dihydrotestosterone [Ligand Id: 2856] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL27769 (4-dihydrotestosterone, 5alpha-dihydrotestosterone, Anabolex, Andractim, Androstanolone, Dihydrotestosterone, Dihydrotestosterone (dht), Neodrol, NSC-10972, Stanolone) |
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| 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] | ||||||||
| GtoPdb | - | - | 9.3 | pKd | 0.5 | nM | Kd | Proc Natl Acad Sci USA (1989) 86: 327-31 [PMID:2911578] |
| ChEMBL | Displacement of fluorescent-tagged R1881 from androgen receptor after 4 hrs by fluorometric assay | B | 8 | pKi | 10 | nM | Ki | ACS Med Chem Lett (2011) 2: 124-129 [PMID:24900290] |
| ChEMBL | Displacement of [3H]DHT from human androgen receptor after 16 hrs by scintillation counting | B | 8.33 | pKi | 4.7 | nM | Ki | Bioorg Med Chem (2010) 18: 4255-4268 [PMID:20510622] |
| ChEMBL | Binding affinity for human Androgen receptor expressed in COS-1 cells | B | 8.52 | pKi | 3 | nM | Ki | J Med Chem (1999) 42: 210-212 [PMID:9925725] |
| ChEMBL | Binding affinity to the human androgen receptor (hAR), using [3H]DHT as radioligand in a competitive binding assay | B | 8.7 | pKi | 2 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 1335-1340 [PMID:10340624] |
| ChEMBL | Binding affinity against Androgen receptor expressed COS cells | B | 8.7 | pKi | 2 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 745-750 [PMID:9871534] |
| ChEMBL | Binding affinity towards human androgen receptor (hAR), using dihydrotestosterone as radioligand for competitive binding assay | B | 8.7 | pKi | 2 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 1009-1012 [PMID:10230629] |
| ChEMBL | Displacement of [3H]DHT from human Androgen receptor in human MDA-MB-453 cells | B | 9.05 | pKi | 0.9 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 2967-2971 [PMID:18400499] |
| ChEMBL | Displacement of [3H]DHT from human AR expressed in MDA-MB-453 cells | B | 9.52 | pKi | 0.3 | nM | Ki | J Med Chem (2007) 50: 2486-2496 [PMID:17439112] |
| ChEMBL | Displacement of [3H]DHT from human AR in MDA453 cells | B | 9.52 | pKi | 0.3 | nM | Ki | J Med Chem (2006) 49: 7596-7599 [PMID:17181141] |
| ChEMBL | Binding affinity to human AR | B | 9.7 | pKi | 0.2 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 1527-1531 [PMID:17267219] |
| ChEMBL | Binding affinity to human androgen receptor expressed in CV1 cells | B | 9.7 | pKi | 0.2 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 1523-1526 [PMID:17257838] |
| ChEMBL | Binding affinity to human androgen receptor expressed in monkey COS7 cells by whole cell binding assay | B | 9.7 | pKi | 0.2 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 3431-3435 [PMID:18442912] |
| ChEMBL | Displacement of [3H]DHT from human androgen receptor expressed in MDA-MB-453 cells by whole cell receptor binding assay | B | 9.7 | pKi | 0.2 | nM | Ki | J Med Chem (2006) 49: 6143-6146 [PMID:17034117] |
| ChEMBL | Binding affinity to human AR | B | 9.7 | pKi | 0.2 | nM | Ki | J Med Chem (2007) 50: 5049-5052 [PMID:17887661] |
| ChEMBL | Antagonist activity at human androgen receptor expressed in COS7 cells assessed as inhibition of DHT-induced luciferase activity after 24 hrs by reporter gene assay | F | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem (2012) 20: 422-434 [PMID:22094279] |
| ChEMBL | Antagonistic activity against human androgen receptor (hAR) in CV-1 cells using cotransfection assay | F | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 1335-1340 [PMID:10340624] |
| ChEMBL | Antagonist activity at wild type Androgen receptor (unknown origin) expressed in human Cos-7 cells co-expressing pGL3-MMTV-luc vector assessed as luciferase activity by reporter gene assay | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem (2013) 21: 70-83 [PMID:23199477] |
| ChEMBL | Antagonistic activity against human androgen receptor (hAR) expressed in CV-1 cell lines | F | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 1009-1012 [PMID:10230629] |
| ChEMBL | Antagonist activity against human androgen receptor in CV1 cells measured as inhibition of DHT-stimulated luciferase reporter gene activity by cotransfection assay | F | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2006) 49: 6143-6146 [PMID:17034117] |
| ChEMBL | Antagonist activity at Androgen receptor T877A mutant (unknown origin) expressed in human Cos-7 cells co-expressing pGL3-MMTV-luc vector assessed as luciferase activity by reporter gene assay | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem (2013) 21: 70-83 [PMID:23199477] |
| ChEMBL | Antagonist activity at human androgen receptor expressed in CV1 cells by transcriptional activation assay | F | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2007) 50: 2486-2496 [PMID:17439112] |
| ChEMBL | Antagonist activity at human androgen receptor by luciferase reporter gene assay | F | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2007) 50: 5049-5052 [PMID:17887661] |
| ChEMBL | Antagonist activity at human AR | F | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 1527-1531 [PMID:17267219] |
| ChEMBL | Antagonist activity at human androgen receptor expressed in CV1 cells by transcriptional activation assay | F | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 5442-5446 [PMID:17703938] |
| ChEMBL | Antagonist activity at human androgen receptor african green monkey CV1 cells by cotransfection assay | F | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 3431-3435 [PMID:18442912] |
| ChEMBL | Antagonist activity at human androgen receptor W741C mutant expressed in COS7 cells assessed as inhibition of DHT-induced luciferase activity after 24 hrs by reporter gene assay | F | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem (2012) 20: 422-434 [PMID:22094279] |
| ChEMBL | Antagonist activity at human androgen receptor T877A mutant expressed in COS7 cells assessed as inhibition of DHT-induced luciferase activity after 24 hrs by reporter gene assay | F | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem (2012) 20: 422-434 [PMID:22094279] |
| ChEMBL | Displacement of fluormone-AL green from GST-tagged androgen receptor LBD (unknown origin) measured after 4 hrs by fluorescence polarization assay | B | 7.74 | pIC50 | 18 | nM | IC50 | Eur J Med Chem (2020) 192: 112156-112156 [PMID:32114360] |
| ChEMBL | Competitive inhibition of androgen binding to androgen receptor (unknown origin) by invitrogen polar screen assay | B | 7.88 | pIC50 | 13.1 | nM | IC50 | J Med Chem (2015) 58: 6984-6993 [PMID:26305181] |
| ChEMBL | Displacement of [3H]mibolerone from human AR expressed in COS cells after 3.5 hrs by liquid scintillation counting analysis | B | 7.96 | pIC50 | 11 | nM | IC50 | Medchemcomm (2013) 4: 582-589 |
| ChEMBL | In vitro antagonistic activity against human androgen receptor using cotransfection assay in CV-1 cells; Not active. | F | 8 | pIC50 | >10 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 1003-1008 [PMID:10230628] |
| ChEMBL | Binding affinity to androgen receptor by fluorescence binding assay | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 7516-7520 [PMID:21036041] |
| ChEMBL | In vitro binding affinity at human androgen receptor transfected into COS cells. | B | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 1003-1008 [PMID:10230628] |
| ChEMBL | Displacement of [17-alpha-methyl-3H]-mibolerone from human androgen receptor T877A mutant expressed in HEK293 derived FreeStyle293F cells after 3 hrs | B | 8.59 | pIC50 | 2.6 | nM | IC50 | Bioorg Med Chem (2012) 20: 422-434 [PMID:22094279] |
| ChEMBL | Inhibition of Androgen receptor T877A mutant (unknown origin) expressed in Freestyle293F cells | B | 8.59 | pIC50 | 2.6 | nM | IC50 | Bioorg Med Chem (2013) 21: 70-83 [PMID:23199477] |
| ChEMBL | Displacement of [17-alpha-methyl-3H]-mibolerone from human androgen receptor expressed in HEK293 derived FreeStyle293F cells after 3 hrs | B | 8.68 | pIC50 | 2.1 | nM | IC50 | Bioorg Med Chem (2012) 20: 422-434 [PMID:22094279] |
| ChEMBL | Inhibition of wild type Androgen receptor (unknown origin) expressed in Freestyle293F cells | B | 8.68 | pIC50 | 2.1 | nM | IC50 | Bioorg Med Chem (2013) 21: 70-83 [PMID:23199477] |
| ChEMBL | Activity against human androgen receptor expressed in HepG2 cells assessed as luciferase reporter gene activation | B | 8.74 | pIC50 | 1.82 | nM | IC50 | J Med Chem (2006) 49: 7366-7372 [PMID:17149866] |
| ChEMBL | Displacement of [3H]methyltrienolone from androgen receptor in human MDA-MB-453 cells | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2009) 52: 4578-4581 [PMID:19606870] |
| ChEMBL | Displacement of [3H]mibolerone from human AR after 3 hrs | B | 9.17 | pIC50 | 0.67 | nM | IC50 | Bioorg Med Chem (2017) 25: 3330-3349 [PMID:28454849] |
| ChEMBL | Activity at androgen receptor in human Saos2 cells assessed as IL6 repression | B | 10.3 | pIC50 | 0.05 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 3431-3435 [PMID:18442912] |
| ChEMBL | Agonist activity at androgen receptor ligand binding domain expressed in african green monkey COS7 cells co-transfected with Gal4-DBD by luciferase reporter gene assay | B | 7.7 | pEC50 | 20 | nM | EC50 | J Nat Prod (2009) 72: 1944-1948 [PMID:19863083] |
| ChEMBL | Agonist activity at Androgen receptor T877A mutant in human LNCaP-hr cells assessed as prostate specific antigen secretion measured after 3 days by enzyme-immunoassay | B | 7.82 | pEC50 | 15 | nM | EC50 | Bioorg Med Chem (2013) 21: 70-83 [PMID:23199477] |
| ChEMBL | Agonist activity at human androgen receptor T877A mutant expressed in COS7 cells assessed as luciferase activity after 24 hrs by reporter gene assay | F | 7.82 | pEC50 | 15 | nM | EC50 | Bioorg Med Chem (2012) 20: 422-434 [PMID:22094279] |
| ChEMBL | Agonist activity at human androgen receptor W741C mutant expressed in COS7 cells assessed as luciferase activity after 24 hrs by reporter gene assay | F | 7.92 | pEC50 | 12 | nM | EC50 | Bioorg Med Chem (2012) 20: 422-434 [PMID:22094279] |
| ChEMBL | Agonist activity at wild type Androgen receptor in human LNCaP-hr cells assessed as prostate specific antigen secretion measured after 3 days by enzyme-immunoassay | B | 8.21 | pEC50 | 6.2 | nM | EC50 | Bioorg Med Chem (2013) 21: 70-83 [PMID:23199477] |
| ChEMBL | Agonist activity at human androgen receptor expressed in COS7 cells assessed as luciferase activity after 24 hrs by reporter gene assay | F | 8.21 | pEC50 | 6.2 | nM | EC50 | Bioorg Med Chem (2012) 20: 422-434 [PMID:22094279] |
| ChEMBL | Agonist activity to the human androgen receptor (hAR) in CV-1 cells | F | 8.22 | pEC50 | 6 | nM | EC50 | Bioorg Med Chem Lett (1999) 9: 1335-1340 [PMID:10340624] |
| ChEMBL | Agonistic activity (EC50) against human androgen receptor expressed in CV-1 cell | F | 8.22 | pEC50 | 6 | nM | EC50 | Bioorg Med Chem Lett (1998) 8: 745-750 [PMID:9871534] |
| ChEMBL | In vitro agonistic activity against human androgen receptor using cotransfection assay in CV-1 cells. | F | 8.22 | pEC50 | 6 | nM | EC50 | Bioorg Med Chem Lett (1999) 9: 1003-1008 [PMID:10230628] |
| ChEMBL | Agonistic activity against human androgen receptor (hAR) expressed in CV-1 cell lines | F | 8.22 | pEC50 | 6 | nM | EC50 | Bioorg Med Chem Lett (1999) 9: 1009-1012 [PMID:10230629] |
| ChEMBL | Agonist activity at human androgen receptor expressed in CV1 cells by transcriptional activation assay | F | 8.24 | pEC50 | 5.7 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 5442-5446 [PMID:17703938] |
| ChEMBL | Agonist activity at human androgen receptor in CV1 cells by transcriptional activation assay | F | 8.24 | pEC50 | 5.7 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 2967-2971 [PMID:18400499] |
| ChEMBL | Agonist activity at human androgen receptor expressed in CV1 cells by transcriptional activation assay | F | 8.24 | pEC50 | 5.7 | nM | EC50 | J Med Chem (2007) 50: 2486-2496 [PMID:17439112] |
| ChEMBL | Agonist activity at human androgen receptor african green monkey CV1 cells by cotransfection assay | F | 8.29 | pEC50 | 5.1 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 3431-3435 [PMID:18442912] |
| ChEMBL | Agonist activity at human androgen receptor in CV1 cells measured as stimulation of luciferase reporter gene activity by cotransfection assay | F | 8.29 | pEC50 | 5.1 | nM | EC50 | J Med Chem (2006) 49: 6143-6146 [PMID:17034117] |
| ChEMBL | Agonist activity at human androgen receptor expressed in CV1 cells | F | 8.29 | pEC50 | 5.1 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 1523-1526 [PMID:17257838] |
| ChEMBL | Agonist activity at human androgen receptor by luciferase reporter gene assay | F | 8.29 | pEC50 | 5.1 | nM | EC50 | J Med Chem (2007) 50: 5049-5052 [PMID:17887661] |
| ChEMBL | Agonist activity at human AR | F | 8.29 | pEC50 | 5.1 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 1527-1531 [PMID:17267219] |
| ChEMBL | Agonist activity against Human Androgen receptor expressed in CV-1 cells | F | 8.3 | pEC50 | 5 | nM | EC50 | J Med Chem (1999) 42: 210-212 [PMID:9925725] |
| ChEMBL | Agonist activity at human AR expressed in African green monkey COS7 cells after 24 hrs by luciferase reporter gene assay | B | 8.52 | pEC50 | 3 | nM | EC50 | Bioorg Med Chem (2017) 25: 3330-3349 [PMID:28454849] |
| ChEMBL | Agonist activity at androgen receptor in human MDA-MB-453 cells transfected with MMTV-LUC assessed as induction of MMTV-LTR/promoter linked LUC gene by luciferase transactivation assay | F | 8.7 | pEC50 | 2 | nM | EC50 | J Med Chem (2009) 52: 4578-4581 [PMID:19606870] |
| ChEMBL | Agonist activity at human androgen receptor expressed in HEK293 cells by luciferase reporter gene assay | B | 9.74 | pEC50 | 0.18 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 5265-5267 [PMID:25305688] |
| ChEMBL | Agonist activity at human androgen receptor expressed in mouse C2C12 cells by androgen-specific response element-driven luciferase reporter gene assay | B | 9.89 | pEC50 | 0.13 | nM | EC50 | J Med Chem (2014) 57: 7396-7411 [PMID:25121964] |
| ChEMBL | Agonist activity at androgen receptor expressed in mouse C2C12 cells assessed as osteoblast differentiation after 5 days | F | 10.3 | pEC50 | 0.05 | nM | EC50 | ACS Med Chem Lett (2011) 2: 124-129 [PMID:24900290] |
| Androgen receptor/Androgen Receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3056] [GtoPdb: 628] [UniProtKB: P19091] | ||||||||
| ChEMBL | Displacement of [3H] ]5alpha-DHT from mouse androgen receptor expressed in monkey COS7 cells after 2 hrs by scintillation counting analysis | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2013) 56: 3414-3418 [PMID:23527816] |
| 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 | 8.4 | pEC50 | 3.98 | 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 | DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone) | B | 8.81 | pKi | 1.54 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | Inhibitory constant against rat prostate cytosol androgen receptor using [3H]mibolerone | B | 9.16 | pKi | 0.69 | nM | Ki | J Med Chem (2000) 43: 3344-3347 [PMID:10966753] |
| ChEMBL | Inhibition of [3H]mibolerone binding to cytosolic androgen receptor of rat ventral prostate | B | 9.55 | pKi | 0.28 | nM | Ki | J Med Chem (2005) 48: 917-925 [PMID:15715462] |
| ChEMBL | Binding affinity to rat androgen receptor by competitive inhibition assay | B | 9.57 | pKi | 0.27 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 5567-5570 [PMID:18805694] |
| ChEMBL | Ability to inhibit binding of [3H]R-1881 to rat ventral prostate cytosolic androgen receptor was measured in a radioligand binding assay. | B | 5.49 | pIC50 | 3200 | nM | IC50 | J Med Chem (2000) 43: 4629-4635 [PMID:11101354] |
| ChEMBL | Displacement of androgen fluormone from rat androgen receptor | B | 7.73 | pIC50 | 18.5 | nM | IC50 | J Med Chem (2006) 49: 7366-7372 [PMID:17149866] |
| ChEMBL | Displacement of [3H]testosterone from Sprague-Dawley rat AR by liquid scintillation counting | B | 8.51 | pIC50 | 3.1 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1744-1747 [PMID:21349712] |
| ChEMBL | Competitive binding affinity to rat androgen receptor | B | 8.51 | pIC50 | 3.1 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6310-6313 [PMID:21944856] |
| ChEMBL | DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone) | B | 8.64 | pIC50 | 2.31 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| ChEMBL | Inhibitory concentration against recombinant rat androgen receptor expressed in Escherichia coli using [3H]methyltrienolone (R 1881) | B | 8.65 | pIC50 | 2.24 | nM | IC50 | J Med Chem (2005) 48: 5666-5674 [PMID:16134935] |
| GtoPdb | - | - | 8.65 | pIC50 | - | - | - | Chem Res Toxicol (2003) 16: 1338-58 [PMID:14565775] |
| ChEMBL | In vitro antagonist activity against rat prostatic androgen receptor (AR) | F | 8.66 | pIC50 | 2.2 | nM | IC50 | J Med Chem (1986) 29: 2298-2315 [PMID:3783591] |
| ChEMBL | Displacement of [3H]testosterone from androgen receptor in Sprague-Dawley rat prostate gland after 2 hrs by liquid scintillation counting | B | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6310-6313 [PMID:21944856] |
| ChEMBL | Displacement of [3H]-MIB from wild-type rat AR LBD measured after 16 hrs by scintillation counting method | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2020) 63: 12642-12665 [PMID:33095584] |
| ChEMBL | Agonist activity at rat AR transfected in mouse C2C12 cells by luciferase reporter transactivation assay | F | 8.55 | pEC50 | 2.8 | nM | EC50 | J Med Chem (2006) 49: 7596-7599 [PMID:17181141] |
| ChEMBL | Agonist activity at rat androgen receptor | F | 9.01 | pEC50 | 0.97 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 6310-6313 [PMID:21944856] |
| Corticosteroid binding globulin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2421] [UniProtKB: P08185] | ||||||||
| ChEMBL | In silico binding affinity to human corticosteriod binding globulin | B | 4.92 | pKd | 4.92 | - | -Log Kdiss | J Med Chem (1997) 40: 3161-3172 [PMID:9379435] |
| ChEMBL | Binding affinity to human CBG receptor (corticosteroid-binding globulins) | B | 5.92 | pKi | 1202.26 | 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 | Inactivation rate (Ki) for human placental Cytochrome P450 19A1 | B | 5.81 | pKi | 1550 | nM | Ki | J Med Chem (1989) 32: 651-658 [PMID:2918514] |
| ChEMBL | Competitive inhibition of binding to human placental Cytochrome P450 19A1 | B | 6.66 | pKi | 220 | nM | Ki | J Med Chem (1989) 32: 651-658 [PMID:2918514] |
| Glucocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150] | ||||||||
| ChEMBL | Binding affinity to GR (unknown origin) | B | 6.27 | pIC50 | 540 | nM | IC50 | Bioorg Med Chem (2017) 25: 3330-3349 [PMID:28454849] |
| Glucocorticoid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3368] [GtoPdb: 625] [UniProtKB: P06536] | ||||||||
| ChEMBL | Displacement of [3H]dexamethasone from Sprague-Dawley rat GR by liquid scintillation counting | B | 4.7 | pIC50 | 20000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1744-1747 [PMID:21349712] |
| ChEMBL | Displacement of [3H]Dex from glucocorticoid receptor in Sprague-Dawley rat liver after 2 hrs by liquid scintillation counting | B | 4.7 | pIC50 | 20000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6310-6313 [PMID:21944856] |
| 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 | 5.35 | pEC50 | 4490 | nM | EC50 | J Med Chem (2008) 51: 1831-1841 [PMID:18307294] |
| Mineralocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1994] [GtoPdb: 626] [UniProtKB: P08235] | ||||||||
| ChEMBL | Binding affinity to MR (unknown origin) | B | 6.44 | pIC50 | 360 | nM | IC50 | Bioorg Med Chem (2017) 25: 3330-3349 [PMID:28454849] |
| Mineralocorticoid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3507] [GtoPdb: 626] [UniProtKB: P22199] | ||||||||
| ChEMBL | Displacement of [3H]aldosterone from Sprague-Dawley rat MR by liquid scintillation counting | B | 5.68 | pIC50 | 2100 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1744-1747 [PMID:21349712] |
| ChEMBL | Displacement of [3H]Aldo from mineralocorticoid receptor in Sprague-Dawley rat kidney after 2 hrs by liquid scintillation counting | B | 5.68 | pIC50 | 2100 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6310-6313 [PMID:21944856] |
| Progesterone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL208] [GtoPdb: 627] [UniProtKB: P06401] | ||||||||
| ChEMBL | Binding affinity to PR (unknown origin) | B | 5.14 | pIC50 | 7300 | nM | IC50 | Bioorg Med Chem (2017) 25: 3330-3349 [PMID:28454849] |
| ChEMBL | Agonist activity at PR (unknown origin) by luciferase reporter gene assay | B | 5.09 | pEC50 | 8200 | nM | EC50 | Bioorg Med Chem (2017) 25: 3330-3349 [PMID:28454849] |
| Progesterone receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1909044] [UniProtKB: Q690N0] | ||||||||
| ChEMBL | DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) | B | 6.79 | pKi | 163 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) | B | 5.9 | pIC50 | 1247 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Progesterone receptor in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3456] [UniProtKB: P06186] | ||||||||
| ChEMBL | Displacement of [3H]progesterone from rabbit PR by liquid scintillation counting | B | 6.36 | pIC50 | 440 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1744-1747 [PMID:21349712] |
| ChEMBL | Displacement of [3H]progesterone from progesterone receptor in JW rabbit uterus after 2 hrs by liquid scintillation counting | B | 6.36 | pIC50 | 440 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6310-6313 [PMID:21944856] |
| Testis-specific androgen-binding protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3305] [UniProtKB: P04278] | ||||||||
| ChEMBL | Binding affinity towards human testosterone binding globulin. | B | 8.74 | pKd | 8.74 | - | -Log Kdiss | J Med Chem (1997) 40: 3161-3172 [PMID:9379435] |
| ChEMBL | Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | B | 9.74 | pKd | 0.18 | nM | Kd | J Med Chem (2008) 51: 2047-2056 [PMID:18330978] |
| ChEMBL | Inhibition of hSHBG (human sex hormone binding globulin ) | F | 8.42 | pIC50 | 3.8 | nM | IC50 | J Med Chem (1990) 33: 129-132 [PMID:2296011] |
| Testis-specific androgen-binding protein in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4932] [UniProtKB: P08689] | ||||||||
| ChEMBL | Inhibition of rat androgen binding protein (rABP) | F | 7.64 | pIC50 | 23 | nM | IC50 | J Med Chem (1990) 33: 129-132 [PMID:2296011] |
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]
