CORT 108297: a fused-ring azadecalin [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 44454750 |
| CHEMBL ID | 271220 |
| SCHEMBL ID | 755070 |
| MeSH ID | M0558088 |
| Synonym |
|---|
| ads-108297 |
| cort-108297 |
| CHEMBL271220 , |
| cort 108297 |
| bdbm50372968 |
| (r)-4a-(ethoxymethyl)-1-(4-fluorophenyl)-6-((4-(trifluoromethyl)phenyl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1h-pyrazolo(3,4-g)isoquinoline |
| unii-a17w0640nb |
| a17w0640nb , |
| 1018679-79-2 |
| 4a-(ethoxymethyl)-1-(4-fluorophenyl)-6-((4-(trifluoromethyl)phenyl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1h-pyrazolo(3,4-g)isoquinoline, (r)- |
| 1h-pyrazolo(3,4-g)isoquinoline, 4a-(ethoxymethyl)-1-(4-fluorophenyl)-4,4a,5,6,7,8-hexahydro-6-((4-(trifluoromethyl)phenyl)sulfonyl)-, (4ar)- |
| SCHEMBL755070 |
| DTXSID70144304 |
| cort108297 |
| AKOS027338706 |
| (r)-4a-(ethoxymethyl)-1-(4-fluorophenyl)-6-((4-(trifluoromethyl)phenyl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1h-pyrazolo[3,4-g]isoquinoline |
| mfcd28044284 |
| 1h-pyrazolo[3,4-g]isoquinoline, 4a-(ethoxymethyl)-1-(4-fluorophenyl)-4,4a,5,6,7,8-hexahydro-6-[[4-(trifluoromethyl)phenyl]sulfonyl]-, (4ar)-;1h-pyrazolo[3,4-g]isoquinoline, 4a-(ethoxymethyl)-1-(4-fluorophenyl)-4,4a,5,6,7,8-hexahydro-6-[[4-(trifluoromethyl |
| HY-15710 |
| CS-0008503 |
| BCP16798 |
| slkurxrzhjozod-ruzdidtesa-n |
| AS-35226 |
| SB17316 |
| Q27273492 |
| (4ar)-4a-(ethoxymethyl)-1-(4-fluorophenyl)-6-[4-(trifluoromethyl)phenyl]sulfonyl-4,5,7,8-tetrahydropyrazolo[3,4-g]isoquinoline |
| 1h-pyrazolo[3,4-g]isoquinoline, 4a-(ethoxymethyl)-1-(4-fluorophenyl)-4,4a,5,6,7,8-hexahydro-6-[[4-(trifluoromethyl)phenyl]sulfonyl]-, (4ar)- |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Analogues 43 and 45 had >50% oral bioavailability in the dog." | ( 1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as selective glucocorticoid receptor antagonists with high functional activity. Belanoff, J; Blaney, P; Bright, CP; Clark, DE; Clark, RD; Crackett, PH; Devos, R; Dyke, HJ; Hurley, C; Jenkins, RE; Lockey, P; Porres, SS; Ray, NC; Ward, S; Williams, K; Wong, M, 2008) | 0.35 |
| " Optimization of the sulfonamide substituent has provided compounds with a very desirable overall profile, including minimal hERG activity, good bioavailability and in vivo efficacy." | ( 1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as potent GR antagonists with reduced hERG inhibition and an improved pharmacokinetic profile. Belanoff, JK; Golding, E; Gourdet, B; Hunt, HJ; Phillips, T; Swift, D; Thomas, J; Unitt, JF; Walters, I, 2015) | 0.42 |
| Excerpt | Relevance | Reference |
|---|---|---|
| " In the first experiment, rats dosed only with olanzapine gained a statistically significant amount of weight." | ( Selective glucocorticoid receptor (type II) antagonist prevents and reverses olanzapine-induced weight gain. Belanoff, JK; Blasey, CM; Clark, RD; Roe, RL, 2010) | 0.36 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Glucocorticoid receptor | Homo sapiens (human) | Ki | 0.0048 | 0.0001 | 0.3863 | 7.0010 | AID1262374; AID318132; AID318133 |
| Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | IC50 (µMol) | 0.8000 | 0.0009 | 1.9014 | 10.0000 | AID1262382 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID318133 | Antagonist activity at GR in SW1353/MMTV5 cells assessed as inhibition of dexamethasone-induced luciferase expression | 2008 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4 | 1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as selective glucocorticoid receptor antagonists with high functional activity. |
| AID1262374 | Binding affinity to glucocorticoid receptor (unknown origin) by reporter gene assay | 2015 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24 | 1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as potent GR antagonists with reduced hERG inhibition and an improved pharmacokinetic profile. |
| AID1262382 | Inhibition of human ERG by patch clamp technique | 2015 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24 | 1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as potent GR antagonists with reduced hERG inhibition and an improved pharmacokinetic profile. |
| AID318132 | Displacement of [3H]dexamethasone from human recombinant GR | 2008 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4 | 1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as selective glucocorticoid receptor antagonists with high functional activity. |
| AID1262371 | Reduction in olanzapine-induced weight gain in rat at 20 mg/kg, po bid administered for 21 days measured from day 4 of compound dosing | 2015 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24 | 1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as potent GR antagonists with reduced hERG inhibition and an improved pharmacokinetic profile. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 1 (6.25) | 29.6817 |
| 2010's | 11 (68.75) | 24.3611 |
| 2020's | 4 (25.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (20.15) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 1 (6.25%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 15 (93.75%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||