ChEMBL ligand: CHEMBL166444 (Methyltrienolone, Metribolona, 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	Binding affinity to GST-tagged androgen receptor LBD (unknown origin) incubated for 4 hrs by fluorescence polarization assay	B	8.3	pIC50	5	nM	IC50	J Med Chem (2023) 66: 13280-13303 [PMID:37683104]
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]
GtoPdb	-	-	5	pEC50	>10000	nM	EC50	Biochem Pharmacol (1998) 55: 1427-33 [PMID:10076535]
ChEMBL	Modulation of Androgen receptor (unknown origin)	B	9.96	pEC50	0.11	nM	EC50	Eur J Med Chem (2022) 230: 114119-114119 [PMID:35063736]
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]
GtoPdb	-	-	8.51	pIC50	-	-	-	Chem Res Toxicol (2003) 16: 1338-58 [PMID:14565775]
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]
ChEMBL	Binding affinity to rat Androgen receptor in African green monkey COS-7 cells measured by whole-cell binding assay	B	8.82	pIC50	1.5	nM	IC50	J Med Chem (2022) 65: 8772-8797 [PMID:35786895]
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 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]