Page last updated: 2024-08-07 15:41:48
Progesterone receptor
A progesterone receptor that is encoded in the genome of human. [PRO:DNx, UniProtKB:P06401]
Synonyms
PR;
Nuclear receptor subfamily 3 group C member 3
Research
Bioassay Publications (94)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 10 (10.64) | 18.2507 |
2000's | 45 (47.87) | 29.6817 |
2010's | 35 (37.23) | 24.3611 |
2020's | 4 (4.26) | 2.80 |
Compounds (43)
Drugs with Inhibition Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
bicalutamide | Homo sapiens (human) | IC50 | 1.8190 | 1 | 1 |
raloxifene | Homo sapiens (human) | IC50 | 0.1000 | 1 | 1 |
prednisolone | Homo sapiens (human) | IC50 | 6.0133 | 6 | 6 |
prednisolone | Homo sapiens (human) | Ki | 5.4286 | 7 | 7 |
spironolactone | Homo sapiens (human) | IC50 | 3.3400 | 5 | 5 |
spironolactone | Homo sapiens (human) | Ki | 0.3997 | 1 | 1 |
norethindrone | Homo sapiens (human) | IC50 | 0.0032 | 1 | 1 |
norethindrone | Homo sapiens (human) | Ki | 0.0019 | 1 | 1 |
medroxyprogesterone acetate | Homo sapiens (human) | IC50 | 2.5081 | 4 | 4 |
medroxyprogesterone acetate | Homo sapiens (human) | Ki | 0.0005 | 8 | 8 |
cyproterone acetate | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
dihydrotestosterone | Homo sapiens (human) | IC50 | 7.3000 | 1 | 1 |
promegestone | Homo sapiens (human) | IC50 | 0.0002 | 1 | 1 |
mifepristone | Homo sapiens (human) | IC50 | 0.1347 | 42 | 45 |
mifepristone | Homo sapiens (human) | Ki | 0.0045 | 13 | 13 |
4-[1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenylbut-1-enyl]phenol | Homo sapiens (human) | IC50 | 50.0004 | 2 | 2 |
hydroxyflutamide | Homo sapiens (human) | IC50 | 2.0130 | 1 | 1 |
fulvestrant | Homo sapiens (human) | IC50 | 50.0001 | 2 | 2 |
ulipristal acetate | Homo sapiens (human) | IC50 | 0.0002 | 1 | 1 |
ru 58841 | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
metribolone | Homo sapiens (human) | Ki | 0.0005 | 1 | 1 |
eplerenone | Homo sapiens (human) | IC50 | 12.0000 | 5 | 5 |
eplerenone | Homo sapiens (human) | Ki | 19.9526 | 1 | 1 |
fluticasone propionate | Homo sapiens (human) | IC50 | 0.0210 | 1 | 1 |
tamoxifen | Homo sapiens (human) | IC50 | 50.0644 | 2 | 2 |
tanaproget | Homo sapiens (human) | IC50 | 0.0005 | 1 | 1 |
pulmicort | Homo sapiens (human) | IC50 | 0.0280 | 1 | 1 |
baicalein | Homo sapiens (human) | IC50 | 15.0000 | 1 | 1 |
afimoxifene | Homo sapiens (human) | IC50 | 0.1000 | 1 | 1 |
gw 5638 | Homo sapiens (human) | IC50 | 51.9905 | 2 | 2 |
onapristone | Homo sapiens (human) | IC50 | 0.0026 | 6 | 6 |
onapristone | Homo sapiens (human) | Ki | 0.0180 | 5 | 5 |
pregna-4,17-diene-3,16-dione | Homo sapiens (human) | IC50 | 50.6000 | 2 | 2 |
pregna-4,17-diene-3,16-dione | Homo sapiens (human) | Ki | 0.2010 | 1 | 1 |
pregna-4,17-diene-3,16-dione, (17z)-isomer | Homo sapiens (human) | IC50 | 0.7400 | 1 | 1 |
pregna-4,17-diene-3,16-dione, (17z)-isomer | Homo sapiens (human) | Ki | 0.2240 | 1 | 1 |
lonaprisan | Homo sapiens (human) | IC50 | 0.0000 | 2 | 2 |
asoprisnil | Homo sapiens (human) | IC50 | 0.0003 | 3 | 3 |
gw 7604 | Homo sapiens (human) | IC50 | 15.8174 | 2 | 2 |
zk 216348 | Homo sapiens (human) | IC50 | 0.0195 | 2 | 2 |
fluticasone furoate | Homo sapiens (human) | IC50 | 0.0210 | 1 | 1 |
way-362450 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
metapristone | Homo sapiens (human) | IC50 | 0.0001 | 3 | 3 |
lgd 2226 | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
way 252623 | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
pf 998425 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
pf-03882845 | Homo sapiens (human) | IC50 | 0.4160 | 2 | 2 |
bay 94-8862 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
azd9496 | Homo sapiens (human) | IC50 | 0.9284 | 4 | 4 |
Drugs with Activation Measurements
Drugs with Other Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
prednisolone | Homo sapiens (human) | Activity | 5.0000 | 1 | 1 |
mifepristone | Homo sapiens (human) | Activity | 0.0013 | 1 | 1 |
mifepristone | Homo sapiens (human) | Kif | 0.0118 | 1 | 1 |
Discovery of a subnanomolar and selective spirocyclic agonist of the glucocorticoid receptor.European journal of medicinal chemistry, , Jan-01, Volume: 161, 2019
Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile.Journal of medicinal chemistry, , 03-08, Volume: 61, Issue:5, 2018
Discovery of indazole ethers as novel, potent, non-steroidal glucocorticoid receptor modulators.Bioorganic & medicinal chemistry letters, , 12-01, Volume: 26, Issue:23, 2016
Discovery of a potent and dissociated non-steroidal glucocorticoid receptor agonist containing an alkyl carbinol pharmacophore.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 24, Issue:8, 2014
Glucocorticoid receptor modulators informed by crystallography lead to a new rationale for receptor selectivity, function, and implications for structure-based design.Journal of medicinal chemistry, , Feb-13, Volume: 57, Issue:3, 2014
Azaxanthene based selective glucocorticoid receptor modulators: design, synthesis, and pharmacological evaluation of (S)-4-(5-(1-((1,3,4-thiadiazol-2-yl)amino)-2-methyl-1-oxopropan-2-yl)-5H-chromeno[2,3-b]pyridin-2-yl)-2-fluoro-N,N-dimethylbenzamide (BMS-Journal of medicinal chemistry, , Oct-27, Volume: 54, Issue:20, 2011
Non-steroidal dissociated glucocorticoid agonists: indoles as A-ring mimetics and function-regulating pharmacophores.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 21, Issue:22, 2011
Dimethyl-diphenyl-propanamide derivatives as nonsteroidal dissociated glucocorticoid receptor agonists.Journal of medicinal chemistry, , Dec-09, Volume: 53, Issue:23, 2010
Nonsteroidal dissociated glucocorticoid agonists containing azaindoles as steroid A-ring mimetics.Journal of medicinal chemistry, , Sep-23, Volume: 53, Issue:18, 2010
Discovery of nonsteroidal glucocorticoid receptor ligands based on 6-indole-1,2,3,4-tetrahydroquinolines.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 18, Issue:12, 2008
Differentiation of in vitro transcriptional repression and activation profiles of selective glucocorticoid modulators.Bioorganic & medicinal chemistry letters, , Apr-05, Volume: 14, Issue:7, 2004
Nonsteroidal selective glucocorticoid modulators: the effect of C-10 substitution on receptor selectivity and functional potency of 5-allyl-2,5-dihydro-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines.Journal of medicinal chemistry, , Mar-13, Volume: 46, Issue:6, 2003
Synthesis and characterization of non-steroidal ligands for the glucocorticoid receptor: selective quinoline derivatives with prednisolone-equivalent functional activity.Journal of medicinal chemistry, , Aug-30, Volume: 44, Issue:18, 2001
Nonsteroidal selective glucocorticoid modulators: the effect of C-5 alkyl substitution on the transcriptional activation/repression profile of 2,5-dihydro-10-methoxy-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines.Journal of medicinal chemistry, , Dec-06, Volume: 44, Issue:25, 2001
Discovery of 6-[5-(4-fluorophenyl)-3-methyl-pyrazol-4-yl]-benzoxazin-3-one derivatives as novel selective nonsteroidal mineralocorticoid receptor antagonists.Bioorganic & medicinal chemistry, , Oct-01, Volume: 22, Issue:19, 2014
Discovery of novel oxazolidinedione derivatives as potent and selective mineralocorticoid receptor antagonists.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 23, Issue:15, 2013
Identification of benzoxazin-3-one derivatives as novel, potent, and selective nonsteroidal mineralocorticoid receptor antagonists.Journal of medicinal chemistry, , Dec-22, Volume: 54, Issue:24, 2011
Discovery of (3S,3aR)-2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydro-2H-benzo[g]indazole-7-carboxylic acid (PF-3882845), an orally efficacious mineralocorticoid receptor (MR) antagonist for hypertension and nephropathy.Journal of medicinal chemistry, , Aug-26, Volume: 53, Issue:16, 2010
(S)-N-{3-[1-cyclopropyl-1-(2,4-difluoro-phenyl)-ethyl]-1H-indol-7-yl}-methanesulfonamide: a potent, nonsteroidal, functional antagonist of the mineralocorticoid receptor.Journal of medicinal chemistry, , Dec-27, Volume: 50, Issue:26, 2007
Progesterone receptor ligand binding pocket flexibility: crystal structures of the norethindrone and mometasone furoate complexes.Journal of medicinal chemistry, , Jun-17, Volume: 47, Issue:13, 2004
5-Aryl-1,2-dihydro-5H-chromeno[3,4-f]quinolines as potent, orally active, nonsteroidal progesterone receptor agonists: the effect of D-ring substituents.Journal of medicinal chemistry, , Jan-29, Volume: 41, Issue:3, 1998
Nonsteroidal progesterone receptor ligands. 2. High-affinity ligands with selectivity for bone cell progesterone receptors.Journal of medicinal chemistry, , Dec-08, Volume: 38, Issue:25, 1995
A tissue-selective nonsteroidal progesterone receptor modulator: 7,9-difluoro-5-(3-methylcyclohex-2-enyl)-2,2,4-trimethyl-1,2-dihydrochromeno[3,4-f]quinoline.Journal of medicinal chemistry, , Jul-10, Volume: 51, Issue:13, 2008
Docking and three-dimensional quantitative structure-activity relationship (3D QSAR) analyses of nonsteroidal progesterone receptor ligands.Journal of medicinal chemistry, , Jul-13, Volume: 49, Issue:14, 2006
Novel pyrrole-containing progesterone receptor modulators.Bioorganic & medicinal chemistry letters, , May-03, Volume: 14, Issue:9, 2004
Novel 6-aryl-1,4-dihydrobenzo[d]oxazine-2-thiones as potent, selective, and orally active nonsteroidal progesterone receptor agonists.Bioorganic & medicinal chemistry letters, , Apr-07, Volume: 13, Issue:7, 2003
Novel 5-aryl-1,3-dihydro-indole-2-thiones. potent, orally active progesterone receptor agonists.Bioorganic & medicinal chemistry letters, , Apr-07, Volume: 13, Issue:7, 2003
5-benzylidene-1,2-dihydrochromeno[3,4-f]quinolines as selective progesterone receptor modulators.Journal of medicinal chemistry, , Sep-11, Volume: 46, Issue:19, 2003
Potent nonsteroidal progesterone receptor agonists: synthesis and SAR study of 6-aryl benzoxazines.Bioorganic & medicinal chemistry letters, , Mar-11, Volume: 12, Issue:5, 2002
5-Aryl-1,2,3,4-tetrahydrochromeno[3,4-f]quinolin-3-ones as a novel class of nonsteroidal progesterone receptor agonists: effect of A-ring modification.Journal of medicinal chemistry, , Apr-22, Volume: 42, Issue:8, 1999
5-Alkyl 1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal progesterone receptor modulators.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 8, Issue:23, 1998
5-Benzylidene 1,2-dihydrochromeno[3,4-f]quinolines, a novel class of nonsteroidal human progesterone receptor agonists.Journal of medicinal chemistry, , Oct-22, Volume: 41, Issue:22, 1998
5-Aryl-1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal human progesterone receptor agonists.Journal of medicinal chemistry, , Jan-29, Volume: 41, Issue:3, 1998
5-Aryl-1,2-dihydro-5H-chromeno[3,4-f]quinolines as potent, orally active, nonsteroidal progesterone receptor agonists: the effect of D-ring substituents.Journal of medicinal chemistry, , Jan-29, Volume: 41, Issue:3, 1998
Discovery of (Journal of medicinal chemistry, , 07-28, Volume: 65, Issue:14, 2022
Discovery of a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (OP-3633).Journal of medicinal chemistry, , 07-25, Volume: 62, Issue:14, 2019
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).Journal of medicinal chemistry, , 09-13, Volume: 61, Issue:17, 2018
Novel Nonsteroidal Progesterone Receptor (PR) Antagonists with a Phenanthridinone Skeleton.ACS medicinal chemistry letters, , Jul-12, Volume: 9, Issue:7, 2018
Indole Glucocorticoid Receptor Antagonists Active in a Model of Dyslipidemia Act via a Unique Association with an Agonist Binding Site.Journal of medicinal chemistry, , Aug-27, Volume: 58, Issue:16, 2015
Synthesis and Biological Evaluation of Cyclopentaquinoline Derivatives as Nonsteroidal Glucocorticoid Receptor Antagonists.Journal of medicinal chemistry, , Jun-25, Volume: 58, Issue:12, 2015
Lead diversification. Application to existing drug molecules: mifepristone 1 and antalarmin 8.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
Structure guided design of 5-arylindazole glucocorticoid receptor agonists and antagonists.Journal of medicinal chemistry, , Jun-10, Volume: 53, Issue:11, 2010
1-Methyl-1H-pyrrole-2-carbonitrile containing tetrahydronaphthalene derivatives as non-steroidal progesterone receptor antagonists.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 20, Issue:16, 2010
Synthesis, in vitro progesterone receptors affinity of gadolinium containing mifepristone conjugates and estimation of binding sites in human breast cancer cells.Bioorganic & medicinal chemistry, , Mar-01, Volume: 18, Issue:5, 2010
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.Bioorganic & medicinal chemistry, , Jun-15, Volume: 18, Issue:12, 2010
Synthesis and SAR study of novel pseudo-steroids as potent and selective progesterone receptor antagonists.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 19, Issue:14, 2009
Syntheses and antigestagenic activity of mifepristone derivatives.Journal of medicinal chemistry, , Mar-12, Volume: 52, Issue:5, 2009
7-aryl 1,5-dihydro-benzo[e][1,4]oxazepin-2-ones and analogs as non-steroidal progesterone receptor antagonists.Bioorganic & medicinal chemistry, , Jul-01, Volume: 16, Issue:13, 2008
1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as selective glucocorticoid receptor antagonists with high functional activity.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 18, Issue:4, 2008
Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
1,5-Dihydro-benzo[e][1,4]oxazepin-2(1H)-ones containing a 7-(5'-cyanopyrrol-2-yl) group as nonsteroidal progesterone receptor modulators.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 18, Issue:18, 2008
Synthesis and identification of novel oxa-steroids as progesterone receptor antagonists.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 17, Issue:4, 2007
Synthesis and identification of novel 11beta-aryl-4',5'-dihydrospiro[estra-4,9-diene-17beta,4'-oxazole] analogs with dissociated antiprogesterone activities.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 17, Issue:21, 2007
Discovery of novel phosphorus-containing steroids as selective glucocorticoid receptor antagonist.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 17, Issue:5, 2007
Parallel synthesis and SAR study of novel oxa-steroids as potent and selective progesterone receptor antagonists.Bioorganic & medicinal chemistry letters, , May-01, Volume: 17, Issue:9, 2007
Array synthesis of progesterone receptor antagonists: 3-aryl-1,2-diazepines.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 16, Issue:14, 2006
Discovery of non-steroidal mifepristone mimetics: pyrazoline-based PR antagonists.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 15, Issue:13, 2005
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.Journal of medicinal chemistry, , Aug-11, Volume: 48, Issue:16, 2005
Synthesis, activity, metabolic stability, and pharmacokinetics of glucocorticoid receptor modulator-statin hybrids.Bioorganic & medicinal chemistry letters, , Aug-16, Volume: 14, Issue:16, 2004
Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.Journal of medicinal chemistry, , Aug-12, Volume: 47, Issue:17, 2004
Synthesis and biological evaluation of novel, selective, nonsteroidal glucocorticoid receptor antagonists.Bioorganic & medicinal chemistry letters, , May-03, Volume: 14, Issue:9, 2004
Synthesis and biological activity of 5-methylidene 1,2-dihydrochromeno[3,4-f]quinoline derivatives as progesterone receptor modulators.Bioorganic & medicinal chemistry letters, , Jun-16, Volume: 13, Issue:12, 2003
Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore.Bioorganic & medicinal chemistry letters, , Jun-16, Volume: 13, Issue:12, 2003
Potent nonsteroidal progesterone receptor agonists: synthesis and SAR study of 6-aryl benzoxazines.Bioorganic & medicinal chemistry letters, , Mar-11, Volume: 12, Issue:5, 2002
6-Aryl-1,4-dihydro-benzo[d][1,3]oxazin- 2-ones: a novel class of potent, selective, and orally active nonsteroidal progesterone receptor antagonists.Journal of medicinal chemistry, , Sep-26, Volume: 45, Issue:20, 2002
New progesterone receptor antagonists: 3,3-disubstituted-5-aryloxindoles.Bioorganic & medicinal chemistry letters, , Dec-02, Volume: 12, Issue:23, 2002
Discovery of potent, nonsteroidal, and highly selective glucocorticoid receptor antagonists.Journal of medicinal chemistry, , Jun-06, Volume: 45, Issue:12, 2002
Synthesis and progesterone receptor antagonist activities of 6-aryl benzimidazolones and benzothiazolones.Bioorganic & medicinal chemistry letters, , Oct-22, Volume: 11, Issue:20, 2001
Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist.Journal of medicinal chemistry, , Dec-28, Volume: 43, Issue:26, 2000
Synthesis and biological activity of a novel series of nonsteroidal, peripherally selective androgen receptor antagonists derived from 1,2-dihydropyridono[5,6-g]quinolines.Journal of medicinal chemistry, , Feb-12, Volume: 41, Issue:4, 1998
Discovery and preliminary SAR studies of a novel, nonsteroidal progesterone receptor antagonist pharmacophore.Journal of medicinal chemistry, , Aug-27, Volume: 41, Issue:18, 1998
Nonsteroidal progesterone receptor antagonists based on a conformationally-restricted subseries of 6-aryl-1,2-dihydro-2,2,4-trimethylquinolines.Bioorganic & medicinal chemistry letters, , Oct-06, Volume: 8, Issue:19, 1998
Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether.Journal of medicinal chemistry, , Apr-26, Volume: 39, Issue:9, 1996
Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor DownreguJournal of medicinal chemistry, , Oct-22, Volume: 58, Issue:20, 2015
Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor DownreguJournal of medicinal chemistry, , Oct-22, Volume: 58, Issue:20, 2015
[no title available]Journal of medicinal chemistry, , 02-14, Volume: 62, Issue:3, 2019
Discovery of 6-[5-(4-fluorophenyl)-3-methyl-pyrazol-4-yl]-benzoxazin-3-one derivatives as novel selective nonsteroidal mineralocorticoid receptor antagonists.Bioorganic & medicinal chemistry, , Oct-01, Volume: 22, Issue:19, 2014
Discovery of novel oxazolidinedione derivatives as potent and selective mineralocorticoid receptor antagonists.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 23, Issue:15, 2013
Identification of benzoxazin-3-one derivatives as novel, potent, and selective nonsteroidal mineralocorticoid receptor antagonists.Journal of medicinal chemistry, , Dec-22, Volume: 54, Issue:24, 2011
Discovery of (3S,3aR)-2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydro-2H-benzo[g]indazole-7-carboxylic acid (PF-3882845), an orally efficacious mineralocorticoid receptor (MR) antagonist for hypertension and nephropathy.Journal of medicinal chemistry, , Aug-26, Volume: 53, Issue:16, 2010
Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor DownreguJournal of medicinal chemistry, , Oct-22, Volume: 58, Issue:20, 2015
Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor DownreguJournal of medicinal chemistry, , Oct-22, Volume: 58, Issue:20, 2015
Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore.Bioorganic & medicinal chemistry letters, , Jun-16, Volume: 13, Issue:12, 2003
Nonsteroidal progesterone receptor antagonists based on 6-thiophenehydroquinolines.Bioorganic & medicinal chemistry letters, , Mar-06, Volume: 10, Issue:5, 2000
5-Alkyl 1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal progesterone receptor modulators.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 8, Issue:23, 1998
Discovery and preliminary SAR studies of a novel, nonsteroidal progesterone receptor antagonist pharmacophore.Journal of medicinal chemistry, , Aug-27, Volume: 41, Issue:18, 1998
Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether.Journal of medicinal chemistry, , Apr-26, Volume: 39, Issue:9, 1996
Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool.MedChemComm, , Aug-01, Volume: 10, Issue:8, 2019
Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 2005
Novel progesterone receptor modulators: 4-aryl-phenylsulfonamides.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 22, Issue:23, 2012
11-(pyridinylphenyl)steroids--a new class of mixed-profile progesterone agonists/antagonists.Bioorganic & medicinal chemistry, , Mar-15, Volume: 16, Issue:6, 2008
Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor DownreguJournal of medicinal chemistry, , Oct-22, Volume: 58, Issue:20, 2015
Discovery of quinolines as selective glucocorticoid receptor agonists.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 20, Issue:19, 2010
Quinol-4-ones as steroid A-ring mimetics in nonsteroidal dissociated glucocorticoid agonists.Journal of medicinal chemistry, , Dec-28, Volume: 49, Issue:26, 2006
Synthesis, in vitro progesterone receptors affinity of gadolinium containing mifepristone conjugates and estimation of binding sites in human breast cancer cells.Bioorganic & medicinal chemistry, , Mar-01, Volume: 18, Issue:5, 2010
Syntheses and antigestagenic activity of mifepristone derivatives.Journal of medicinal chemistry, , Mar-12, Volume: 52, Issue:5, 2009
Identification of (R)-6-(1-(4-cyano-3-methylphenyl)-5-cyclopentyl-4,5-dihydro-1H-pyrazol-3-yl)-2-methoxynicotinic acid, a highly potent and selective nonsteroidal mineralocorticoid receptor antagonist.Journal of medicinal chemistry, , May-22, Volume: 57, Issue:10, 2014
Discovery of (3S,3aR)-2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydro-2H-benzo[g]indazole-7-carboxylic acid (PF-3882845), an orally efficacious mineralocorticoid receptor (MR) antagonist for hypertension and nephropathy.Journal of medicinal chemistry, , Aug-26, Volume: 53, Issue:16, 2010
Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor DownreguJournal of medicinal chemistry, , Oct-22, Volume: 58, Issue:20, 2015
Enables
This protein enables 15 target(s):
Target | Category | Definition |
RNA polymerase II cis-regulatory region sequence-specific DNA binding | molecular function | Binding to a specific upstream regulatory DNA sequence (transcription factor recognition sequence or binding site) located in cis relative to the transcription start site (i.e., on the same strand of DNA) of a gene transcribed by RNA polymerase II. [GOC:txnOH-2018] |
DNA-binding transcription factor activity, RNA polymerase II-specific | molecular function | A DNA-binding transcription factor activity that modulates the transcription of specific gene sets transcribed by RNA polymerase II. [GOC:txnOH-2018] |
transcription coactivator binding | molecular function | Binding to a transcription coactivator, a protein involved in positive regulation of transcription via protein-protein interactions with transcription factors and other proteins that positively regulate transcription. Transcription coactivators do not bind DNA directly, but rather mediate protein-protein interactions between activating transcription factors and the basal transcription machinery. [GOC:krc] |
DNA-binding transcription activator activity, RNA polymerase II-specific | molecular function | A DNA-binding transcription factor activity that activates or increases transcription of specific gene sets transcribed by RNA polymerase II. [GOC:aruk, GOC:txnOH-2018, PMID:20737563, PMID:27145859] |
DNA binding | molecular function | Any molecular function by which a gene product interacts selectively and non-covalently with DNA (deoxyribonucleic acid). [GOC:dph, GOC:jl, GOC:tb, GOC:vw] |
nuclear steroid receptor activity | molecular function | Combining with a steroid hormone and transmitting the signal within the cell to initiate a change in cell activity or function. [GOC:signaling, PMID:14708019] |
G protein-coupled receptor activity | molecular function | Combining with an extracellular signal and transmitting the signal across the membrane by activating an associated G-protein; promotes the exchange of GDP for GTP on the alpha subunit of a heterotrimeric G-protein complex. [GOC:bf, http://www.iuphar-db.org, Wikipedia:GPCR] |
steroid binding | molecular function | Binding to a steroid, any of a large group of substances that have in common a ring system based on 1,2-cyclopentanoperhydrophenanthrene. [GOC:jl, ISBN:0198506732] |
protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
zinc ion binding | molecular function | Binding to a zinc ion (Zn). [GOC:ai] |
enzyme binding | molecular function | Binding to an enzyme, a protein with catalytic activity. [GOC:jl] |
identical protein binding | molecular function | Binding to an identical protein or proteins. [GOC:jl] |
ATPase binding | molecular function | Binding to an ATPase, any enzyme that catalyzes the hydrolysis of ATP. [GOC:ai] |
estrogen response element binding | molecular function | Binding to an estrogen response element (ERE), a conserved sequence found in the promoters of genes whose expression is regulated in response to estrogen. [GOC:ecd, PMID:15036253, PMID:17975005] |
nuclear receptor activity | molecular function | A DNA-binding transcription factor activity regulated by binding to a ligand that modulates the transcription of specific gene sets transcribed by RNA polymerase II. Nuclear receptor ligands are usually lipid-based (such as a steroid hormone) and the binding of the ligand to its receptor often occurs in the cytosol, which leads to its translocation to the nucleus. [GOC:txnOH-2018, PMID:23457262] |
Located In
This protein is located in 3 target(s):
Target | Category | Definition |
nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
mitochondrial outer membrane | cellular component | The outer, i.e. cytoplasm-facing, lipid bilayer of the mitochondrial envelope. [GOC:ai] |
cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
Active In
This protein is active in 2 target(s):
Target | Category | Definition |
plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
Part Of
This protein is part of 1 target(s):
Target | Category | Definition |
chromatin | cellular component | The ordered and organized complex of DNA, protein, and sometimes RNA, that forms the chromosome. [GOC:elh, PMID:20404130] |
Involved In
This protein is involved in 18 target(s):
Target | Category | Definition |
ovulation from ovarian follicle | biological process | The process leading to the rupture of the follicle, releasing the centrally located oocyte into the oviduct. An example of this is found in Mus musculus. [GOC:mtg_sensu, https://www.ncbi.nlm.nih.gov/books/NBK279054/] |
glandular epithelial cell maturation | biological process | The developmental process, independent of morphogenetic (shape) change, that is required for a glandular epithelial cell to attain its fully functional state. A glandular epithelial cell is a columnar/cuboidal epithelial cell is a cell found in a two dimensional sheet with a free surface exposed to the lumen of a gland. [GOC:dph] |
regulation of DNA-templated transcription | biological process | Any process that modulates the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH] |
signal transduction | biological process | The cellular process in which a signal is conveyed to trigger a change in the activity or state of a cell. Signal transduction begins with reception of a signal (e.g. a ligand binding to a receptor or receptor activation by a stimulus such as light), or for signal transduction in the absence of ligand, signal-withdrawal or the activity of a constitutively active receptor. Signal transduction ends with regulation of a downstream cellular process, e.g. regulation of transcription or regulation of a metabolic process. Signal transduction covers signaling from receptors located on the surface of the cell and signaling via molecules located within the cell. For signaling between cells, signal transduction is restricted to events at and within the receiving cell. [GOC:go_curators, GOC:mtg_signaling_feb11] |
G protein-coupled receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to its receptor, in which the activated receptor promotes the exchange of GDP for GTP on the alpha-subunit of an associated heterotrimeric G-protein complex. The GTP-bound activated alpha-G-protein then dissociates from the beta- and gamma-subunits to further transmit the signal within the cell. The pathway begins with receptor-ligand interaction, and ends with regulation of a downstream cellular process. The pathway can start from the plasma membrane, Golgi or nuclear membrane. [GOC:bf, GOC:mah, PMID:16902576, PMID:24568158, Wikipedia:G_protein-coupled_receptor] |
cell-cell signaling | biological process | Any process that mediates the transfer of information from one cell to another. This process includes signal transduction in the receiving cell and, where applicable, release of a ligand and any processes that actively facilitate its transport and presentation to the receiving cell. Examples include signaling via soluble ligands, via cell adhesion molecules and via gap junctions. [GOC:dos, GOC:mah] |
positive regulation of gene expression | biological process | Any process that increases the frequency, rate or extent of gene expression. Gene expression is the process in which a gene's coding sequence is converted into a mature gene product (protein or RNA). [GOC:txnOH-2018] |
negative regulation of gene expression | biological process | Any process that decreases the frequency, rate or extent of gene expression. Gene expression is the process in which a gene's coding sequence is converted into a mature gene product (protein or RNA). [GOC:txnOH-2018] |
paracrine signaling | biological process | The transfer of information from one cell to another, where the signal travels from the signal-producing cell to the receiving cell by passive diffusion or bulk flow in intercellular fluid. The signaling cell and the receiving cell are usually in the vicinity of each other. [GOC:mtg_signaling_feb11, ISBN:3527303782] |
negative regulation of phosphorylation | biological process | Any process that stops, prevents or decreases the rate of addition of phosphate groups to a molecule. [GOC:jl] |
positive regulation of transcription by RNA polymerase II | biological process | Any process that activates or increases the frequency, rate or extent of transcription from an RNA polymerase II promoter. [GOC:go_curators, GOC:txnOH] |
lung alveolus development | biological process | The process whose specific outcome is the progression of the alveolus over time, from its formation to the mature structure. The alveolus is a sac for holding air in the lungs; formed by the terminal dilation of air passageways. [GOC:mtg_lung, PMID:9751757] |
regulation of epithelial cell proliferation | biological process | Any process that modulates the frequency, rate or extent of epithelial cell proliferation. [GOC:ai] |
progesterone receptor signaling pathway | biological process | The series of molecular signals initiated by progesterone binding to its receptor in the cytoplasm. [GOC:ai, GOC:mah, PMID:14744870] |
maintenance of protein location in nucleus | biological process | Any process in which a protein is maintained in the nucleus and prevented from moving elsewhere. These include sequestration within the nucleus, protein stabilization to prevent transport elsewhere and the active retrieval of proteins that escape the nucleus. [GOC:ai] |
tertiary branching involved in mammary gland duct morphogenesis | biological process | The branching process in which the mammary gland ducts form tertiary branches off of the secondary branches as part of diestrus and pregnancy. [GOC:dph, PMID:18614704] |
regulation of transcription by RNA polymerase II | biological process | Any process that modulates the frequency, rate or extent of transcription mediated by RNA polymerase II. [GOC:go_curators, GOC:txnOH] |
intracellular steroid hormone receptor signaling pathway | biological process | The series of molecular signals initiated by a steroid binding to an intracellular steroid hormone receptor. [GOC:mah, GOC:signaling] |