m6A-centered Crosstalk Information

Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
Crosstalk ID
M6ACROT03081
 [1]
m6A modification EZH2 EZH2 ALKBH5 Demethylation : m6A sites Direct Enhancement Histone modification H3K27me3 EZH2 Downstream Gene
m6A Modification:
m6A Regulator RNA demethylase ALKBH5 (ALKBH5) ERASER
 Regulator Info 
m6A Target Histone-lysine N-methyltransferase EZH2 (EZH2)
 Targert Gene 
Epigenetic Regulation that have Cross-talk with This m6A Modification:
Epigenetic Regulation Type Histone modification (HistMod)
Epigenetic Regulator Histone-lysine N-methyltransferase EZH2 (EZH2) WRITER View Details
Regulated Target Histone H3 lysine 27 trimethylation (H3K27me3) View Details
Crosstalk Relationship m6A  →  Histone modification Enhancement
Crosstalk Mechanism m6A modification impacts directly histone modification through modulating the expression level of histone-associated enzymes
Crosstalk Summary Increased Histone-lysine N-methyltransferase EZH2 (EZH2) expression was due to the increased expression of m6A demethylase ALKBH5 and decreased expression of the m6A reader protein YTHDF2. YTHDF2 directly bind to the m6A modification site of EZH2 to promote EZH2 mRNA degradation in ESCs. Enhancer of zeste homology 2 (EZH2) is a methyltransferase which catalyses Histone H3 lysine 27 trimethylation (H3K27me3), leading to decreased expression levels of target genes.
Responsed Disease Endometriosis ICD-11: GA10
 Disease Info 
Full List of Potential Compound(s) Related to This m6A-centered Crosstalk
Histone-lysine N-methyltransferase EZH2 (EZH2) 74 Compound(s) Regulating the Target Click to Show/Hide the Full List
 Compound Name Tazemetostat Approved [2]
Synonyms
EPZ-6438; 1403254-99-8; EPZ6438; UNII-Q40W93WPE1; N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4'-(morpholinomethyl)-[1,1'-biphenyl]-3-carboxamide; Q40W93WPE1; EPZ 6438; E7438; (1,1'-Biphenyl)-3-carboxamide, N-((1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4'-(4-morpholinylmethyl)-
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 2.5 nM
External Link
CID: 66558664
TTD: D00EQL
DrugBank: DB12887
 Compound Name DS-3201b Phase 2 [3]
Synonyms
Valemetostat; 1809336-39-7; UNII-60RD0234VE; 60RD0234VE; 1809336-39-7 (free base); DS-3201; (2R)-7-chloro-2-[trans-4-(dimethylamino)cyclohexyl]-N-[(4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-2,4-dimethyl-1,3-benzodioxole-5-carboxamide; Valemetostat 2HCl; Valemetostat [INN]; Valemetostat (DS-3201); CHEMBL4597193; EZH1/2 inhibitor DS-3201; SCHEMBL18393626; SCHEMBL18393627; SCHEMBL18639210; EX-A3423; DS3201; NSC813381; s8926; NSC-813381; HY-109108; CS-0039740; D11551
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 126481870
TTD: DNM79H
 Compound Name CPI-1205 Phase 1/2 [4]
Synonyms
HPODOLXTMDHLLC-QGZVFWFLSA-N; 1621862-70-1; UNII-455J2479FY; CPI1205; CPI 1205; 455J2479FY; (R)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide; GTPL9115; SCHEMBL17329268; MolPort-044-560-382; KS-000006BA; EX-A1068; s8353; AKOS030628484; ZINC220982768; CS-7648; compound 13 [PMID: 27739677]; HY-100021; J3.556.402K; N-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-2-methyl-1-[(1R)-1-[1-(2,2,2-trifluoroethyl)piperidin-4-
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 78320408
TTD: D0E6AG
DrugBank: DB14581
 Compound Name SHR2554 Phase 1/2 [5]
MOA Inhibitor
External Link
TTD: DM5X0L
 Compound Name CPI-0209 Phase 1/2 [6]
MOA Inhibitor
External Link
TTD: DXL38G
 Compound Name GSK2816126 Phase 1 [7]
Synonyms
GSK 126; GSK-126
    Click to Show/Hide
MOA Modulator
Activity Ki = 0.5 nM
External Link
CID: 68210102
TTD: D05FIJ
 Compound Name PF-06821497 Phase 1 [8]
Synonyms
UNII-S4L4MM20B6; S4L4MM20B6; CHEMBL4080228; PF06821497; 1844849-10-0; 5,8-dichloro-2-[(4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-7-[(R)-methoxy(oxetan-3-yl)methyl]-3,4-dihydroisoquinolin-1(2H)-one; SCHEMBL17330426; GTPL10516; BDBM50246967; NSC800019; DB14799; HY-101571A; NSC-800019; compound 23a [PMID: 29211475]; CS-0092626; Q29209799; 1(2H)-Isoquinolinone, 5,8-dichloro-2-((1,2-dihydro-4-methoxy-6-methyl-2-oxo-3-pyridinyl)methyl)-3,4-dihydro-7-((R)-methoxy-3-oxetanylmethyl)-; 5,8-dichloro-2-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-7-[(R)-methoxy(oxetan-3-yl)methyl]-3,4-dihydroisoquinolin-1-one; CJD
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 118572065
TTD: DI1L7M
DrugBank: DB14799
 Compound Name DS-3201 Phase 1 [4]
Synonyms
QTGYNKYZRZATJB-UHFFFAOYSA-N; 701899-63-0; 2-(2-(2-Methyl-1H-imidazol-5-yl)ethyl)isoindoline-1,3-dione; 2-(2-(2-Methyl-1H-imidazol-5-yl)-ethyl)isoindoline-1,3-dione; SCHEMBL7743461; MolPort-035-945-474; MolPort-035-690-353; ZINC98086069; AKOS024459002; AKOS024262663; MCULE-2708350770; FCH4077443; AK158834; AX8292467; ST2403812; 2-[2-(2-methyl-1H-imidazol-5-yl)ethyl]-2,3-dihydro-1H-isoindole-1,3-dione
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 22627096
TTD: D0LG8T
 Compound Name HH2853 Phase 1 [9]
MOA Inhibitor
External Link
TTD: D6EU7R
 Compound Name PMID28394193-Compound-33 Patented [10]
MOA Inhibitor
Activity IC50 = 100 nM
External Link
CID: 121305270
TTD: D03MYI
 Compound Name PMID28394193-Compound-Figure3bI Patented [10]
MOA Inhibitor
External Link
TTD: D04PCW
 Compound Name PMID28394193-Compound-35 Patented [10]
MOA Inhibitor
Activity IC50 = 10 nM
External Link
TTD: D05MAR
 Compound Name PMID28394193-Compound-54 Patented [10]
MOA Inhibitor
External Link
TTD: D07CZI
 Compound Name PMID28394193-Compound-24 Patented [10]
MOA Inhibitor
Activity IC50 < 1000 nM
External Link
CID: 117807842
TTD: D08MXO
 Compound Name PMID28394193-Compound-27 Patented [10]
MOA Inhibitor
Activity IC50 < 1000 nM
External Link
CID: 76684269
TTD: D09GFF
 Compound Name PMID28394193-Compound-25 Patented [10]
MOA Inhibitor
Activity IC50 < 1000 nM
External Link
CID: 117807842
TTD: D09PQQ
 Compound Name PMID28394193-Compound-50 Patented [10]
MOA Inhibitor
Activity IC50 > 1 nM; IC50 < 2 nM; Ki > 0.01 nM; Ki < 0.04 nM
External Link
CID: 118580552
TTD: D0A0VH
 Compound Name PMID28394193-Compound-47 Patented [10]
MOA Inhibitor
Activity IC50 = 2 nM; Ki < 1 nM
External Link
CID: 118616529
TTD: D0B4TX
 Compound Name PMID28394193-Compound-21 Patented [10]
MOA Inhibitor
External Link
TTD: D0BL8W
 Compound Name PMID28394193-Compound-41 Patented [10]
MOA Inhibitor
External Link
CID: 118101320
TTD: D0BT6Y
 Compound Name PMID28394193-Compound-53 Patented [10]
MOA Inhibitor
Activity IC50 = 80 nM
External Link
CID: 121322599
TTD: D0CH4O
 Compound Name PMID28394193-Compound-Figure5aVIII Patented [10]
MOA Inhibitor
External Link
TTD: D0D1QD
 Compound Name PMID28394193-Compound-38 Patented [10]
MOA Inhibitor
External Link
CID: 78320108
TTD: D0DQ6N
 Compound Name PMID28394193-Compound-51 Patented [10]
MOA Inhibitor
Activity IC50 > 1 nM; IC50 < 2 nM; Ki > 0.01 nM; Ki < 0.04 nM
External Link
CID: 118580509
TTD: D0FC9J
 Compound Name PMID28394193-Compound-31 Patented [10]
MOA Inhibitor
Activity IC50 = 20 nM
External Link
TTD: D0FI3A
 Compound Name PMID28394193-Compound-42 Patented [10]
MOA Inhibitor
External Link
CID: 118096643
TTD: D0H4HR
 Compound Name PMID28394193-Compound-15 Patented [10]
MOA Inhibitor
External Link
TTD: D0KR2T
 Compound Name PMID28394193-Compound-52 Patented [10]
MOA Inhibitor
Activity IC50 > 1 nM; IC50 < 2 nM; Ki > 0.01 nM; Ki < 0.04 nM
External Link
CID: 118580510
TTD: D0LR5O
 Compound Name PMID28394193-Compound-32 Patented [10]
MOA Inhibitor
Activity IC50 = 500 nM
External Link
TTD: D0M1TG
 Compound Name PMID28394193-Compound-23 Patented [10]
MOA Inhibitor
Activity IC50 < 1000 nM
External Link
CID: 117807623
TTD: D0M9BY
 Compound Name PMID28394193-Compound-29 Patented [10]
MOA Inhibitor
Activity IC50 = 100 nM
External Link
TTD: D0MH8G
 Compound Name PMID28394193-Compound-30 Patented [10]
MOA Inhibitor
Activity IC50 = 16 nM
External Link
TTD: D0MO2X
 Compound Name PMID28394193-Compound-39 Patented [10]
MOA Inhibitor
External Link
TTD: D0MZ8D
 Compound Name PMID28394193-Compound-49 Patented [10]
MOA Inhibitor
Activity IC50 > 1 nM; IC50 < 2 nM; Ki > 0.01 nM; Ki < 0.04 nM
External Link
CID: 118572078
TTD: D0PB6T
 Compound Name PMID28394193-Compound-43 Patented [10]
MOA Inhibitor
External Link
CID: 118096796
TTD: D0PI5O
 Compound Name PMID28394193-Compound-40 Patented [10]
MOA Inhibitor
External Link
CID: 118095598
TTD: D0QH1J
 Compound Name PMID28394193-Compound-Figure3bIII Patented [10]
MOA Inhibitor
External Link
TTD: D0R2TQ
 Compound Name PMID28394193-Compound-36 Patented [10]
MOA Inhibitor
Activity IC50 = 316 nM
External Link
TTD: D0RD5P
 Compound Name PMID28394193-Compound-28 Patented [10]
MOA Inhibitor
Activity IC50 = 32 nM
External Link
CID: 91884579
TTD: D0S4OP
 Compound Name PMID28394193-Compound-22 Patented [10]
MOA Inhibitor
External Link
TTD: D0SQ1R
 Compound Name PMID28394193-Compound-18 Patented [10]
MOA Inhibitor
External Link
TTD: D0SY6P
 Compound Name PMID28394193-Compound-16 Patented [10]
MOA Inhibitor
External Link
TTD: D0T8QL
 Compound Name PMID28394193-Compound-44 Patented [10]
MOA Inhibitor
External Link
CID: 118096614
TTD: D0U9OH
 Compound Name PMID28394193-Compound-20 Patented [10]
MOA Inhibitor
External Link
TTD: D0UG5O
 Compound Name PMID28394193-Compound-19 Patented [10]
MOA Inhibitor
External Link
TTD: D0VF0M
 Compound Name PMID28394193-Compound-37 Patented [10]
MOA Inhibitor
External Link
CID: 78320107
TTD: D0W2KL
 Compound Name PMID28394193-Compound-Figure3bII Patented [10]
MOA Inhibitor
External Link
TTD: D0W4MW
 Compound Name PMID28394193-Compound-26 Patented [10]
MOA Inhibitor
Activity IC50 < 1000 nM
External Link
CID: 75203283
TTD: D0Z0NC
 Compound Name PMID28394193-Compound-17 Patented [10]
MOA Inhibitor
External Link
TTD: D0Z0QS
 Compound Name PMID28394193-Compound-34 Patented [10]
MOA Inhibitor
Activity IC50 = 100 nM
External Link
TTD: D0Z7GN
 Compound Name PMID28394193-Compound-56 Patented [10]
MOA Inhibitor
Activity IC50 = 0.93 nM
External Link
TTD: D01PZZ
 Compound Name PMID28394193-Compound-46 Patented [10]
MOA Inhibitor
Activity IC50 = 5 nM
External Link
CID: 102593999
TTD: D0D4UH
 Compound Name PMID28394193-Compound-57 Patented [10]
MOA Inhibitor
Activity IC50 = 6.45 nM
External Link
TTD: D0G1JR
 Compound Name PMID28394193-Compound-14 Patented [10]
MOA Inhibitor
Activity IC50 = 21900 nM
External Link
CID: 90467336
TTD: D0GT7A
 Compound Name PMID28394193-Compound-12 Patented [10]
MOA Inhibitor
Activity IC50 < 10 nM
External Link
TTD: D0H8VN
 Compound Name PMID26882240-Compound-1 Patented [11]
MOA Inhibitor
External Link
CID: 5712
TTD: D0L1TA
 Compound Name PMID28394193-Compound-55 Patented [10]
MOA Inhibitor
Activity IC50 = 8.13 nM
External Link
TTD: D0M4LK
 Compound Name PMID28394193-Compound-45 Patented [10]
MOA Inhibitor
Activity IC50 = 168000 nM
External Link
CID: 118607675
TTD: D0M8AA
 Compound Name PMID28394193-Compound-13 Patented [10]
MOA Inhibitor
Activity IC50 = 1470 nM
External Link
CID: 86765324
TTD: D0TA4N
 Compound Name EPZ005687 Investigative [12]
Synonyms
EPZ-005687; EPZ 005687
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 60160561
TTD: D02BBA
 Compound Name EI1 Investigative [13]
Synonyms
KB-145943
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 72199293
TTD: D02CIT
 Compound Name UNC1999 Investigative [14]
Synonyms
UNC 1999; UNC-1999
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 72551585
TTD: D02YXP
 Compound Name MS1943 Investigative [5]
Synonyms
2225938-17-8; SCHEMBL21271666; EX-A3962; s8918; HY-133129; CS-0112146; 6-(6-(4-(2-(2-((3r,5r,7r)-adamantan-1-yl)acetamido)ethyl)piperazin-1-yl)pyridin-3-yl)-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-1H-indazole-4-carboxamide; 6-(6-(4-(2-(2-(Adamantan-1-yl)acetamido)ethyl)piperazin-1-yl)pyridin-3-yl)-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-1H-indazole-4-carboxamide
    Click to Show/Hide
MOA Degrader
External Link
CID: 139211327
TTD: D65IMT
 Compound Name GSK343 Investigative [15]
Synonyms
compound 6 [PMID 24900432]; GSK 343
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 174 nM
External Link
CID: 71268957
TTD: D02TVQ
 Compound Name PMID28394193-Compound-11 Patented [16]
External Link
TTD: D0MH5C
 Compound Name PMID28394193-Compound-10 Patented [16]
External Link
TTD: D0MZ9P
 Compound Name PMID28394193-Compound-14 Patented [10]
MOA Inhibitor
Activity IC50 = 21900 nM
External Link
CID: 90467336
TTD: D0GT7A
 Compound Name PMID28394193-Compound-12 Patented [10]
MOA Inhibitor
Activity IC50 < 10 nM
External Link
TTD: D0H8VN
 Compound Name PMID28394193-Compound-13 Patented [10]
MOA Inhibitor
Activity IC50 = 1470 nM
External Link
CID: 86765324
TTD: D0TA4N
 Compound Name PMID28394193-Compound-56 Patented [10]
MOA Inhibitor
Activity IC50 = 0.93 nM
External Link
TTD: D01PZZ
 Compound Name PMID28394193-Compound-46 Patented [10]
MOA Inhibitor
Activity IC50 = 5 nM
External Link
CID: 102593999
TTD: D0D4UH
 Compound Name PMID28394193-Compound-57 Patented [10]
MOA Inhibitor
Activity IC50 = 6.45 nM
External Link
TTD: D0G1JR
 Compound Name PMID28394193-Compound-55 Patented [10]
MOA Inhibitor
Activity IC50 = 8.13 nM
External Link
TTD: D0M4LK
 Compound Name PMID28394193-Compound-45 Patented [10]
MOA Inhibitor
Activity IC50 = 168000 nM
External Link
CID: 118607675
TTD: D0M8AA
GA10: Endometriosis 32 Compound(s) Regulating the Disease Click to Show/Hide the Full List
 Compound Name Elagolix sodium Approved [17]
Synonyms
Elagolix sodium salt; UNII-5948VUI423; Elagolix sodium [USAN]; 5948VUI423; Elagolix sodium (USAN); SCHEMBL1641994; NBI 56418NA; NBI-56418-NA; MolPort-003-984-965; NBI-56418 NA; DQYGXRQUFSRDCH-UQIIZPHYSA-M; AKOS030524154; VA12044; KS-0000063K; KB-76766; HY-14369; AC-29671; CS-0003317; D09336
    Click to Show/Hide
External Link
CID: 24785956
TTD: D0VG7Y
 Compound Name Histrelin Approved [18]
Synonyms
Supprelin (TN)
    Click to Show/Hide
External Link
CID: 25077993
TTD: D0O7DG
 Compound Name Relugolix Phase 3 [19]
Synonyms
737789-87-6; TAK-385; TAK 385; UNII-P76B05O5V6; CHEMBL1800159; TAK-385/TAK385; P76B05O5V6; 1-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-3-methoxyurea; Relugolix [USAN:INN]; TAK385; Relugolix (JAN/INN); SCHEMBL778416; GTPL5586; DTXSID40224167; MolPort-044-567-649; AOMXMOCNKJTRQP-UHFFFAOYSA-N; EX-A1083; BCP21587; ZINC43206033; BDBM50347982; AKOS027440398; SB16721; DB11853; CS-5917
    Click to Show/Hide
External Link
CID: 10348973
TTD: D0F2WP
DrugBank: DB11853
 Compound Name Naproxen Approved [20]
Synonyms
22204-53-1; (S)-Naproxen; Naproxene; Naprosyn; (+)-Naproxen; Equiproxen; Laraflex; Naproxenum; Naproxeno; d-Naproxen; (S)-(+)-2-(6-Methoxy-2-naphthyl)propionic acid; (S)-(+)-Naproxen; Calosen; Nycopren; Naprosyne; Bonyl; Reuxen; Naixan; Axer; (+)-(S)-Naproxen; Ec-Naprosyn; (S)-2-(6-methoxynaphthalen-2-yl)propanoic acid; Flexipen; Clinosyn; Artrixen; Anexopen; Acusprain; Novonaprox; Arthrisil; Leniartil; Danaprox; Bipronyl; Artroxen; Napren; Naposin; Napflam; Genoxen; Daprox; Atiflan; Artagen; Apronax; Naprius; Nalyxan; Lefaine; Congex
    Click to Show/Hide
External Link
CID: 156391
TTD: D0DJ1B
DrugBank: DB00788
 Compound Name Nafarelin Approved [21]
Synonyms
Nafarelina; Nafareline; Nafarelinum; Synarel; NAFARELIN ACETATE; Nafarelina [Spanish]; Nafareline [French]; Nafarelinum [Latin]; HS-2018; Nafarelin (INN); Nafarelin Acetate, Hydrate; Nafarelin [INN:BAN]; Synarel (TN); RS-94991-298; 6-(3-(2-Naphthalenyl)-D-alanine)luteinizing hormone-releasing factor (pig)
    Click to Show/Hide
External Link
CID: 25077405
TTD: D08WYM
DrugBank: DB00666
 Compound Name Oestradiol valerate and dienogest Approved [22]
Synonyms
Dienogest; 65928-58-7; Dienogestrel; Dienogestum; Dienogestril; Dinagest; Natazia; Endometrion; Visanne; STS-557; STS 557; Dienogestum [Latin]; UNII-46M3EV8HHE; MJR-35; 17alpha-17-Hydroxy-3-oxo-19-norpregna-4,9-diene-21-nitrile; BAY86-5258; BAY 86-5258; 46M3EV8HHE; CHEBI:70708; 17-alpha-Cyanomethyl-17-beta-hydroxy-estra-4,9(10)-dien-3-one; 2-[(8S,13S,14S,17R)-17-hydroxy-13-methyl-3-oxo-1,2,6,7,8,11,12,14,15,16-decahydrocyclopenta[a]phenanthren-17-yl]acetonitrile; 17-alpha-Cyanomethyl-17-beta-hydroxyestra-4,9(10)-diene-3-one; Natazia (TN)
    Click to Show/Hide
External Link
CID: 68861
TTD: D04CBI
DrugBank: DB09123
 Compound Name TZTX-001 Phase 3 [23]
Synonyms
Teverelix LA; TX 12-001-HR
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External Link
TTD: D0IC7A
 Compound Name Nestorone Phase 3 [24]
Synonyms
Nestorone MDTS; Nestorone metered dose transdermal system; Nestorone transdermal spray, Acrux; ST-1435; Nestorone transdermal spray, Population Council/Acrux
    Click to Show/Hide
External Link
CID: 108059
TTD: D02HUB
DrugBank: DB14583
 Compound Name Telapristone Phase 2 [25]
Synonyms
Telapristone acetate; Proellex; 198414-31-2; UNII-1K9EYK92PQ; CDB-4124; 1K9EYK92PQ; Telapristone acetate [USAN]; Telapristone acetate (USAN); CCRIS 9331; CDB 4124; SCHEMBL374762; CHEMBL2105694; DTXSID60173587; RU-44675; 17alpha-Acetoxy-11beta-(4-(dimethylamino)phenyl)-21-methoxy-19-norpregna-4,9-dien-3,20-dione; D09972; 19-Norpregna-4,9-diene-3,20-dione, 17-(acetyloxy)-11-(4-(dimethylamino)phenyl)-21-methoxy-, (11beta)-; A-Acetoxy-21-methoxy-11
    Click to Show/Hide
External Link
CID: 20761503
TTD: D0U8AS
 Compound Name F-8-IL-10 fusion protein Phase 2 [26]
Synonyms
Dekavil; F-8-IL-10; F-8-IL-10 fusion protein (rheumatoid arthritis/endometriosis); F-8-IL-10 fusion protein (rheumatoid arthritis/endometriosis), Philogen
    Click to Show/Hide
External Link
TTD: D0T4KG
 Compound Name PGL-2 Phase 2 [27]
External Link
TTD: D0I3RN
 Compound Name BAY 98-7196 Phase 2 [28]
External Link
TTD: D0E7VY
 Compound Name KLH-2109 Phase 2 [29]
External Link
CID: 16656889
TTD: D08FKH
 Compound Name Vilaprisan Phase 2 [30]
Synonyms
UNII-IN59K53GI9; BAY1002670; IN59K53GI9; 1262108-14-4; Vilaprisan [INN]; BAY 1002670; Vilaprisan [USAN:INN]; Vilaprisan (USAN/INN); SCHEMBL2121854; CHEMBL3989936; BCP24069; DB11971; 20,20,21,21,21-Pentafluoro-17-hydroxy-11beta-(4-(methanesulfonyl)phenyl)-19-nor-17alpha-pregna-4,9-dien-3-one; 19-Norpregna-4,9-dien-3-one, 20,20,21,21,21-pentafluoro-17-hydroxy-11-(4-(methylsulfonyl)phenyl)-, (11beta,17alpha)-
    Click to Show/Hide
External Link
CID: 50915138
TTD: D07YGK
DrugBank: DB11971
 Compound Name PGL-2001 Phase 2 [31]
Synonyms
Steroid sulfatase inhibitor (endometriosis), PregLem
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CID: 6918339
TTD: D04ZND
DrugBank: DB06597
 Compound Name BGS-649 Phase 2 [32]
External Link
TTD: D02XMD
 Compound Name ASP-1707 Phase 2 [33]
External Link
TTD: D02ROU
 Compound Name BAY 1817080 Phase 1 [34]
Synonyms
Eliapixant
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TTD: DF0PI8
 Compound Name Alfa-interferon Phase 1 [35]
External Link
TTD: D0SX9C
 Compound Name PF-4418948 Phase 1 [36]
Synonyms
PF-04418948; Prostaglandin E2 EP2 subtype antagonist (endometriosis), Pfizer
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CID: 25114442
TTD: D0S5EF
DrugBank: DB12024
 Compound Name BAY-1817080 Phase 1 [37]
External Link
TTD: D0NF1D
 Compound Name PF-2413873 Phase 1 [38]
Synonyms
PF-02413873
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CID: 16662425
TTD: D0K2HA
 Compound Name BAY 1026153 Phase 1 [39]
External Link
TTD: D0FJ0W
 Compound Name PMID27215781-Compound-28 Patented [40]
External Link
TTD: D03YAA
 Compound Name Asoprisnil Discontinued in Phase 3 [41]
Synonyms
J867; J-867; Asoprisnil (USAN/INN); 11beta-(4-((E)-(Hydroxyimino)methyl)phenyl)-17beta-methoxy-17-(methoxymethyl)estra-4,9-dien-3-one
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CID: 9577221
TTD: D0W5RL
DrugBank: DB06680
 Compound Name FP-1096 Discontinued in Phase 3 [42]
External Link
TTD: D0K8MQ
 Compound Name ASP-0265 Terminated [43]
External Link
TTD: D0J3PS
 Compound Name NS398 Terminated [44]
Synonyms
ns-398; 123653-11-2; NS 398; N-(2-Cyclohexyloxy-4-nitrophenyl)methanesulfonamide; N-[2-(Cyclohexyloxy)-4-nitrophenyl]methanesulfonamide; CHEMBL7162; CHEBI:73458; Methanesulfonamide, N-(2-(cyclohexyloxy)-4-nitrophenyl)-; n-(2-cyclohexyloxy-4-nitrophenyl)methane sulfonamide; N-(2-Cyclohexyloxy-4-nitro-phenyl)-methanesulfonamide; Taisho NS 398; SR-01000597479; N-[2-Cyclohexyloxy-4-nitrophenyl]methanesulfonamide; N-(2-(cyclohexyloxy)-4-nitrophenyl)methanesulfonamide; CCRIS 8523; KTDZCOWXCWUPEO-UHFFFAOYSA-N; Tocris-0942
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CID: 4553
TTD: D09BKE
DrugBank: DB14060
 Compound Name LHRH Investigative [45]
Synonyms
SCHEMBL7378993
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CID: 36523
TTD: D0V6KF
DrugBank: DB00644
 Compound Name PF-02367982 Investigative [46]
Synonyms
CHEMBL1083754; BDBM50318934
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CID: 11964844
TTD: D0H2MF
 Compound Name Recombinant human CC10 Investigative [47]
Synonyms
Claragen-WH; Recombinant human CC10 (intravaginal, endometriosis/infertility); Recombinant human CC10 (intravaginal, endometriosis/infertility), Clarassance; Uteroglobin (intravaginal, endometriosis/infertility), Clarassance
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TTD: D05RZJ
 Compound Name DXL-1215 Investigative [47]
Synonyms
Monoclonal antibody (endometriosis), InNexus
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TTD: D01UBV
References
Ref 1 The involvement of RNA N6-methyladenosine and histone methylation modification in decidualization and endometriosis-associated infertility. Clin Transl Med. 2024 Feb;14(2):e1564. doi: 10.1002/ctm2.1564.
Ref 2 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
Ref 3 Development of new agents for peripheral T-cell lymphoma. Expert Opin Biol Ther. 2019 Mar;19(3):197-209. doi: 10.1080/14712598.2019.1572746. Epub 2019 Jan 29.
Ref 4 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
Ref 5 Epigenetics and beyond: targeting writers of protein lysine methylation to treat disease. Nat Rev Drug Discov. 2021 Apr;20(4):265-286. doi: 10.1038/s41573-020-00108-x. Epub 2021 Jan 19.
Ref 6 ClinicalTrials.gov (NCT04104776) A Study of CPI-0209 in Patients With Advanced Tumors. U.S. National Institutes of Health.
Ref 7 National Cancer Institute Drug Dictionary (drug id 756211).
Ref 8 Optimization of Orally Bioavailable Enhancer of Zeste Homolog 2 (EZH2) Inhibitors Using Ligand and Property-Based Design Strategies: Identification of Development Candidate (R)-5,8-Dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3,4-dihydroisoquinolin-1(2H)-one (PF-06821497). J Med Chem. 2018 Feb 8;61(3):650-665. doi: 10.1021/acs.jmedchem.7b01375. Epub 2017 Dec 27.
Ref 9 Clinical pipeline report, company report or official report of HaiHe Biopharma.
Ref 10 EZH2 inhibitors: a patent review (2014-2016). Expert Opin Ther Pat. 2017 Jul;27(7):797-813. doi: 10.1080/13543776.2017.1316976. Epub 2017 Apr 20.
Ref 11 Hypoxia-inducible factor (HIF) inhibitors: a patent survey (2011-2015). Expert Opin Ther Pat. 2016;26(3):309-22. doi: 10.1517/13543776.2016.1146252. Epub 2016 Feb 16.
Ref 12 A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells. Nat Chem Biol. 2012 Nov;8(11):890-6. doi: 10.1038/nchembio.1084. Epub 2012 Sep 30.
Ref 13 Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation. Proc Natl Acad Sci U S A. 2012 Dec 26;109(52):21360-5. doi: 10.1073/pnas.1210371110. Epub 2012 Dec 10.
Ref 14 An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1. ACS Chem Biol. 2013;8(6):1324-34. doi: 10.1021/cb400133j. Epub 2013 Apr 24.
Ref 15 Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2. ACS Med Chem Lett. 2012 Oct 19;3(12):1091-6. doi: 10.1021/ml3003346. eCollection 2012 Dec 13.
Ref 16 TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751.
Ref 17 2018 FDA drug approvals. Nat Rev Drug Discov. 2019 Feb;18(2):85-89. doi: 10.1038/d41573-019-00014-x.
Ref 18 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3884).
Ref 19 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
Ref 20 New drugs in development for the treatment of endometriosis. Expert Opin Investig Drugs. 2008 Aug;17(8):1187-202. doi: 10.1517/13543784.17.8.1187.
Ref 21 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3902).
Ref 22 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7654).
Ref 23 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800038089)
Ref 24 ClinicalTrials.gov (NCT00455156) Study of the Safety, Efficacy and Cycle Control of a Contraceptive Vaginal Ring. U.S. National Institutes of Health.
Ref 25 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014404)
Ref 26 ClinicalTrials.gov (NCT02270632) A Randomized, Placebo-controlled Phase II Clinical Trial to Evaluate the Safety and Efficacy of F8IL10 Dekavil) in Patients With Active RA Receiving MTX. U.S. National Institutes of Health.
Ref 27 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026648)
Ref 28 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800040286)
Ref 29 ClinicalTrials.gov (NCT01533532) A Randomized, Placebo-controlled, Double-blind Study of KLH-2109 in Patients With Endometriosis (2). U.S. National Institutes of Health.
Ref 30 ClinicalTrials.gov (NCT02465814) Assess Safety and Efficacy of Vilaprisan in Patients With Uterine Fibroids.
Ref 31 ClinicalTrials.gov (NCT01631981) PGL2001 Proof of Concept Study in Symptomatic Endometriosis. U.S. National Institutes of Health.
Ref 32 ClinicalTrials.gov (NCT01190475) BGS649 Monotherapy in Moderate to Severe Endometriosis Patients. U.S. National Institutes of Health.
Ref 33 ClinicalTrials.gov (NCT01767090) A Study to Assess the Effectiveness and Safety of Different Doses of ASP1707 Compared to Placebo for Endometriosis Associated Pelvic Pain. U.S. National Institutes ofHealth.
Ref 34 ClinicalTrials.gov (NCT04471337) Study on the Safety of BAY1817080 How it is Tolerated and the Way the Body Absorbs, Distributes and Gets Rid of the Study Drug Given to Participants With Moderate Renal Impairment and End Stage Renal Disease Requiring Dialysis Compared With Matched Participants With Normal Renal Function. U.S. National Institutes of Health.
Ref 35 A phase I trial of alpha-interferon in combination with pentostatin in hematologic malignancies. Med Pediatr Oncol. 1991;19(4):276-82.
Ref 36 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5817).
Ref 37 Antibodies and venom peptides: new modalities for ion channels. Nat Rev Drug Discov. 2019 May;18(5):339-357. doi: 10.1038/s41573-019-0013-8.
Ref 38 ClinicalTrials.gov (NCT00800618) A Study To Investigate How The Body Handles Multiple Doses Of PF-0243873 And To Investigate The Effect Of PF-02413873 On Sex Hormone Levels In Healthy Young Women. U.S. National Institutes of Health.
Ref 39 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800035640)
Ref 40 Cannabinoid receptor 2 (CB2) agonists and antagonists: a patent update.Expert Opin Ther Pat. 2016 Jul;26(7):843-56.
Ref 41 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2883).
Ref 42 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018823)
Ref 43 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028953)
Ref 44 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002344)
Ref 45 Discovery of a novel, potent, and orally active nonpeptide antagonist of the human luteinizing hormone-releasing hormone (LHRH) receptor. J Med Chem. 1998 Oct 22;41(22):4190-5.
Ref 46 Optimisation of a pyrazole series of progesterone antagonists; Part 1. Bioorg Med Chem Lett. 2010 Jun 1;20(11):3384-6.
Ref 47 The ChEMBL database in 2017. Nucleic Acids Res. 2017 Jan 4;45(D1):D945-D954.