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), 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 | Binding affinity to human Androgen receptor | B | 9.6 | pKd | 0.25 | 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 | 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 | 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 (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 | 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 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 | J Med Chem (2007) 50: 2486-2496 [PMID:17439112] |
| 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 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 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 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 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 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 | Modulation of Androgen receptor (unknown origin) | B | 9.85 | pEC50 | 0.14 | nM | EC50 | Eur J Med Chem (2022) 230: 114119-114119 [PMID:35063736] |
| 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 human Androgen receptor measured by CALUX bioassay | B | 10 | pEC50 | 0.1 | nM | EC50 | J Med Chem (2022) 65: 8772-8797 [PMID:35786895] |
| 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 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]
