m6A-centered Crosstalk Information
Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
| Crosstalk ID |
M6ACROT02082
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[1] | |||
DNA methylation
DNMT3A
FTO
Direct
Inhibition
m6A modification
NR3C1
NR3C1
FTO
Demethylation
: m6A sites
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| m6A Modification: | |||||
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| m6A Regulator | Fat mass and obesity-associated protein (FTO) | ERASER | |||
| m6A Target | Glucocorticoid receptor (NR3C1) | ||||
| Epigenetic Regulation that have Cross-talk with This m6A Modification: | |||||
| Epigenetic Regulation Type | DNA methylation (DNAMeth) | ||||
| Epigenetic Regulator | Cysteine methyltransferase DNMT3A (DNMT3A) | WRITER | View Details | ||
| Regulated Target | FTO alpha-ketoglutarate dependent dioxygenase (FTO) | View Details | |||
| Crosstalk Relationship | DNA methylation → m6A | Inhibition | |||
| Crosstalk Mechanism | DNA methylation directly impacts m6A modification through modulating the expression level of m6A regulator | ||||
| Crosstalk Summary | A downregulation in demethylating enzyme Fto and upregulation in methylating enzyme Mettl3 were also noted. The FTO promoter was hypomethylated due to the lower expression of DNMT1 and DNMT3A and Glucocorticoid receptor (NR3C1), Creb1, Ntrk2, Bdnf are downstream target genes of both METTL3 and FTO. | ||||
| Responsed Disease | Major depressive disorder | ICD-11: 6A70.3 | |||
In-vitro Model |
SH-SY5Y | Neuroblastoma | Homo sapiens | CVCL_0019 | |
| In-vivo Model | Rats were housed at 23 ° C and 55% humidity and were given ad libitum food and water. During acclimatization (1 week), rats were placed randomly (3/cage); however, after initial behavioral testing, they were grouped according to their behavioral phenotypes. All experiments were performed under a light cycle (8:00 AM and 10:00 AM). The protocol to induce LH behavior was approved by the Institutional Animal Care and Use Committee of the University of Alabama at Birmingham. The animal study also adhered to the international guidelines for the use and care of laboratory animals. | ||||
Full List of Potential Compound(s) Related to This m6A-centered Crosstalk
| Cysteine methyltransferase DNMT3A (DNMT3A) | 8 Compound(s) Regulating the Target | Click to Show/Hide the Full List | ||
| PMID27376512-Compound-Figure3CN | Patented | [2] | ||
| MOA | Inhibitor | |||
| Activity | EC50 = 1100 nM | |||
| External Link | ||||
| PMID27376512-Compound-Figure3CG | Patented | [2] | ||
| MOA | Inhibitor | |||
| Activity | EC50 = 2400 nM | |||
| External Link | ||||
| PMID27376512-Compound-Figure3CM | Patented | [2] | ||
| MOA | Inhibitor | |||
| Activity | EC50 = 1100 nM | |||
| External Link | ||||
| PMID27376512-Compound-Figure2aExample1 | Patented | [2] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 3000 nM | |||
| External Link | ||||
| PMID27376512-Compound-MTC-424 | Patented | [2] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 1940 nM | |||
| External Link | ||||
| PMID27376512-Compound-MTC-427 | Patented | [2] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 295 nM | |||
| External Link | ||||
| PMID27376512-Compound-MTC-422 | Patented | [2] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 1430 nM | |||
| External Link | ||||
| PMID27376512-Compound-MTC-423 | Patented | [2] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 363 nM | |||
| External Link | ||||
| Glucocorticoid receptor (NR3C1) | 74 Compound(s) Regulating the Target | Click to Show/Hide the Full List | ||
| Fluocinolone Acetonide | Approved | [3] | ||
| Synonyms |
Coriphate; Cortiplastol; Dermalar; Flucinar; Flucinolone; Flucort; Fluocet; Fluocinolonacetonidum; Fluonid; Fluotrex; Fluovitif; Flupollon; Jellin; Localyn; Medidur; Omniderm; Percutina; Prodermin; Radiocin; Retisert; Sinalar; Synalar; Synamol; Synandone; Synandrone; Synemol; Synotic; Synsac; Tefunote;Acetonida de fluocinolona; Acetonide de fluocinolone; Fluocinolone acetonide [DCIT]; Fluocinoloni acetonidum; Fluortriamcinolone Acetonide; Fs Shampoo; Localyn Syntex; F0657; RS 1401AT; Acetonida de fluocinolona [INN-Spanish]; Acetonide de fluocinolone [INN-French]; Component of Neo-Synalar; Dermatin (steroid); Fluocet (TN); Fluocinoloni acetonidum [INN-Latin]; Neo-Synalar; RS-1401 AT; Retisert (TN); Synalar (TN); Synalar-HP; Derma-smoothe/fs; Flucort-N (TN); Fluocinolone 16,17-acetonide; Fluocinolone acetonide [USAN:INN:JAN]; Ydroxyprednisolone 16,17-acetonide; Fluocinolone acetonide (JP15/USP/INN); Pregna-1,4-diene-3,20-dione, 6alpha,9-difluoro-11beta,16alpha,17,21-tetrahydroxy-, cyclic 16,17-acetal with acetone; Pregna-1,4-diene-3,20-dione, 6alpha,9-difluoro-11beta,16alpha,17,21-tetrahydroxy-, cyclic 16,17-acetal with acetone (8CI); Pregna-1,4-diene-3,20-dione, 6.alpha.,9-difluoro-11.beta.,16.alpha.,17,21-tetrahydroxy-, cyclic 16,17-acetal with acetone; (4aS,4bR,5S,6aS,6bS,9aR,10aS,10bS,12S)-4b,12-difluoro-5-hydroxy-6b-(hydroxyacetyl)-4a,6a,8,8-tetramethyl-4a,4b,5,6,6a,6b,9a,10,10a,10b,11,12-dodecahydro-2H-naphtho[2',1':4,5]indeno[1,2-d][1,3]dioxol-2-one; 4b,12-Difluoro-6b-glycoloyl-5-hydroxy-4a,6a,8,8-tetramethyl-4a,4b,5,6,6a,6b,9a,10,10a,10b,11,12-dodecahydro-2H-naphtho[2',1':4,5]indeno[1,2-d][1,3]dioxol-2-one; 6-alpha,9-alpha-Difluoro-16-alpha-hydroxyprednisolone 16,17-acetonide; 6.Alpha., 9.alpha.-Difluoro-16.alpha.-h; 6.Alpha.,9-Difluoro; 6.alpha.,9-Difluoro-11.beta.,16.alpha.,17,21-tetrahydroxypregna-1,4-diene-3,20-dione, cyclic 16,17-acetal with acetone; 6.alpha.,9.alpha.-Difluoro-16.alpha.-hydroxyprednisolone 16,17-acetonide; 6.alpha.-Fluorotriamcinolone acetonide; 6a,9a-difluoro-16a-hydroxyprednisolone 16,17-acetonide; 6alpha,9-Difluoro-11beta,16alpha,17,21-tetrahydroxypregna-1,4-diene-3,20-dione, cyclic 16,17-acetal with acetone; 6alpha,9alpha-Difluoro-11beta,16alpha,17alpha,21-tetrahydroxy-1,4-pregnadiene-3,20-dione; 6alpha,9alpha-Difluoro-11beta,16alpha,17alpha,21-tetrahydroxy-1,4-pregnadiene-3,20-dione 16,17-Acetonide; 6alpha,9alpha-Difluoro-16alpha-hydroxyprednisolone 16,17-acetonide; 6alpha-Fluorotriamcinolone acetonide
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| MOA | Modulator | |||
| External Link | ||||
| Triamcinolone | Approved | [3] | ||
| Synonyms |
Adcortyl; Aristocort; Celeste; Cinolone; Delphicort; Fluoxiprednisolone; Fluoxyprednisolone; Fougera; Ione; Kenacort; Ledercort; Mycolog; Omcilon; Omicilon; Orion; Rodinolone; Tiamcinolonum; Triamcet; Triamcinalone; Triamcinlon; Triamcinolon; Triamcinolona; Triamcinolonum; Tricortale; Trilone; Tristoject; Volon; Aristocort Tablets; Triamcinolonum [INN]; CL 19823; Aristocort (TN); Azmacort (TN); Cinolone-T; Fougera (TN); Kenacort (TN); Kenacort-AG; Kenalog (TN); Nasacort (TN); SK-Triamcinolone; Tiamcinolonum [INN-Latin]; Triam-Tablinen; Triamcinolona [INN-Spanish]; Tricortone (TN); Triderm (TN); Triesence (TN); Trilone (TN); Tristoject (TN); Volon A (TN); Tri-Nasal (TN); Triamcinolone (JP15/USP/INN); Triamcinolone [USAN:INN:BAN:JAN]; Droxypregna-1,4-diene-3,20-dione; Pregna-1,4-diene-3,20-dio; TRIAMCINOLONE (SEE ALSO TRIAMCINOLONE ACETONIDE (76-25-5) AND TRIAMCINOLONE DIACETATE (67-78-7)); Pregna-1,4-diene-3,20-dione, 9-fluoro-11beta,16alpha,17,21-tetrahydroxy-(8CI); Pregna-1,4-diene-3,20-dione, 9-fluoro-11,16,17,21-tetrahydroxy-, (11beta,16alpha); (8S,9R,10S,11S,13S,14S,16R,17S)-9-fluoro-11,16,17-trihydroxy-17-(2-hydroxyacetyl)-10,13-dimethyl-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-3-one; 11-beta,16-alpha,17-alpha,21-Tetrahydroxy-9-alpha-fluoro-1,4-pregnadiene-3,20-dione; 11.Beta.,16.alpha.,17.alpha., 21-Tetrahydroxy-9.alpha.-fluoro-1,4-pregnadiene-3,20-dione; 11.beta.,16.alpha.,17.alpha.,21-Tetrahydroxy-9.alpha.-fluoro-1,4-pregnadiene-3,20-dione; 9-Fluoro-11,16,17,21-tetrahydroxypregna-1,4-diene-3,20-dione; 9-Fluoro-11beta,16alpha,17,21-tetrahydroxypregna-1,4-diene-3,20-dione; 9-alpha-Fluoro-11-beta,16-alpha,17,21-tetrahydroxypregna-1,4-diene-3,20-dione; 9-alpha-Fluoro-16-alpha-hydroxyprednisolone; 9.Alpha.-Fluoro-11.beta.,16.alpha.,17,21-tetrahy; 9.Alpha.-Fluoro-11.beta.,16.alpha.,17,21-tetrahydroxy-1,4-pregnadiene-3,20-dione; 9.Alpha.-Fluoro-11.beta.,16.alpha.,17.alpha., 21-tetrahydroxypregna-1,4-diene-3,20-d; 9.Alpha.-Fluoro-16.alpha.-hydroxyprednisolone; 9.alpha.-Fluoro-11.beta.,16.alpha.,17,21-tetrahydroxypregna-1,4-diene-3,20-dione; 9.alpha.-Fluoro-11.beta.,16.alpha.,17.alpha.,21-tetrahydroxypregna-1,4-diene-3,20-dione; 9alpha-Fluoro-11beta,16alpha,17,21-tetrahydroxy-1,4-pregnadiene-3,20-dione; 9alpha-Fluoro-11beta,16alpha,17,21-tetrahydroxypregna-1,4-diene-3,20-dione; 9alpha-Fluoro-16alpha-hydroxyprednisolone
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| MOA | Modulator | |||
| External Link | ||||
| Mometasone | Approved | [4] | ||
| Synonyms |
Elocom; Mometasona; Mometasonum; Mometasona [Spanish]; Mometasonum [Latin]; Asmanex (TN); Elocon (TN); Mometasone (INN); Nasonex (TN); Twisthaler (TN); (+)-Mometasone; (8S,9R,10S,11S,13S,14S,16R,17R)-9-chloro-17-(2-chloroacetyl)-11,17-dihydroxy-10,13,16-trimethyl-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-3-one; (9R,10S,11S,13S,14S,16R,17R)-9-chloro-17-(2-chloroacetyl)-11,17-dihydroxy-10,13,16-trimethyl-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-3-one; 9,21-dichloro-11beta,17-dihydroxy-16alpha-methylpregna-1,4-diene-3,20-dione
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| MOA | Agonist | |||
| External Link | ||||
| Betamethasone Valerate | Approved | [3] | ||
| Synonyms |
Beta-val; Betaderm; Betatrex; Dermabet; Valnac
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| MOA | Modulator | |||
| External Link | ||||
| Hydrocortamate | Approved | [3] | ||
| Synonyms |
Hidrocortamato; Hydrocortamatum; Idrocortamato; Magnacort; Hydrocortamate [INN]; Idrocortamato [DCIT]; Hidrocortamato [INN-Spanish]; Hydrocortamatum [INN-Latin]; Hydrocortisone 21-(diethylamino)acetate; Hyddrocortison-21-(beta-diethylaminoacetat); Glycine, N,N-diethyl-, 21-ester with cortisol; Glycine, N,N-diethyl-, (11beta)-11,17-dihydroxy-3,20-dioxopregn-4-en-21-yl ester; [2-[(8S,9S,10R,11S,13S,14S,17R)-11,17-dihydroxy-10,13-dimethyl-3-oxo-2,6,7,8,9,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthren-17-yl]-2-oxoethyl] 2-(diethylamino)acetate; 11beta,17-Dihydroxy-3,20-dioxo-4-pregnen-21-yl 2-(diethylamino)acetat; 11beta,17-dihydroxy-3,20-dioxopregn-4-en-21-yl N,N-diethylglycinate; 11beta,17alpha,21-Trihydroxypregn-4-ene-3,20-dione 21-diethylaminoacetate; 17-Hydroxycorticosterone, 21-(diethylamino)acetate
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| MOA | Modulator | |||
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| Betamethasone Benzoate | Approved | [3] | ||
| Synonyms |
Uticort
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| MOA | Modulator | |||
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| Methylprednisolone | Approved | [3] | ||
| Synonyms |
Depo-medrol; M-predrol; Medrol; Medrol Acetate
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| MOA | Modulator | |||
| External Link | ||||
| Deflazacort | Approved | [3] | ||
| Synonyms |
C25H33NO6; Deflazacort (Calcort); Deflazacortum [INN-Latin]; EINECS 238-483-7; Deflan (TN); AC1L1BQ2; Deflazacort [USAN:BAN:INN]; CTK8F9001; MolPort-035-394-927
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| MOA | Modulator | |||
| External Link | ||||
| Betamethasone | Approved | [5] | ||
| Synonyms |
378-44-9; Betadexamethasone; Flubenisolone; Betamethazone; Rinderon; Visubeta; Celestene; Betnelan; Betapredol; Betacortril; Betacorlan; Methazon; Betsolan; Betamamallet; Hormezon; Betasolon; Betametasone; Cidoten; Bebate; Bedifos; Becort; beta-Methasone; Desacort-Beta; Rinderon A; beta-Methasone alcohol; Betametasona; Betafluorene; Betamethasonum; Celestone; Betamethasone cream; Betamethasone alcohol; Betametasone [DCIT]; 9alpha-Fluoro-16beta-methylprednisolone; Celestone Syrup and Tablets; Celeston; Celestona; Cellestoderm; Luxiqo; Betamethasone Base; Betamethasone Valearate; Betamethasonvalerat Mikron; LT00441022; SCH 4831; Betametasona [INN-Spanish]; Betamethasonum [INN-Latin]; Betnovate (TN); Celestone (TN); Diprolene (TN); Diprosone (TN); Lotrisone (TN); Rinderon (TN); SCH-4831; Betamethasone (JP15/USP/INN); Betamethasone [USAN:BAN:INN:JAN]; Betamethasone [USAN:INN:BAN:JAN]; Celestone, Betadexamethasone, Flubenisolone, Sch-4831, NCS-39470, Betamethasone; 1,4-Pregnadiene-3,20-dione-9alpha-fluoro-16 beta-methyl-11 beta,17alpha,21-triol; 16beta-Methyl-1,4-pregnadiene-9alpha-fluoro-11beta,17alpha,21-triol-3,20-dione; 9-Fluoro-11,17,21-trihydroxy-16-methylpregna-1,4-diene-3,20-dione; 9-Fluoro-11-beta,17,21-trihydroxy-16-beta-methylpregna-1,4-diene-3,20-dione; 9-Fluoro-11beta,17,21-trihydroxy-16beta-methylpregna-1,4-diene-3,20-dione; 9-Fluoro-16beta-methylprednisolone; 9-alpha-Fluoro-16-beta-methylprednisolone; 9alpha-Fluoro-16 beta-methyl-prednisolone; Betamethasone sodium phosphate
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| MOA | Agonist | |||
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| Prednisolone | Approved | [6] | ||
| Synonyms |
Nanocort; Prednisolone (injectable liposome formulation, rheumatoid arthritis); Prednisolone (injectable liposome formulation, rheumatoid arthritis), Enceladus; Prednisolone (injectable liposome formulation, rheumatoid arthritis), Galapagos
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| MOA | Modulator | |||
| Activity | Ki = 1.14 nM | |||
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| Flunisolide | Approved | [7] | ||
| Synonyms |
Aerobid; Aerospan; Bronalide; Flunisolida; Flunisolidum; Lunis; Nasalide; Nasarel; Nisolid; Rhinalar; Rhinolar; Soluzione; Synaclyn; Syntaris; Aerobid M; Aerospan HFA; Flunisolide HFA; Flunisolide [INN]; Flunisolide [anhydrous]; Flunisolide anhydrous; F0437; RS 3999; AeroBid (TN); Flunisolida [INN-Spanish]; Flunisolide (anhydrous); Flunisolidum [INN-Latin]; Nasalide (TN); Nasarel (TN); RS-3999; AeroBid, Nasalide, Nasarel,Flunisolide; Pregna-1,4-diene-3,20-dione, 6-alpha-fluoro-11-beta,16-alpha,17,21-tetrahydroxy-, cyclic 16,17-acetal with acetone; Pregna-1,4-diene-3,20-dione, 6-alpha-fluoro-11-beta,16-alpha,17,21-tetrahydroxy-,cyclic 16,17-acetal with acetone; 6 alpha-fluoro-11 beta,16 alpha,17,21-tetrahydroxypregna-1,4-diene-3,20-dione cyclic 16, 17-acetal with acetone; 6 alpha-fluorodihydroxy-16 alpha,17 alpha-isopropylidenedioxy-1,4-pregnadiene-3,20-dione; 6-Fluoro-11,21-dihydroxy-16,17-(isopropylidenedioxy)pregna-1,4-diene-3,20-dione; 6alpha-Fluoro-11beta,16alpha,17,21-tetrahydroxypregna-1,4-diene-3,20-dione cyclic 16, 17-acetal with acetone; 6alpha-fluoro-11beta,21-dihydroxy-16alpha,17alpha-(isopropylidenedioxy)pregna-1,4-diene-3,20-dione
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| MOA | Agonist | |||
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| Meprednisone | Approved | [3] | ||
| Synonyms |
Betapar
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| MOA | Modulator | |||
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| Prednisone | Approved | [8] | ||
| Synonyms |
Adasone; Ancortone; Bicortone; Cartancyl; Colisone; Cortan; Cortidelt; Cotone; Dacorten; Dacortin; Decortancyl; Decortin; Decortisyl; Dehydrocortisone; Dekortin; Dellacort; Deltacortene; Deltacortisone; Deltacortone; Deltasone; Deltison; Deltisona; Deltisone; Deltra; Diadreson; Econosone; Encorton; Encortone; Enkortolon; Enkorton; Fiasone; Hostacortin; Incocortyl; Juvason; Kortancyl; Lisacort; Lodotra; Metacortandracin; Meticorten; Nisona; Nizon; Novoprednisone; Nurison; Orasone; Panafcort; Panasol; Paracort; Parmenison; Pehacort; Precort; Predeltin; Prednicorm; Prednicort; Prednicot; Prednidib; Prednilonga; Prednison; Prednisona; Prednisonum; Prednitone; Prednizon; Prednovister; Presone; Pronison; Pronisone; Rectodelt; Retrocortine; Servisone; Sone; Sterapred; Supercortil; Ultracorten; Ultracortene; Winpred; Wojtab; Zenadrid; Dellacort A; Delta E; Delta cortelan; Liquid Pred; Origen Prednisone; Prednisone Intensol; Zenadrid [veterinary]; P1276; U 6020; Apo-Prednisone; Delta E.; Delta-Cortelan; Delta-Cortisone; Delta-Cortone; Delta-Dome; Delta-E; Delta1-Cortisone; Delta1-Dehydrocortisone; Di-Adreson; In-Sone; Me-Korti; Meticortelone (TN); Meticorten (TN); Meticorten (Veterinary); Metrevet (Veterinary); Prednicen-M; Prednisona [INN-Spanish]; Prednisone [INN:BAN]; Prednisonum [INN-Latin]; SK-Prednisone; Zenadrid (veterinary); Delta(sup 1)-Cortisone; Delta(sup 1)-Dehydrocortisone; Delta(sup1)-Cortisone; Delta-1-Cortisone; Delta-1-Dehydrocortisone; Deltasone, Liquid Pred, Orasone, Adasone, Deltacortisone,Prednisone; (1S,2R,10S,11S,14R,15S)-14-hydroxy-14-(2-hydroxyacetyl)-2,15-dimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-3,6-diene-5,17-dione; (8S,9S,10R,13S,14S,17R)-17-hydroxy-17-(2-hydroxyacetyl)-10,13-dimethyl-6,7,8,9,12,14,15,16-octahydrocyclopenta[a]phenanthrene-3,11-dione; (8xi,9xi,14xi)-17,21-dihydroxypregna-1,4-diene-3,11,20-trione; 1,2-Dehydrocortisone; 1,4-Pregnadiene-17-alpha,21-diol-3,11,20-trione; 1,4-Pregnadiene-17.alpha.,21-diol-3,11,20-trione; 1,4-Pregnadiene-17alpha,21-diol-3,11,20-trione; 1-Cortisone; 1-Dehydrocortisone; 17,21-Dihydroxypregna-1,4-diene-3,11,20-trione; 17alpha,21-Dihydroxy-1,4-pregnadiene-3,11,20-trione
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| MOA | Agonist | |||
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| Dexamethasone | Approved | [9] | ||
| Synonyms |
Adexone; Anaflogistico; Aphtasolon; Aphthasolone; Auxiron; Azium; Calonat; Corson; Corsone; Cortisumman; DXM; Decacort; Decacortin; Decaderm; Decadron; Decagel; Decaject; Decalix; Decameth; Decasone; Decaspray; Dectancyl; Dekacort; Deltafluorene; Dergramin; Deronil; Desadrene; Desametasone; Desamethasone; Desameton; Deseronil; Dexacort; Dexacortal; Dexacortin; Dexadeltone; Dexafarma; Dexair; Dexalona; Dexaltin; Dexametasona; Dexameth; Dexamethansone; Dexamethasonum; Dexamethazone; Dexamonozon; Dexapolcort; Dexaprol; Dexason; Dexasone; Dexinolon; Dexinoral; Dexone; Dexonium; Dexpak; Dextelan; Dezone; Dinormon; Dxms; Fluormethylprednisolone; Fluormone; Fluorocort; Fortecortin; Gammacorten; Hexadecadrol; Hexadrol; IontoDex; Loverine; Luxazone; Maxidex; Mediamethasone; Methylfluorprednisolone; Mexidex; Millicorten; Mymethasone; Oradexon; Policort; Posurdex; Prodex; Spoloven; Superprednol; Turbinaire; Visumetazone; Alcon Brand of Dexamethasone; Bisu DS; Desametasone [DCIT]; Dexa Mamallet; Dexamethasone Base; Dexamethasone Intensol; Dexamethasone alcohol; ECR Brand of Dexamethasone; Foy Brand of Dexamethasone; Hexadrol Elixir; Hexadrol Tablets; ICN Brand of Dexamethasone; Lokalison F; Merck Brand of Dexamethasone; Pet Derm III; Prednisolon F; Prednisolone F; Sunia Sol D; Dexone 4; MK 125; Merz Brand 1 of Dexamethasone; Merz Brand 2 of Dexamethasone; Aeroseb-D; Aeroseb-Dex; Azium (Veterinary); Decadron (TN); Decadron Tablets, Elixir; Decadron, Dexamethasone; Decadron-LA; Dex-ide; Dexa-Cortidelt;Dexa-Cortisyl; Dexa-Mamallet; Dexa-Scheroson; Dexa-sine; Dexacen-4; Dexametasona [INN-Spanish]; Dexamethasonum [INN-Latin]; Dexone 0.5; Dexone 0.75; Dexone 1.5; Hl-dex; Isopto-Dex; OTO-104; Ocu-trol;Pet-Derm Iii; SK-Dexamethasone; Decaject L.A.; Dexamethasone [INN:BAN:JAN]; Decaject-L.A.; Dexamethasone (JP15/USP/INN); Delta1-9alpha-Fluoro-16alpha-methylcortisol; Delta(sup 1)-9-alpha-Fluoro-16-alpha-methylcortisol; (3H)-Dexamethasone; 1-Dehydro-16.alpha.-methyl-9.alpha.-fluorohydrocortisone; 1-Dehydro-16alpha-methyl-9alpha-fluorohydrocortisone; 16-alpha-Methyl-9-alpha-fluoro-1-dehydrocortisol; 16-alpha-Methyl-9-alpha-fluoro-delta(sup 1)-hydrocortisone; 16-alpha-Methyl-9-alpha-fluoro-delta1-hydrocortisone; 16-alpha-Methyl-9-alpha-fluoroprednisolone; 16.alpha.-Methyl-9.alpha.-fluoro-1-dehydrocortisol; 16.alpha.-Methyl-9.alpha.-fluoroprednisolone; 16alpha-Methyl-9alpha-fluoro-1-dehydrocortisol; 16alpha-Methyl-9alpha-fluoro-delta(sup 1)-hydrocortisone; 16alpha-Methyl-9alpha-fluoroprednisolone; 9-alpha-Fluoro-16-alpha-methylprednisolone; 9.alpha.-Fluoro-16.alpha.-methylprednisolone; 9A-FLUORO-16BETA-METHYLPREDNISOLONE; 9alpha-Fluoro-16alpha-methylprednisolone
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| MOA | Agonist | |||
| Activity | EC50 = 0.1 nM | |||
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| Hydrocortisone | Approved | [3] | ||
| Synonyms |
Acticort; Alacort; Algicirtis; Alphaderm; Amberin; Anflam; Anucort; Aquacort; Cetacort; Chronocort; Cleiton; Cobadex; Colocort; Corhydron; Cortanal; Cortef; Cortenema; Cortesal; Corticreme; Cortifair; Cortifan; Cortiment; Cortisol; Cortisolonum; Cortisporin; Cortispray; Cortolotion; Cortonema; Cortoxide; Cortril; Cremesone; Cutisol; Delacort; Dermacort; Dermaspray; Dermil; Dermocortal; Dermolate; Dihydrocostisone; Dioderm; Drotic; DuoCort; Efcorbin; Efcortelan; Efcortelin; Eldecort; Eldercort; Epicort; Epicortisol; Evacort; Ficortril; Fiocortril; Flexicort; Genacort; Glycort; Hidalone; Hycort; Hycortol; Hycortole; Hydracort; Hydrasson; Hydrocortal; Hydrocorticosterone; Hydrocortisyl; Hydrocortone; Hydroskin; Hydroxycortisone; Hytisone; Hytone; Idrocortisone; Kyypakkaus; Lactisona; Lubricort; Maintasone; Medicort; Meusicort; Mildison; Milliderm; Nutracort; Optef; Otocort; Penecort; Permicort; Prepcort; Proctocort; Protocort; Rectoid; Sanatison; Schericur; Sigmacort; Signef; Stiefcorcil; Synacort; Tarcortin; Texacort; Timocort; Traumaide; Uniderm; Vytone; Zenoxone; ACETASOL HC; Aeroseb HC; AnusolHC; Aquanil HC; Barseb HC; CaldeCORT Spray; Clear aid; Component of Lubricort; Component of Otalgine; Cortisol alcohol; Cortisporin Otico; Ef corlin; Epiderm H; Esiderm H; Foille Insetti; HYDROCORTISONE AND ACETIC ACID; HYDROCORTISONE IN ABSORBASE; Heb Cort; Hydrocortisone alcohol; Hydrocortisone base; Hydrocortisone free alcohol; Hydrocortisone solution; Hytone lotion; Idrocortisone [DCIT]; Komed HC; Lacticare HC; Nogenic HC; ORLEX HC; Pediotic Suspension; Polcort H; Preparation H Hydrocortisone Cream; Prevex HC; Proctozone HC; Remederm HC; Scalpicin Capilar; Scheroson F; Systral Hydrocort; Transderma H; VoSol HC; H 4001; Texacort lotion 25; [3H]cortisol; ACETIC ACID W/ HYDROCORTISONE; Acticort (TN); Aeroseb-HC; Ala-Cort; Ala-Scalp; Anti-inflammatory hormone; Anucort-HC; Anusol HC (TN); Balneol-hc; Basan-Corti; Beta-hc; COR-OTICIN; Colocort (TN); Cort-Dome; Cortef (TN); Cortisol, Hydrocortisone; Cremicort-H; Cyclodextrin-encapsulated hydrocortisone; Derm-Aid; Dome-cort; Domolene-HC; Genacort (lotion); Gyno-Cortisone; H-Cort; HC #1; HC #4; HC (HYDROCORTISONE); Heb-Cort; Hi-cor; Hidro-Colisona; Hidrocortisona [INN-Spanish]; Hydro-Adreson; Hydro-Colisona; Hydro-RX; Hydrocortisone-Water Soluble; Hydrocortisonum [INN-Latin]; Hytone (TN); Incortin-H; Incortin-hydrogen; Kendall's compound F; Lacticare-HC; Neo-Cortef; Neosporin-H Ear; Nystaform-HC; Otosone-F; Rectasol-HC; Reichstein's substance M; Scalp-Cort; Stie-cort; Component of Neo-Cort-Dome; Hydrocortisone [INN:BAN:JAN]; Hydrocortisone (JP15/USP/INN); 11-beta-Hydrocortisone; 11-beta-Hydroxycortisone; 11beta,17,21-Trihydroxyprogesterone; 11beta-Hydrocortisone; 11beta-Hydroxycortisone; 17-Hydroxycorticosterone; 17alpha-Hydroxycorticosterone
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| MOA | Modulator | |||
| External Link | ||||
| Fluticasone | Approved | [10] | ||
| Synonyms |
Fluticaps; Fluticaps (TN); Fluticasone (INN); S-(fluoromethyl) (6S,8S,9R,10S,11S,13S,14S,16R,17R)-6,9-difluoro-11,17-dihydroxy-10,13,16-trimethyl-3-oxo-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthrene-17-carbothioate
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| MOA | Antagonist | |||
| External Link | ||||
| Dexamethasone sodium phosphate | Approved | [11] | ||
| Synonyms |
EryDex; Dexamethasone sodium phosphate (erythrocyte encapsulated); Dexamethasone sodium phosphate (erythrocyte encapsulated), Urbino University/EryDel; Dex 21-P (red blood cell encapsulated), Urbino University/EryDel; Intra-erythrocyte dexamethasone (inflammatory diseases), Urbino University/EryDel
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| MOA | Agonist | |||
| External Link | ||||
| Fluorometholone | Approved | [12] | ||
| Synonyms |
Cortilet; Cortisdin; Delmeson; Efflumidex; FML; Fluaton; Flucon; Flumetholon; Fluormetholon; Fluormetholone; Fluormetholonum; Fluoromethalone; Fluorometholonum; Fluorometolona; Fluorometolone; Fluoropos; Loticort; Oxylone; Trilcin; Ursnon; Alcon Brand of Fluorometholone; FML Forte; FML Liquifilm; Fluor Op; Fluoro Ophtal; Fluorometolone [DCIT]; Isdin Brand of Fluorometholone; Isopto Flucon; Novartis Brand of Fluorometholone; PMS Fluorometholone; Pharm Allergan Brand of Fluorometholone; Pharmascience Brand of Fluorometholone; Ursapharm Brand of Fluorometholone; Winzer Brand of Fluorometholone; Allergan Brand 1 of Fluorometholone; Allergan Brand 2 of Fluorometholone; Allergan Brand 3 of Fluorometholone; F0414; U 8614; Component of Neo-Oxylone; FML (TN); FML-S Liquifilm; Flarex (TN); Flucon, Isopto; Fluor-Op; Fluoro-Ophtal; Fluorometholonum [INN-Latin]; Fluorometolona [INN-Spanish]; Neo-Oxylone; Oxylone (TN); PMS-Fluorometholone; Pharm-Allergan Brand of Fluorometholone; FML S.O.P; Fluor-op (TN); Fluorometholone [INN:BAN:JAN]; Fluorometholone (JP15/USP/INN); Pregna-1,4-diene-3,20-dione, 9-fluoro-11.beta.,17; Pregna-1,4-diene-3,20-dione, 9-fluoro-11beta,17-dihydroxy-6alpha-methyl-(8CI); (6S,8S,9R,10S,11S,13S,14S,17R)-17-acetyl-9-fluoro-11,17-dihydroxy-6,10,13-trimethyl-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-3-one; 11beta,17alpha-Dihydroxy-9-fluoro-6-methyl-1,4-pregnadiene-3,20-dione; 9-Fluoro-11,17-dihydroxy-6-methylpregna-1,4-diene-3,20-dione; 9-Fluoro-11-beta,17-dihydroxy-6-alpha-methylpregna-1,4-diene-3,20-dione; 9-Fluoro-11beta,17-dihydroxy-6alpha-methylpregna-1,4-diene-3,20-dione
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| MOA | Binder | |||
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| Budesonide | Approved | [13] | ||
| Synonyms |
Bidien; Budenofalk; Budeson; Budesonido; Budesonidum; Budiair; Cortivent; Entocort; Horacort; Inflammide; Micronyl; Miflonide; Preferid; Pulmaxan; Respules; Rhinocort; Spirocort; UDB; Budecort Inhaler; Budesonide Easyhaler; Budesonide MMX; Entocort EC; GionaEasyhaler; Pulmaxan turbohaler; Pulmicort Flexhaler; Pulmicort Nebuamp; Pulmicort Respules; Pulmicort Topinasal; Pulmicort turbuhaler; Rhinocort Aqua; Rhinocort Turbuhaler; Rhinocort alpha; Unit dosebudesonide; B 7777; S 1320; Budesonido [INN-Spanish]; Budesonidum [INN-Latin]; Entocort (TN); Entocort EC (TN); MAP-0010; Noex (TN); Pulmicort (TN); Rhinocort (TN); S-1320; Budesonide (JAN/USAN/INN); Budesonide [USAN:INN:BAN:JAN]; Rhinocort, Pulmicort , Entocort, Symbicort, Noex. Entocort EC, Budesonide; Pregna-1,4-diene-3,20-dione, 16,17-butylidenebis(oxy)-11,21-dihydroxy-, (11beta,16alpha(R))-,and 16alpha,17-((S)-Butylidenebis(oxy))-11beta,21-dihydroxypregna-1,4-diene-3,20-dione; (11-beta,16-alpha)-16,17-(Butylidenebis(oxy))-11,21-dihydroxypregna-1,4-diene-3,20-dione; (11beta,16alpha)-16,17-(Butylidenebis(oxy))-11,21-dihydroxypregna-1,4-diene-3,20-dione; (4aR,4bS,5S,6aS,6bS,8R,9aR,10aS,10bS)-5-hydroxy-6b-(hydroxyacetyl)-4a,6a-dimethyl-8-propyl-4a,4b,5,6,6a,6b,9a,10,10a,10b,11,12-dodecahydro-2H-naphtho[2',1':4,5]indeno[1,2-d][1,3]dioxol-2-one; (4aR,4bS,5S,6aS,6bS,9aR,10aS,10bS)-5-hydroxy-6b-(hydroxyacetyl)-4a,6a-dimethyl-8-propyl-4a,4b,5,6,6a,6b,9a,10,10a,10b,11,12-dodecahydro-2H-naphtho[2',1':4,5]indeno[1,2-d][1,3]dioxol-2-one; (R,S)-11b,16a,17,21,tetrahydroxypregna-1,4-diene-3,20-dione cyclic 16,17-acetal with buty raldehyde; (RS)-(11beta,16alpha)-16,17-[Butylidenebis(oxy)]-11,21-dihydroxypregna-1,4-diene-3,20-dione; (RS)-11beta,16alpha,17,21-Tetrahydroxypregna-1,4-diene-3,20-dione cyclic 16,17-acetal with butyraldehyde; (S)-16alpha,17-(Butylidenedioxy)-11beta,21-dihydroxypregna-1,4-diene-3,20-dione; 11beta,21-dihydroxy-16alpha,17alpha-(butane-1,1-diyldioxy)pregna-1,4-diene-3,20-dione; 16,17-Butylidenebis(oxy)-11,21-dihydroxypregna-1,4-diene-3,20-dione; 16,17-Butylidenebis(oxy)-11-,21-dihydroxypregna-1,4-diene-3,20-dione; 16-alpha,17-alpha-Butylidenedioxy-11-beta,21-dihydroxy-1,4-pregnadiene-3,20-dione; 16alpha(R),17-(Butylidenebis(oxy))-11beta,21-dihydroxypregna-1,4-diene-3,20-dione; 16alpha-,17alpha-butylidenedioxypregna-1,4-diene-11beta-,21-diol-3,20-dione
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| MOA | Antagonist | |||
| Activity | Ki = 1.3 nM | |||
| External Link | ||||
| GW685698X | Approved | [14] | ||
| Synonyms |
Allermist; Avamys; Veramyst; Fluticasone furoate; GW 685698X; GW6; GW-685698; GW-685698X; Veramyst (TN); Fluticasone furoate (JAN/USAN/INN); (6alpha,11beta,16alpha,17alpha)-6,9-Difluoro-17-(((fluoromethyl)thio)carbonyl)-11-hydroxy-16-methyl-3-oxoandrosta-1,4-dien-17-yl-2-furancarboxylate; 6alpha,9-Difluoro-17-(((fluoromethyl)sulfanyl)carbonyl)-11beta-hydroxy-16alpha-methyl-3-oxoandrosta-1,4-dien-17alpha-yl furan-2-carboxylate
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| MOA | Agonist | |||
| Activity | IC50 = 0.03981 nM | |||
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| Mifepristone | Approved | [15] | ||
| Synonyms |
Mifedren; HRA-052015; Mifepristone (Cushing's disease); ACTH modulator (Cushing's disease), HRA; Adrenocorticotropic hormone modulator (Cushing's disease), HRA Pharma; Mifepristone (Cushing's disease), HRA pharma
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| MOA | Modulator | |||
| Activity | IC50 = 0.008 nM | |||
| External Link | ||||
| FST-201 | Phase 3 | [16] | ||
| Synonyms |
Dexamethasone + povidone iodine (otitis), Foresight Biotherapeutics; Otic anti-infective (otitis), Foresight Biotherapeutics
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| MOA | Agonist | |||
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| Mapracorat | Phase 3 | [17] | ||
| Synonyms |
BOL-303242X; SEGRA, Intendis; SEGRA, Schering AG; ZK-216348; ZK-238587; ZK-245186; Mapracorat (ophthalmic, ocular inflammation); Mapracorat Ophthalmic Suspension, Bausch & Lomb; SEGRA (atopic dermatitis), Bayer; Selective glucocorticoid receptor agonists (SEGRA) Bayer Schering/AstraZeneca; Selective glucocorticoid receptor agonists (SEGRA) Schering AG/AstraZeneca; Selective glucocorticoid receptor agonists (SEGRA), Schering AG; Selective glucocorticoid receptor agonists (dermatology), Schering AG; Mapracorat (dermatological, atopic dermatitis), Intendis; SEGRA (ophthalmic disease), Bausch & Lomb; Selective glucocorticoid receptor agonist (ophthalmic disease), Bausch & Lomb; Selective glucocorticoid receptor agonists (dermatological, eczema), Intendis; Suppressor of pro-inflammatory mediators (eczema), Intendis; BOL-303242-X Ophthalmic Suspension, Bausch & Lomb; Mapracorat (ophthalmic, ocular inflammation), Bausch & Lomb; ZK-245186 (ophthalmic), Bausch & Lomb
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| MOA | Agonist | |||
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| CORT-125134 | Phase 3 | [18] | ||
| Synonyms |
relacorilant; UNII-2158753C7E; 2158753C7E; 1496510-51-0; Relacorilant [INN]; Relacorilant [WHO-DD]; Relacorilant [USAN:INN]; SCHEMBL15454999; WANIDIGFXJFFEL-SANMLTNESA-N; CORT125134; ZINC141949519; AKOS032945759; J3.651.009I; ((4aR)-1-(4-fluorophenyl)-6-(1-methyl-1H-pyrazole-4-sulfonyl)-1,4,5,6,7,8-hexahydro-4aH-pyrazolo(3,4-g)isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone; Methanone, ((4aR)-1-(4-fluorophenyl)-1,4,5,6,7,8-hexahydro-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4ah-pyrazolo(3,4-g)isoqui
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| MOA | Antagonist | |||
| Activity | Ki = 7.2 nM | |||
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| TLC599 | Phase 3 | [19] | ||
| MOA | Agonist | |||
| External Link | ||||
| IONIS-GCCRRX | Phase 2 | [20] | ||
| MOA | Antagonist | |||
| External Link | ||||
| ORG-34517 | Phase 2 | [21] | ||
| Synonyms |
11beta-(1,3-Benzodioxol-5-yl)-17beta-hydroxy-17-(1-propynyl)estra-4,9-dien-3-one
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| MOA | Antagonist | |||
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| LAS-41002 | Phase 2 | [22] | ||
| Synonyms |
Monovo; Corticosteroid receptor modulator (eczema, psoriasis), Almirall
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| MOA | Modulator | |||
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| GW-870086-X | Phase 2 | [23] | ||
| Synonyms |
GW-870086-X (topical, atopic dermatitis), GlaxoSmithKline
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| MOA | Agonist | |||
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| DE-110 | Phase 2 | [24] | ||
| Synonyms |
Selective glucocorticoid receptor agonist (allergy), Santen
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| MOA | Agonist | |||
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| GW-870086-X | Phase 2 | [23] | ||
| Synonyms |
Glucocorticoid agonist (asthma), GlaxoSmithKline; GW-870086-X (inhaled, asthma), GlaxoSmithKline
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| MOA | Agonist | |||
| External Link | ||||
| ETIPREDNOL DICLOACETATE | Phase 2 | [25] | ||
| Synonyms |
BNP-166; Cronaze (Ivax); Ethinase (Ivax); Etiprednol dicloacetate < USAN; Respicort (Ivax); (11beta,17alpha)-17-(2,2-Dichloroacetoxy)-11-hydroxy-3-oxoandrosta-1,4-diene-17-carboxylic acid ethyl ester
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| MOA | Modulator | |||
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| TPI-1020 | Phase 2 | [26] | ||
| Synonyms |
Nitrobudesonide; NCX-1020; NO-budesonide; Budesonide-21-nitrooxymethylbenzoate
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| MOA | Antagonist | |||
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| CORT113176 | Phase 2 | [27] | ||
| Synonyms |
(R)-(1-(4-fluorophenyl)-6-((4-(trifluoromethyl)phenyl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(pyridin-2-yl)methanone; {(4aR)-1-(4-fluorophenyl)-6-[4-(trifluoromethyl)benzene-1-sulfonyl]-1,4,5,6,7,8-hexahydro-4aH-pyrazolo[3,4-g]isoquinolin-4a- yl}(pyridin-2-yl)methanone; 1496508-34-9; AKOS040756862; BDBM50265674; CHEMBL3734774; CORT113176; CORT-113176; CS-0204060; Dazucorilant; Dazucorilant [INN]; DAZUCORILANT [USAN]; HR4RD5RBJ6; HY-132811; Methanone, ((4aR)-1-(4-fluorophenyl)-1,4,5,6,7,8-hexahydro-6-((4-(trifluoromethyl)phenyl)sulfonyl)-4ah-pyrazolo(3,4-g)isoquinolin-4a-yl)-2-pyridinyl-; Methanone, [(4aR)-1-(4-fluorophenyl)-1,4,5,6,7,8-hexahydro-6-[[4-(trifluoromethyl)phenyl]sulfonyl]-4aH-pyrazolo[3,4-g]isoquinolin-4a-yl]-2-pyridinyl-; MS-30438; SCHEMBL15455041; UNII-HR4RD5RBJ6
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| MOA | Modulator | |||
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| ORG 34517/34850 | Phase 2 | [28] | ||
| Synonyms |
Sardomozide; 4-Aiah; SAM 486A; Cgp 48664; UNII-CEB05S0B9I; SAM486A; 149400-88-4; CEB05S0B9I; 4-amidinoindan-1-one 2'-amidinohydrazone; (E)-2-(4-carbamimidoyl-2,3-dihydro-1H-inden-1-ylidene)hydrazinecarboximidamide; Urea azine with 1-oxo-4-indancarboxamidine; Sardomozide chloride; Hydrazinecarboximidamide, 2-(4-(aminoiminomethyl)-2,3-dihydro-1H-inden-1-ylidene)-; 4-AMIDINOINDAN-1-ONE-2'-AMIDINOHYDRAZONE; 1443105-76-7; C11H14N6; Cgp 48664A; CHEMBL1202793; Sardomozide [INN]
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| MOA | Antagonist | |||
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| BAY 86-5044 | Phase 2 | [29] | ||
| Synonyms |
Lonaprisan; ZK-230211; 211254-73-8; UNII-F5Z5EL4D26; F5Z5EL4D26; AC1OCFKM; ZK-PRA; Lonaprisan [USAN:INN]; Lonaprisan (USAN/INN); SCHEMBL977182; CHEMBL146032; zk230211; BDBM50409115; BAY86-5044; ZK 230211; ZK 232011; D10016; Z-3103; (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
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| MOA | Inhibitor | |||
| External Link | ||||
| IBI-20089 | Phase 1 | [20] | ||
| MOA | Agonist | |||
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| NCX-1015 | Phase 1 | [30] | ||
| Synonyms |
Nitroprednisolone; NCX-1004; NCX-1016; NO-prednisolone
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| MOA | Modulator | |||
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| PT-150 | Phase 1 | [31] | ||
| Synonyms |
(11R,13S,17S)-11-(1,3-benzodioxol-5-yl)-17-hydroxy-13-methyl-17-prop-1-ynyl-1,2,6,7,8,11,12,14,15,16-decahydrocyclopenta[a]phenanthren-3-one; CHEMBL3545391; PT150; PT-150; SCH 900636; SCH-900636; SCHEMBL11914193
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| MOA | Antagonist | |||
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| GSK870086 | Discontinued in Phase 2 | [32] | ||
| MOA | Modulator | |||
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| NM-135 | Discontinued in Phase 2 | [33] | ||
| Synonyms |
Glucocorticoid, Nissin Food
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| MOA | Modulator | |||
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| AZD-5423 | Discontinued in Phase 2 | [34] | ||
| Synonyms |
1034148-04-3; UNII-641H0Q518W; 641H0Q518W; 2,2,2-trifluoro-N-[(1R,2S)-1-[1-(4-fluorophenyl)indazol-5-yl]oxy-1-(3-methoxyphenyl)propan-2-yl]acetamide; 2,2,2-Tris(Fluoranyl)-~{n}-[(1~{r},2~{s})-1-[1-(4-Fluorophenyl)indazol-5-Yl]oxy-1-(3-Methoxyphenyl)propan-2-Yl]ethanamide; Acetamide, 2,2,2-trifluoro-N-[(1S,2R)-2-[[1-(4-fluorophenyl)-1H-indazol-5-yl]oxy]-2-(3-methoxyphenyl)-1-methylethyl]-;Acetamide, 2,2,2-trifluoro-N-[(1S,2R)-2-[[1-(4-fluorophenyl)-1H-indazol-5-yl]oxy]-2-(3-methoxyphenyl)-1-methylethyl]-
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| MOA | Agonist | |||
| Activity | IC50 = 0.049 nM | |||
| External Link | ||||
| WC-3027 | Discontinued in Phase 2 | [35] | ||
| Synonyms |
SEGRA, Warner Chilcott; SEGRA, Warner Chilcott/Schering AG; Selective glucocorticoid receptor agonist (dermatitis), Warner Chilcott; Selective glucocorticoid receptor agonist (dermatitis), Warner Chilcott/Schering AG
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| MOA | Agonist | |||
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| PF-251802 | Discontinued in Phase 1 | [36] | ||
| Synonyms |
PF-00251802; Selective glucocorticoid receptor agonist (1), Pfizer
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| MOA | Agonist | |||
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| Org-34116 | Terminated | [37] | ||
| MOA | Antagonist | |||
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| Hexane-1,6-Diol | Investigative | [38] | ||
| Synonyms |
1,6-HEXANEDIOL; 629-11-8; Hexamethylene glycol; 1,6-Dihydroxyhexane; Hexamethylenediol; alpha,omega-Hexanediol; .alpha.,.omega.-Hexanediol; UNII-ZIA319275I; CCRIS 8982; 6-hydroxy-1-hexanol; 1,6-Hexylene Glycol; HSDB 6488; NSC 508; EINECS 211-074-0; 1,6-Hexanediol, 97%; BRN 1633461; AI3-03307; CHEBI:43078; XXMIOPMDWAUFGU-UHFFFAOYSA-N; ZIA319275I; HEZ; 1,6hexanediol; 1.6-hexanediol; 1,6 hexanediol; 1,6-hexandiol; 1.6-hexandiol; .omega.-Hexanediol; 1,6-hexane diol; hexan-1,6-diol; 1,6-hexan-diol
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| MOA | Inhibitor | |||
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| B-Octylglucoside | Investigative | [38] | ||
| Synonyms |
29836-26-8; Octyl-beta-D-glucopyranoside; OCTYL BETA-D-GLUCOPYRANOSIDE; Octyl beta-D-glucoside; Octyl glucoside; Octyl b-D-Glucopyranoside; n-Octyl-beta-D-Glucoside; 1-O-n-Octyl-beta-D-glucopyranoside; Octyl-beta-D-glucoside; beta-D-Octyl glucoside; 1-O-Octyl-beta-D-glucopyranoside; (2R,3S,4S,5R,6R)-2-(hydroxymethyl)-6-(octyloxy)tetrahydro-2H-pyran-3,4,5-triol; UNII-V109WUT6RL; n-Octyl glucoside; n-Octyl-beta-D-glucopyranoside; Octyl-beta-D-Glucopyranose; Octyl; V109WUT6RL
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| MOA | Inhibitor | |||
| External Link | ||||
| Vamorolone | Approved | [39] | ||
| Synonyms |
vamorolone; 13209-41-1; UNII-8XP29XMB43; VBP-15; 8XP29XMB43; CHEMBL2348780; 17,21-Dihydroxy-16alpha-methylpregna-1,4,9(11)-triene-3,20-dione; A-Methyl-9,11-dehydro Prednisolone; (8S,10S,13S,14S,16R,17R)-17-hydroxy-17-(2-hydroxyacetyl)-10,13,16-trimethyl-7,8,12,14,15,16-hexahydro-6H-cyclopenta[a]phenanthren-3-one; Vamorolone [USAN]; VBP-15 free alcohol; VBP 15; EINECS 236-177-8; AC1MHYKY; Vamorolone (USAN/INN); SCHEMBL143459; GTPL9247; A)-17,21-dihydroxy-16-methylpregna-1,4,9(11)-triene-3,20-dione; ZINC33650317
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| External Link | ||||
| CORT125281 | Phase 2 | [39] | ||
| Synonyms |
Exicorilant; UNII-GTB859B7K8; GTB859B7K8; Exicorilant [INN]; SCHEMBL16737057; CORT-125281; 1781244-77-6; Methanone, ((4aR,8aS)-1-(4-fluorophenyl)-1,4,5,6,7,8,8a,9-octahydro-6-((2-methyl-2H-1,2,3-triazol-4-yl)sulfonyl)-4ah-pyrazolo(3,4-g)isoquinolin-4a-yl)(4-(trifluoromethyl)-2-pyridinyl)-
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| Activity | Ki = 12 nM | |||
| External Link | ||||
| ISIS-GCCR | Phase 2 | [39] | ||
| External Link | ||||
| ORIC-101 | Phase 1 | [39] | ||
| Synonyms |
VNLTWJIWEYPBIF-SXJSTINISA-N; 2222344-98-9
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| Activity | IC50 = 5.6 nM | |||
| External Link | ||||
| AZD9567 | Phase 1 | [39] | ||
| Synonyms |
ZQFNDBISEYQVRR-LOSJGSFVSA-N; AZD-9567; GTPL9812; SCHEMBL17643955; AZD 9567; example 1 [WO2016046260A1]; compound 15 [PMID: 29424542]; B9W; 2,2-difluoro-N-[(1R,2S)-3-methyl-1-[1-(1-methyl-6-oxopyridin-3-yl)indazol-5-yl]oxy-1-phenylbutan-2-yl]propanamide; 2,2-bis(fluoranyl)-~{N}-[(1~{R},2~{S})-3-methyl-1-[1-(1-methyl-6-oxidanylidene-pyridin-3-yl)indazol-5-yl]oxy-1-phenyl-butan-2-yl]propanamide
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| Activity | IC50 = 3.8 nM | |||
| External Link | ||||
| A-348441 | Phase 1 | [39] | ||
| Synonyms |
CHEMBL219684; SCHEMBL699533; BDBM50195155; KB-3305
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| Activity | IC50 = 1.2 nM | |||
| External Link | ||||
| 1-Methoxy-6-phenyl-6H-benzo[c]chromen-8-ylamine | Investigative | [39] | ||
| Synonyms |
CHEMBL292721; SCHEMBL7234473; MVULNNIYAGEMCC-UHFFFAOYSA-N; BDBM50144165
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| Activity | IC50 = 1937 nM | |||
| External Link | ||||
| RU26988 | Investigative | [39] | ||
| Synonyms |
RU 26988; RU-26988
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| External Link | ||||
| ENDIANDRIN A | Investigative | [39] | ||
| Synonyms |
CHEMBL228274; BDBM50216277; 4,4''-((1R,2R,3S,4S)-3,4-dimethylcyclobutane-1,2-diyl)bis(2-methoxyphenol)
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| Activity | IC50 = 900 nM | |||
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| 1-(3-CHLORO-4-FLUOROPHENYL)-2,2,2-TRIFLUORO-1-(1-(4-FLUOROPHENYL)-1H-INDAZOL-5-YL)ETHANOL (ENANTIOMERIC MIX) | Investigative | [39] | ||
| Synonyms |
CHEMBL1094231; SCHEMBL4285350; BDBM50316561; 1-(3-chloro-4-fluorophenyl)-2,2,2-trifluoro-1-(1-(4-fluorophenyl)-1H-indazol-5-yl)ethanol
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| Activity | EC50 = 93 nM | |||
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| 1-(2,3-DICHLOROPHENYL)-2,2,2-TRIFLUORO-1-(1-(4-FLUOROPHENYL)-1H-INDAZOL-5-YL)ETHANOL (ENANTIOMERIC MIX) | Investigative | [39] | ||
| Synonyms |
CHEMBL1094208; BDBM50316566; 1-(2,3-dichlorophenyl)-2,2,2-trifluoro-1-(1-(4-fluorophenyl)-1H-indazol-5-yl)ethanol
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| Activity | EC50 = 19 nM | |||
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| 2,2,2-TRIFLUORO-1-(4-FLUOROPHENYL)-1-(1-(4-FLUOROPHENYL)-1H-INDAZOL-5-YL)ETHANOL (DIASTEREOMERIC MIX) | Investigative | [39] | ||
| Synonyms |
SCHEMBL4280142; CHEMBL1095541; BDBM50316555; 2,2,2-trifluoro-1-(4-fluorophenyl)-1-[1-(4-fluorophenyl)-1H-indazol-5-yl]ethan-1-ol
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| Activity | IC50 = 86 nM | |||
| External Link | ||||
| 1-Methoxy-6-phenyl-6H-benzo[c]chromene | Investigative | [39] | ||
| Synonyms |
CHEMBL63422
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| Activity | IC50 = 1914 nM | |||
| External Link | ||||
| DI-O-METHYLENDIANDRIN A | Investigative | [39] | ||
| Synonyms |
CHEMBL388363
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| Activity | IC50 = 13000 nM | |||
| External Link | ||||
| OXDEX | Investigative | [39] | ||
| Synonyms |
Dexamethasone-17-carboxamide; CHEMBL483096; 82137-90-4; DX-17-Carboxamide; 17-Dxb; 17-Carboxamide dexamethasone; Dexamethasone-17beta-carboxamide; AC1L1YA1; DTXSID30231582; BDBM50271344; Androsta-1,4-diene-17-carboxamide, 9-fluoro-11,17-dihydroxy-16-methyl-3-oxo-, (11beta,16alpha,17alpha)-; (8S,9R,10S,11S,13S,14S,16R,17R)-9-fluoro-11,17-dihydroxy-10,13,16-trimethyl-3-oxo-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthrene-17-carboxamide
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| Activity | IC50 = 600 nM | |||
| External Link | ||||
| RU28362 | Investigative | [39] | ||
| Synonyms |
RU-28362
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| deoxycorticosterone | Investigative | [39] | ||
| Synonyms |
11-deoxycorticosterone; 21-hydroxyprogesterone
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| RU-43044 | Investigative | [39] | ||
| Synonyms |
CHEMBL78704; SCHEMBL14289561; 136959-96-1; BDBM50113782; RU43044; 17-Hydroxy-13-methyl-10-(4-methyl-benzyl)-17-prop-1-ynyl-1,2,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-cyclopenta[a]phenanthren-3-one(RU-43044)
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| Activity | IC50 = 2.4 nM | |||
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| (11-BETA)-11,21-DIHYDROXY-PREGN-4-ENE-3,20-DIONE | Investigative | [39] | ||
| Synonyms |
Corticosterone; 50-22-6; 17-Deoxycortisol; Reichstein's substance H; Kendall's compound B; Corticosteron; 11beta,21-Dihydroxyprogesterone; Compound B; Reichstein's B; 11-Hydroxycorticoaldosterone; (11beta)-11,21-Dihydroxypregn-4-ene-3,20-dione; 11beta,21-Dihydroxy-4-pregnene-3,20-dione; 4-Pregnene-11beta,21-diol-3,20-dione; 11,21-Dihydroxyprogesterone; 11Beta,21-dihydroxypregn-4-ene-3,20-dione; 11,12-Dihydroxyprogesterone; UNII-W980KJ009P; CCRIS 6753; 11-beta,21-Dihydroxypregn-3,20-dione; CHEBI:16827; NSC9705
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| External Link | ||||
| LG-120838 | Investigative | [39] | ||
| Synonyms |
CHEMBL302362; SCHEMBL4175160; SCHEMBL4175162; BDBM50067684; 5-(2-Methylbenzylidene)-2,2,4-trimethyl-1,2-dihydro-5H-1-aza-6-oxachrysene
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| Activity | Ki = 564 nM | |||
| External Link | ||||
| Epierenone | Investigative | [39] | ||
| Synonyms |
CHEMBL237122; SCHEMBL13806060
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| Activity | Ki = 1758 nM | |||
| External Link | ||||
| LGD-5552 | Investigative | [39] | ||
| Synonyms |
CHEMBL259820; SCHEMBL4166143
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| Activity | Ki = 2.4 nM | |||
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| AL-43 | Investigative | [39] | ||
| Synonyms |
AL-438; CHEMBL266282; A-240610.0; SCHEMBL4172433; BDBM50107347; A-224817.0; 5-Allyl-2,2,4-trimethyl-10-methoxy-2,5-dihydro-1H-1-aza-6-oxachrysene; 5-Allyl-10-methoxy-2,2,4-trimethyl-2,5-dihydro-1H-6-oxa-1-aza-chrysene; 5-allyl-10-methoxy-2,2,4-trimethyl-2,5-dihydro-1H-chromeno[3,4-f]quinoline; (+/-)5-Allyl-10-methoxy-2,2,4-trimethyl-2,5-dihydro-1H-6-oxa-1-aza-chrysene; (+)5-Allyl-10-methoxy-2,2,4-trimethyl-2,5-dihydro-1H-6-oxa-1-aza-chrysene
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| Activity | Ki = 1.4 nM | |||
| External Link | ||||
| CP-409069 | Investigative | [39] | ||
| Synonyms |
CHEMBL78625; SCHEMBL3114566; BDBM50113780; (2R,4aS,10aR)-4a-benzyl-2-(prop-1-ynyl)-1,2,3,4,4a,9,10,10a-octahydrophenanthrene-2,7-diol
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| Activity | Ki = 0.17 nM | |||
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| CP-394531 | Investigative | [39] | ||
| Synonyms |
UNII-227D9ED2SI; CHEMBL77779; 227D9ED2SI; 305822-63-3; SCHEMBL3111189; BDBM50113783; 2,7-Phenanthrenediol, 2-(chloroethynyl)-1,2,3,4,4a,9,10,10a-octahydro-4a-(phenylmethyl)-, (2R,4aS,10aR)-; 2,7-Phenanthrenediol, 2-(2-chloroethynyl)-1,2,3,4,4a,9,10,10a-octahydro-4a-(phenylmethyl)-, (2R,4aS,10aR)-; 4a-Benzyl-2-chloroethynyl-1,2,3,4,4a,9,10,10a-octahydro-phenanthrene-2,7-diol(CP-394531)
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| Activity | Ki = 0.1 nM | |||
| External Link | ||||
| WAY-214950 | Investigative | [39] | ||
| Synonyms |
SCHEMBL1407572; JMC517161 Compound 13; CHEMBL457977; BDBM26067
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| Activity | IC50 = 7200 nM | |||
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| 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Investigative | [39] | ||
| Synonyms |
AC-42; CHEMBL1242950; AC42; GTPL289; SCHEMBL4504348; ANTKBACNWQHQJE-UHFFFAOYSA-N; ZINC2022527; BDBM50326219; AKOS030284249; NCGC00485453-01; gamma-(4-Butylpiperidino)-2'-methylbutyrophenone; L019209; 4-(4-butylpiperdin-1-yl)-1-(2-methylphenyl)butan-1-one; 4-(4-butylpiperidin-1-yl)-1-(2-methylphenyl)butan-1-one
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| Activity | Ki >= 1000 nM | |||
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References
: m6A sites