15	pIC50	7	nM	IC50	Bioorg. Med. Chem. Lett. (2010) 20: 7516-7520 [PMID:21036041]
ChEMBL	Competitive displacement of [3H]R1881 from human AR-LBD expressed in LNCaP cells incubated for 24 hrs by scintillation counting method based radioligand competitive binding assay	B	8.34	pIC50	4.6	nM	IC50	Eur J Med Chem (2019) 171: 265-281 [PMID:30925341]
ChEMBL	Agonist activity at GAL4 DNA-binding domain fused androgen receptor (unknown origin) ligand binding domain expressed in UAS-bla GripTite 293 cells assessed as beta-lactamase transcriptional activation by FRET-based GeneBLAzer assay	B	9.52	pIC50	0.3	nM	IC50	Eur J Med Chem (2018) 157: 791-804 [PMID:30144697]
ChEMBL	Agonist activity at human androgen receptor expressed in mouse C2C12 cells cotransfected with GRE/ARE reporter plasmid assessed as receptor transactivation after 48 hrs by luciferase reporter gene assay	B	10.89	pEC50	0.01	nM	EC50	J. Med. Chem. (2016) 59: 750-755 [PMID:26683992]
Androgen receptor/Androgen Receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
ChEMBL	Inhibitory concentration against recombinant rat androgen receptor expressed in Escherichia coli using [3H]methyltrienolone (R 1881)	B	8.51	pIC50	3.09	nM	IC50	J. Med. Chem. (2005) 48: 5666-5674 [PMID:16134935]
ChEMBL	Inhibition of rat AR-mediated reporter gene expression in COS7 cells	B	8.82	pIC50	1.5	nM	IC50	Bioorg. Med. Chem. Lett. (2006) 16: 3233-3237 [PMID:16603353]
Glucocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150]
ChEMBL	Displacement of [3H]-dexamethasone from glucocorticoid receptor (unknown origin) expressed in HEK293 cell lysate incubated overnight by microbeta scintillation counting method	B	8.02	pKi	9.65	nM	Ki	J. Med. Chem. (2016) 59: 750-755 [PMID:26683992]
Mineralocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1994] [GtoPdb: 626] [UniProtKB: P08235]
ChEMBL	Displacement of [3H]-aldosterone from mineralocorticoid receptor (unknown origin) expressed in HEK293 cell lysate incubated overnight by microbeta scintillation counting method	B	9.27	pKi	0.54	nM	Ki	J. Med. Chem. (2016) 59: 750-755 [PMID:26683992]
Progesterone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL208] [GtoPdb: 627] [UniProtKB: P06401]
ChEMBL	Displacement of [3H]-methyltrienolone from progesterone receptor (unknown origin) expressed in HEK293 cell lysate incubated overnight by microbeta scintillation counting method	B	9.31	pKi	0.49	nM	Ki	J. Med. Chem. (2016) 59: 750-755 [PMID:26683992]
Testis-specific androgen-binding protein in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4932] [UniProtKB: P08689]
ChEMBL	Inhibition of rat androgen binding protein (rABP) (n=9)	B	8.43	pIC50	3.7	nM	IC50	J. Med. Chem. (1990) 33: 129-132 [PMID:2296011]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]