lonaprisan: structure in first source [MeSH]
| ID Source | ID |
|---|---|
| PubMed CID | 6918548 |
| CHEMBL ID | 146032 |
| SCHEMBL ID | 977182 |
| MeSH ID | M0560040 |
| Synonym |
|---|
| zk-pra |
| zk-230211 |
| lonaprisan |
| CHEMBL146032 |
| bay86-5044 |
| zk 230211 |
| (8s,11r,13s,14s,17s)-11-(4-acetylphenyl)-17-hydroxy-13-methyl-17-(1,1,2,2,2-pentafluoroethyl)-1,2,6,7,8,11,12,14,15,16-decahydrocyclopenta[a]phenanthren-3-one |
| 211254-73-8 |
| lonaprisan (usan/inn) |
| D10016 |
| lonaprisan [usan:inn] |
| zk 232011 |
| zk230211 |
| unii-f5z5el4d26 |
| f5z5el4d26 , |
| 11-(4-acetylphenyl)-17-hydroxy-17-(1,1,2,2,2-pentafluoroethyl)estra-4,9-dien-3-one |
| bdbm50409115 |
| lonaprisan [usan] |
| lonaprisan [who-dd] |
| lonaprisan [inn] |
| 11beta-(4-acetylphenyl)-20,20,21,21,21-pentafluoro-17-hydroxy-19-nor-17alpha-pregna-5,9-dien-3-one |
| (8s,11r,13s,14s,17s)-11-(4-acetylphenyl)-17-hydroxy-13-methyl-17-(perfluoroethyl)-6,7,8,11,12,13,14,15,16,17-decahydro-1h-cyclopenta[a]phenanthren-3(2h)-one |
| SCHEMBL977182 |
| DTXSID60893551 |
| zk 230211; zk 232011 |
| Q27277684 |
| vhzpudnsvgrvmb-rxdlhwjpsa-n |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) |
|---|---|---|---|---|
| Progesterone receptor | Homo sapiens (human) | IC50 | 0.0000 | AID147641; AID147645 |
| Glucocorticoid receptor | Mus musculus (house mouse) | IC50 | 0.0160 | AID147644 |
| Androgen receptor | Homo sapiens (human) | IC50 | 0.0540 | AID147642 |
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID74370 | Relative binding affinity against Glucocorticoid receptor of rat after 2 hr incubation as percent binding compared to Dexamethasone | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26 ISSN: 0022-2623 | Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist. |
| AID147654 | In vitro agonist potency in transactivation assay of CV-1 cells stably transfected with human androgen receptor | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26 ISSN: 0022-2623 | Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist. |
| AID192364 | Incomplete abortifacient effect at 0.3 mg/animal/day in pregnant rats | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26 ISSN: 0022-2623 | Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist. |
| AID181268 | Antiglucocorticoid activity in adrenalectomized young male rats after oral administration | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26 ISSN: 0022-2623 | Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist. |
| AID69529 | Relative binding affinity against Estrogen receptor of rat after 2 hr incubation as percent binding compared to estradiol | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26 ISSN: 0022-2623 | Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist. |
| AID147656 | In vitro agonist potency in transactivation assay in NIH3T3 cells expressing glucocorticoid receptor | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26 ISSN: 0022-2623 | Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist. |
| AID192360 | Full abortifacient effect at 0.1 mg/animal/day in pregnant rats | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26 ISSN: 0022-2623 | Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist. |
| AID192363 | Incomplete abortifacient effect at 0.1 mg/animal/day in pregnant rats | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26 ISSN: 0022-2623 | Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist. |
| AID147644 | In vitro antagonist potency in transactivation assay in NIH3T3 cells expressing glucocorticoid receptor | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26 ISSN: 0022-2623 | Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist. |
| AID147643 | In vitro antagonist potency in transactivation assay in MVLN cells expressing estrogen receptor | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26 ISSN: 0022-2623 | Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist. |
| AID147655 | In vitro agonist potency in transactivation assay of MVLN cells expressing estrogen receptor | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26 ISSN: 0022-2623 | Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist. |
| AID192359 | Full abortifacient effect at 0.03 mg/animal/day in pregnant rats | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26 ISSN: 0022-2623 | Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist. |
| AID181267 | Antiandrogenic activity in orchidectomized young male rats after oral administration | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26 ISSN: 0022-2623 | Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist. |
| AID162452 | Relative binding affinity against rabbit progesterone (PR) receptor after 24 hr incubation as perent binding compared to progesterone | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26 ISSN: 0022-2623 | Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist. |
| AID147645 | In vitro antagonist potency in transactivation assay in neuroblastoma cells expressing human PR-B progesterone receptor | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26 ISSN: 0022-2623 | Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist. |
| AID192362 | Incomplete abortifacient effect at 0.03 mg/animal/day in pregnant rats | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26 ISSN: 0022-2623 | Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist. |
| AID147642 | In vitro antagonist potency in transactivation assay in CV-1 cells expressing androgen receptor | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26 ISSN: 0022-2623 | Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist. |
| AID147641 | In vitro antagonist potency in transactivation assay in neuroblastoma cells expressing human PR-A progesterone receptor | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26 ISSN: 0022-2623 | Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist. |
| AID39309 | Relative binding affinity against androgen (AR) receptor of rat after 24 hr incubation as percent binding compared to R1881 | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26 ISSN: 0022-2623 | Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist. |
| AID147653 | In vitro agonist potency in transactivation assay of neuroblastoma cells expressing human PR-A progesterone receptor | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26 ISSN: 0022-2623 | Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist. |
| AID147657 | In vitro agonist potency in transactivation assay in neuroblastoma cells expressing human PR-B progesterone receptor | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26 ISSN: 0022-2623 | Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist. |
| AID192361 | Full abortifacient effect at 0.3 mg/animal/day in pregnant rats | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26 ISSN: 0022-2623 | Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist. |
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 5 (45.45) | 29.6817 |
| 2010's | 6 (54.55) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 2 (18.18%) | 5.53% |
| Reviews | 2 (18.18%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 7 (63.64%) | 84.16% |
| Substance | Studies | Classes | Roles | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| mifepristone | 3-oxo-Delta(4) steroid; acetylenic compound; tertiary amino compound | abortifacient; contraceptive drug; hormone antagonist; synthetic oral contraceptive | 2000 | 2000 | 24.0 | medium | 0 | 0 | 1 | 0 | 0 | 0 |
| Substance | Studies | Classes | Roles | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| oxazoles | 1,3-oxazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene | 2010 | 2010 | 14.0 | medium | 0 | 0 | 0 | 1 | 0 | 0 | ||
| mifepristone | 3-oxo-Delta(4) steroid; acetylenic compound; tertiary amino compound | abortifacient; contraceptive drug; hormone antagonist; synthetic oral contraceptive | 2000 | 2000 | 24.0 | medium | 0 | 0 | 1 | 0 | 0 | 0 | |
| onapristone | 2000 | 2000 | 24.0 | high | 0 | 0 | 1 | 0 | 0 | 0 | |||
| vilaprisan | 2018 | 2018 | 6.0 | high | 0 | 0 | 0 | 0 | 1 | 0 |
| Condition | Indicated | Studies | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Adenocarcinoma | 0 | 2010 | 2010 | 14.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
| Adenocarcinoma, Basal Cell | 0 | 2010 | 2010 | 14.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
| Adult Pelizaeus-Merzbacher Disease | 0 | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Bleeding Between Periods | 0 | 2006 | 2006 | 18.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
| Breast Cancer | 0 | 2010 | 2013 | 13.0 | medium | 1 | 0 | 0 | 2 | 2 | 0 | |
| Breast Neoplasms | 1 | 2010 | 2013 | 13.0 | medium | 1 | 0 | 0 | 2 | 2 | 0 | |
| Cancer of the Uterus | 0 | 2010 | 2010 | 14.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
| Disease Models, Animal | 0 | 2006 | 2014 | 14.0 | low | 0 | 0 | 0 | 1 | 1 | 0 | |
| Experimental Mammary Neoplasms | 0 | 2000 | 2000 | 24.0 | low | 0 | 0 | 1 | 0 | 0 | 0 | |
| Female Genital Diseases | 0 | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Fibroid | 0 | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Genital Diseases, Female | 0 | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Heavy Menstrual Bleeding | 0 | 2007 | 2007 | 17.0 | low | 1 | 0 | 0 | 1 | 0 | 0 | |
| Leiomyoma | 0 | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Menopause | 0 | 2006 | 2006 | 18.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
| Menorrhagia | 0 | 2007 | 2007 | 17.0 | low | 1 | 0 | 0 | 1 | 0 | 0 | |
| Metrorrhagia | 0 | 2006 | 2006 | 18.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
| Pregnancy | 0 | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Uterine Neoplasms | 0 | 2010 | 2010 | 14.0 | low | 0 | 0 | 0 | 1 | 0 | 0 |
| Article | Year |
|---|---|
| Reversible suppression of menstruation with progesterone antagonists in rhesus macaques. Human reproduction (Oxford, England), , Volume: 16, Issue:8 | 2001 |