m6A-centered Crosstalk Information

Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
Crosstalk ID
M6ACROT02020
 [1]
DNA methylation DNMT3A FTO Direct Inhibition m6A modification PPARA PPARA FTO Demethylation : m6A sites
m6A Modification:
m6A Regulator Fat mass and obesity-associated protein (FTO) ERASER
 Regulator Info 
m6A Target Peroxisome proliferator-activated receptor alpha (PPARalpha/PPARA)
 Targert Gene 
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 Inhibition of DNA methyltransferases (DNMT1, DNMT3A, and DNMT3B) by 5-azacytidine (5-aza) reversed alcohol-induced kidney injury and decreased the mRNA and protein levels of FTO. Importantly, we found that FTO, the m6A demethylase, epigenetically modified Peroxisome proliferator-activated receptor alpha (PPARalpha/PPARA) in a YTH domain family 2 (YTHDF2)-dependent manner, which resulted in inflammation in alcoholic kidney injury models. In conclusion, our findings indicate that alcohol increases the methylation of PPAR-alpha m6A by FTO-mediated YTHDF2 epigenetic modification, which ultimately leads to the activation of NLRP3 inflammasomes and NF-kappaB-driven renal inflammation in the kidney.
Responsed Disease Renal ischemia-reperfusion injury ICD-11: NB92.0Y
 Disease Info 
Responsed Drug 5-azacytidine
 Drug Info 
Pathway Response RNA degradation hsa03018
Cell Process mRNA stability
In-vitro Model
 HK2 Normal Acipenser baerii CVCL_YE28
In-vivo Model Male C57BL/6 mice (aged 6-8 weeks) were acclimated with the Lieber-DeCarli liquid diet control ad libitum for 1 week. Afterward, mice received either Lieber-DeCarli diet ethanol (6% vol/vol) or Lieber-DeCarli diet control (isocaloric maltose dextrin) for 4 and 8 weeks.
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
 Compound Name PMID27376512-Compound-Figure3CN Patented [2]
MOA Inhibitor
Activity EC50 = 1100 nM
External Link
CID: 117968550
TTD: D02VTV
 Compound Name PMID27376512-Compound-Figure3CG Patented [2]
MOA Inhibitor
Activity EC50 = 2400 nM
External Link
CID: 117967861
TTD: D03LZO
 Compound Name PMID27376512-Compound-Figure3CM Patented [2]
MOA Inhibitor
Activity EC50 = 1100 nM
External Link
CID: 117976053
TTD: D0F8AB
 Compound Name PMID27376512-Compound-Figure2aExample1 Patented [2]
MOA Inhibitor
Activity IC50 = 3000 nM
External Link
CID: 71521835
TTD: D01LUJ
 Compound Name PMID27376512-Compound-MTC-424 Patented [2]
MOA Inhibitor
Activity IC50 = 1940 nM
External Link
TTD: D02WRM
 Compound Name PMID27376512-Compound-MTC-427 Patented [2]
MOA Inhibitor
Activity IC50 = 295 nM
External Link
TTD: D0HA0J
 Compound Name PMID27376512-Compound-MTC-422 Patented [2]
MOA Inhibitor
Activity IC50 = 1430 nM
External Link
TTD: D0QY0N
 Compound Name PMID27376512-Compound-MTC-423 Patented [2]
MOA Inhibitor
Activity IC50 = 363 nM
External Link
TTD: D0W9VZ
Peroxisome proliferator-activated receptor alpha (PPARalpha/PPARA) 76 Compound(s) Regulating the Target Click to Show/Hide the Full List
 Compound Name Bezafibrate Approved [3]
Synonyms
Azufibrat; Befibrat; Befizal; BezaLande; BezaPuren; Bezabeta; Bezacur; Bezafibrat; Bezafibrato; Bezafibratum; Bezafisal;Bezalip; Bezamerck; Bezatol; Cedur; Difaterol; Durabezur; Eulitop; Lipox; Reducterol; Sklerofibrat; Solibay; Azupharma Brand of Bezafibrate; Bayer Brand of Bezafibrate; Berlin Chemie Brand of Bezafibrate; Betapharm Brand of Bezafibrate; Beza Lande; Beza Puren; Bezafibrat PB; Bezafibrate Azupharma Brand; Bezafibrate Bayer Brand; Bezafibrate Betapharm Brand; Bezafibrate Cryopharma Brand; Bezafibrate Elfar Brand; Bezafibrate Hennig Brand; Bezafibrate Hexal Brand; Bezafibrate Isis Brand; Bezafibrate Lakeside Brand; Bezafibrate Merckle Brand; Bezafibrate Roche Brand; Bezafibrate Synthelabo Brand; Bezafibrate TAD Brand; Bezafibrate Teva Brand; Bezafibrato [Spanish]; Bezalip Retard; Bezatol SR; Boehringer Mannheim Brand of Bezafibrate; Cryopharma Brand of Bezafibrate; Elfar Brand of Bezafibrate;Hennig Brand of Bezafibrate; Hexal Brand of Bezafibrate; Isis Brand of Bezafibrate; Lakeside Brand of Bezafibrate; Merckle Brand of Bezafibrate; Regadrin B; Roche Brand of Bezafibrate; Synthelabo Brand of Bezafibrate; TAD Brand of Bezafibrate; Teva Brand of Bezafibrate; BM 15075; LO 44; BF-759; BM 15.075; BM-15075; BM15.075; Berlin-Chemie Brand of Bezafibrate; Beza-Lande; Beza-Puren; Bezafibrate Berlin-Chemie Brand; Bezafibrato [INN-Spanish]; Bezafibratum [INN-Latin]; Bezalip (TN); Bezatol SR (TN); PB, Bezafibrat; BM-15.075; Bezafibrate (JP15/USAN/INN); Bezafibrate [USAN:BAN:INN:JAN]; A-[4-(4-chlorobenzoylaminoethyl)phenoxy]isobutyric acid; 2-(4-{2-[(4-chlorobenzoyl)amino]ethyl}phenoxy)-2-methylpropanoic acid; 2-(p-(2-(p-Chlorobenzamido)ethyl)phenoxy)-2-methylpropionic acid; 2-[4-(2-[4-Chlorobenzamido]ethyl)-phenoxy]-2-methylpropanoic acid; 2-[4-[2-(4-Chlorobenzamido)ethyl]phenoxy]-2-methylpropanoic acid; 2-[4-[2-(4-Chlorobenzamido)ethyl]phenoxy]isobutyric Acid; 2-[4-[2-[(4-chlorobenzoyl)amino]ethyl]phenoxy]-2-methylpropanoic acid
    Click to Show/Hide
MOA Agonist
Activity EC50 = 7100 nM
External Link
CID: 39042
TTD: D00WCX
DrugBank: DB01393
 Compound Name Pemafibrate Approved [4]
Synonyms
K-877
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MOA Agonist
Activity EC50 = 1 nM
External Link
CID: 11526038
TTD: D04QIE
DrugBank: DB15212
 Compound Name Fenofibrate Approved [5]
Synonyms
Ankebin; Antara; Controlip; Durafenat; Elasterate; Elasterin; FNF; Fenobeta; Fenobrate; Fenofanton; Fenofibrato; Fenofibratum; Fenogal; Fenoglide; Fenomax; Fenotard; Finofibrate; Fulcro; Lipanthyl; Lipantil; Liparison; Lipidex; Lipidil; Lipifen; Lipirex; Lipoclar; Lipofen; Lipofene; Liposit; Lipsin; Lofibra; Luxacor; Nolipax; Pharmavit; Phenofibrate; Procetofen; Procetofene; Proctofene; Protolipan; Secalip; Sedufen; Supralip; Tricor; Triglide; AbZ Brand of Procetofen; Abbott Brand of Procetofen; Aliud Brand of Procetofen; Antara Micronized Procetofen; Anto Brand of Procetofen; Apo Feno Micro; Apo Fenofibrate; Apotex Brand of Procetofen; Azupharma Brand of Procetofen; Betapharm Brand of Procetofen; Bouchara Brand of Procetofen; Ct Arzneimittel Brand of Procetofen; Fenofibrat AL; Fenofibrat AZU; Fenofibrat AbZ; Fenofibrat FPh; Fenofibrat Heumann; Fenofibrat Hexal; Fenofibrat Stada; Fenofibrat ratiopharm; Fenofibrat von ct; Fenofibrate Debat; Fenofibrate MSD; Fournier Brand of Procetofen; GNR Pharma Brand of Procetofen; Gate Brand of Procetofen; Gen Fenofibrate; Genpharm Brand of Procetofen; Heumann Brand of Procetofen; Hexal Brand of Procetofen; Knoll Brand of Procetofen; Lichtenstein Brand of Procetofen; Lipidil Micro; Lipidil Supra; Lipidil Ter; MTW Brand of Procetofen; MTW Fenofibrat; Merck dura Brand of Procetofen; Novartis Brand of Procetofen; Novo Fenofibrate; Novopharm Brand of Procetofen; Nu Fenofibrate; Nu Pharm Brand of Procetofen; PMS Fenofibrate Micro;Pharmascience Brand of Procetofen; Procetofen Reliant Brand; Q Pharm Brand of Procetofen; Ratiopharm Brand of Procetofen; Reliant Brand of Procetofen; Schering Plough Brand of Procetofen; Stadapharm Brand of Procetofen; United Drug Brand of Procetofen; F 6020; LF 178; LF178; AZU, Fenofibrat; Antara (TN); Antara (micronized); Apo-Fenofibrate; CIP-Fenofibrate; Ct-Arzneimittel Brand of Procetofen; Debat, Fenofibrate; FENOFIBRATE (MICRONIZED); Fenofibrat-ratiopharm; Fenofibrate IDD-P; Fenofibrate [INN:BAN]; Fenofibrato [INN-Spanish]; Fenofibratum [INN-Latin]; Fenogal (TN); GNR-Pharma Brand of Procetofen; GRS-027; Gen-Fenofibrate; Heumann, Fenofibrat; Hexal, Fenofibrat; LCP-Feno; LCP-FenoChol; LF-178; Lipanthyl (TN); Lipantil (TN); Lipidil (TN); Lipidil-Ter; Lipofen (TN); Lofibra (TN); MTW-Fenofibrat; Micronized Procetofen, Antara; Novo-Fenofibrate; Nu-Fenofibrate; Nu-Pharm Brand of Procetofen; PMS-Fenofibrate Micro; Procetofen, Antara Micronized; Q-Pharm Brand of Procetofen; Schering-Plough Brand of Procetofen; Stada, Fenofibrat; TRICOR (MICRONIZED); Tricor (TN); Triglide (TN); Trilipix (TN); Apo-Feno-Micro; Fenocor-67 (TN); Fenofibrate (JAN/INN); Isopropyl 2-[4-(4-chlorobenzoyl)phenoxy]-2-methylpropanoate; Isopropyl 2-(4-(4-chlorobenzoyl)phenoxy)-2-methylpropionate; Isopropyl 2-(p-(p-chlorobenzoyl)phenoxy)-2-methylpropionate
    Click to Show/Hide
MOA Agonist
Activity IC50 = 1000 nM
External Link
CID: 3339
TTD: D07XGR
DrugBank: DB01039
 Compound Name Ciprofibrate Approved [5]
Synonyms
Ciprofibrato; Ciprofibratum; Ciprol; Hiperlipen; Hyperlipen; Lipanor; Modalim; Oroxadin; Sanofi Synthelabo brand of ciprofibrate; Sanofi Winthrop brand of ciprofibrate; C 0330; WIN 35833; Ciprofibrato [INN-Spanish]; Ciprofibratum [INN-Latin]; Win 35,833; Win-35833; Ciprofibrate (USAN/INN); Ciprofibrate [USAN:BAN:INN]; 2-(4-(2,2-Dichlorocyclopropyl)phenoxy)2-methylpropanoic acid; 2-(p-(2,2-Dichlorocyclopropyl)phenoxy)-2-methylpropionic acid; 2-[4-(2,2-Dichlorocyclopropyl)phenoxy]-2-methylpropanoic acid; 2-[p-(2,2-Dichlorocyclopropyl)phenoxy]-2-methylpropanoic acid; 2-{4-[2,2-dichlorocyclopropyl]phenoxy}-2-methylpropanoic acid; 2-{[4-(2,2-dichlorocyclopropyl)phenyl]oxy}-2-methylpropanoic acid
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MOA Agonist
Activity EC50 = 900 nM
External Link
CID: 2763
TTD: D0EJ6O
DrugBank: DB09064
 Compound Name Lobeglitazone Approved [6]
Synonyms
Lobeglitazone sulfate; CKD-501; Dual PPARalpha/delta (type 2 diabetes), Chong Kun Dang
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MOA Agonist
External Link
CID: 9826451
TTD: D04BCB
DrugBank: DB09198
 Compound Name Ragaglitazar Phase 3 [7]
Synonyms
DRF-2725; (2S)-2-ETHOXY-3-{4-[2-(10H-PHENOXAZIN-10-YL)ETHOXY]PHENYL}PROPANOIC ACID; CHEMBL24038; (2S)-2-ethoxy-3-[4-(2-phenoxazin-10-ylethoxy)phenyl]propanoic acid; DRF; 1nyx; DRF2725; AC1L9KVW; 2-Ethoxy-3-[4-(2-phenoxazin-10-yl-ethoxy)-phenyl]-propionic acid; GTPL2664; SCHEMBL4822459; WMUIIGVAWPWQAW-DEOSSOPVSA-N; NN-622; BDBM50109551; DB07675; NNC-61-0029; (-)-DRF-2725; (S)-2-Ethoxy-3-[4-(2-phenoxazin-10-yl-ethoxy)-phenyl]-propionic acid; (2S)-2-ethoxy-3-{4-[2-(phenoxazin-10-yl)ethoxy]phenyl}propanoic acid
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MOA Modulator
Activity Ki = 980 nM
External Link
CID: 447458
TTD: D02NHD
DrugBank: DB07675
 Compound Name CS-038 Phase 3 [8]
Synonyms
Chiglitazar; CS-00098; PPAR alpha/gamma agonist (diabetes), Chipscreen Biosciences
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MOA Modulator
External Link
CID: 71402018
TTD: D0F5JH
 Compound Name TESAGLITAZAR Phase 3 [9]
Synonyms
251565-85-2; Galida; (S)-2-Ethoxy-3-(4-(4-((methylsulfonyl)oxy)phenethoxy)phenyl)propanoic acid; AZ 242; AZ-242; AR-H039242XX; (S)-2-Ethoxy-3-{4-[2-(4-methanesulfonyloxyphenyl)ethoxy]phenyl}propionic acid; UNII-6734037O3L; (S)-2-Ethoxy-3-{4-[2-(4-methanesulfonyloxy-phenyl)-ethoxy]-phenyl}-propionic acid; (2S)-2-ethoxy-3-[4-[2-(4-methylsulfonyloxyphenyl)ethoxy]phenyl]propanoic acid; BR-44608; 6734037O3L; (S)-2-Ethoxy-3-[4-[2-(4-methanesulfonyloxyphenyl)ethoxy]phenyl]propanoic acid
    Click to Show/Hide
MOA Modulator
Activity EC50 = 37 nM
External Link
CID: 208901
TTD: D0H1NL
DrugBank: DB07399
 Compound Name GFT-505 Phase 3 [10]
Synonyms
GFT-1007; PPAR activator (dyslipidemia/type 2 diabetes), Genfit
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MOA Modulator
Activity EC50 = 10 nM
External Link
CID: 9864881
TTD: D0LW1Y
DrugBank: DB05187
 Compound Name MURAGLITAZAR Phase 3 [11]
Synonyms
331741-94-7; Pargluva; BMS-298585; UNII-W1MKM70WQI; BMS 298585; W1MKM70WQI; CHEMBL186179; N-[(4-Methoxyphenoxy)carbonyl]-N-[[4-[2-(5-methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl]methyl]glycine; N-((4-methoxyphenoxy)carbonyl)-N-((4-(2-(5-methyl-2-phenyl-4-oxazolyl)ethoxy)phenyl)methyl)glycine; BMS298585; Muraglitazar [USAN:INN]; CCRIS 9258; AC1L4FVP; Muraglitazar (USAN/INN); DSSTox_CID_31508; DSSTox_RID_97393; DSSTox_GSID_57719; SCHEMBL676469; DTXSID9057719; CTK8E8901; MolPort-006-395-259; IRLWJILLXJGJTD-UHFFFAOYSA-N
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MOA Modulator
Activity EC50 = 40 nM
External Link
CID: 206044
TTD: D0M3UT
DrugBank: DB06510
 Compound Name ZYH-1 Phase 3 [12]
Synonyms
Metabolism disorder treatment, Zydus-Cadila; PPAR alpha/gamma modulator (dyslipdemia), Zydus-Cadila
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MOA Modulator
External Link
TTD: D0T7MN
 Compound Name Imiglitazar Phase 3 [13]
Synonyms
TAK-559
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MOA Modulator
Activity EC50 = 5 nM
External Link
CID: 9890879
TTD: D0VU5M
DrugBank: DB12511
 Compound Name LY-518674 Phase 2 [14]
Synonyms
LY-674; 2-Methyl-2-[4-[3-[1-(4-methylbenzyl)-5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl]propyl]phenoxy]propionic acid
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MOA Agonist
Activity EC50 = 42 nM
External Link
CID: 135449333
TTD: D0I5IM
DrugBank: DB12988
 Compound Name GFT14 Phase 2 [15]
MOA Agonist
External Link
TTD: D0RJ0V
 Compound Name ZYH7 Phase 2 [16]
MOA Agonist
External Link
TTD: DE6GF4
 Compound Name Naveglitazar Phase 2 [17]
Synonyms
LY 519818; LY-818; PPAR alpha/gamma co-agonists, Lilly/Ligand
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MOA Modulator
Activity EC50 = 2800 nM
External Link
CID: 9888484
TTD: D04BPS
DrugBank: DB12662
 Compound Name ONO-5129 Phase 2 [18]
Synonyms
Dual PPAR alpha/gamma agonist (metabolic disorder), Ono
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MOA Modulator
External Link
TTD: D0PP8G
 Compound Name CDT-fenofibrate Phase 1 [19]
MOA Agonist
External Link
TTD: D00HYD
 Compound Name AVE0897 Phase 1 [20]
MOA Agonist
External Link
TTD: D01UJK
 Compound Name TPST-1120 Phase 1 [21]
MOA Antagonist
External Link
TTD: DF8M1T
 Compound Name Oxeglitazar Phase 1 [22]
Synonyms
EMD-336340; EML-16156; EML-4156; LM-4156
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MOA Modulator
External Link
CID: 6445229
TTD: D03RJZ
 Compound Name GW-409544 Phase 1 [23]
Synonyms
GW-409544X; GW-544; GW-6471; Lipid regulators, Ligand/Glaxo
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MOA Modulator
Activity Ki = 2 nM
External Link
CID: 446642
TTD: D0AX9S
 Compound Name PMID25416646-Compound-Figure5-H Patented [24]
MOA Agonist
External Link
TTD: D05AUY
 Compound Name Flavonoid derivative 8 Patented [24]
Synonyms
PMID25416646-Compound-Figure5-B
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MOA Agonist
External Link
TTD: D0HW6Y
 Compound Name PMID25416646-Compound-Figure5-A Patented [24]
MOA Agonist
External Link
TTD: D0O5IN
 Compound Name Aleglitazar Discontinued in Phase 3 [25]
Synonyms
RO7; Aleglitazar (USAN); 2-methoxy-3-[4-[2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethoxy]benzothiophen-7-yl]propanoic Acid
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MOA Agonist
Activity EC50 = 50 nM
External Link
CID: 10274777
TTD: D0B9EN
DrugBank: DB08915
 Compound Name NS-220 Discontinued in Phase 2 [26]
Synonyms
R-1593; Cis-2-Methyl-5-[4-[5-methyl-2-(4-methylphenyl)oxazol-4-yl]butyl]-1,3-dioxane-2-carboxylic acid
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MOA Agonist
Activity EC50 = 10 nM
External Link
CID: 9947731
TTD: D08LZI
 Compound Name KRP-101 Discontinued in Phase 2 [27]
Synonyms
PPAR alpha agonist (hyperlipidemia), Kyorin
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MOA Agonist
Activity EC50 = 0.615 nM
External Link
CID: 9825046
TTD: D0B8JQ
 Compound Name BM-17.0744 Discontinued in Phase 2 [28]
Synonyms
K-111; 12-(4-Chlorophenyl)-2,2-dichlorododecanoic acid
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MOA Activator
External Link
CID: 9929731
TTD: D0Q8UU
 Compound Name AVE-8134 Discontinued in Phase 2 [29]
Synonyms
PPAR alpha agonist, Genfit
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MOA Agonist
External Link
CID: 11625114
TTD: D0R5QQ
 Compound Name KRP-297 Discontinued in Phase 2 [30]
Synonyms
MK 767; MK-767; KRP297; KRP 297; 213252-19-8; L410198; L 410198; 5-((2,4-Dioxo-5-thiazolidinyl)methyl)-2-methoxy-N-((4-(trifluoromethyl)phenyl)methyl)benzamide; Benzamide, 5-((2,4-dioxo-5-thiazolidinyl)methyl)-2-methoxy-N-((4-(trifluoromethyl)phenyl)methyl)-; 5-[(2,4-dioxo-1,3-thiazolidin-5-yl)methyl]-2-methoxy-N-[[4-(trifluoromethyl)phenyl]methyl]benzamide; NFFXEUUOMTXWCX-UHFFFAOYSA-N; SCHEMBL3922; AC1L45TL; MLS006010319; GTPL2677; CTK4E6495; MolPort-018-657-358; AKOS005067111; NCGC00263123-01; SMR004701384
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MOA Modulator
External Link
CID: 151183
TTD: D02RAU
 Compound Name Reglixane Discontinued in Phase 2 [18]
MOA Modulator
External Link
TTD: D02ZKL
 Compound Name AVE-0847 Discontinued in Phase 2 [31]
Synonyms
PPAR alpha/gamma agonists (diabetes/dyslipidemia), Genfit; PPAR alpha/gamma agonists (diabetes/dyslipidemia), aventis; PPAR alpha/gamma agonists (diabetes/dyslipidemia), sanofi-aventis
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MOA Modulator
External Link
TTD: D0W2IU
 Compound Name Sodelglitazar Discontinued in Phase 2 [32]
Synonyms
447406-78-2; UNII-6G973E04VI; 6G973E04VI; GW677954; Sodelglitazar [USAN:INN]; 2-[4-[[[2-[2-Fluoro-4-(trifluoromethyl)phenyl]-4-methyl-1,3-thiazol-5-yl]methyl]sulfanyl]-2-methylphenoxy]-2-methylpropanoic acid; 2-(4-(((2-(2-Fluoro-4-(trifluoromethyl)phenyl)-4-methyl-1,3-thiazol-5-yl)methyl)sulfanyl)-2-methylphenoxy)-2-methylpropanoic acid; Sodelglitazar (USAN); SCHEMBL4822839; CHEMBL2104984; DTXSID90196289; ZUGQWAYOWCBWGM-UHFFFAOYSA-N; ZINC1553281; AN-28238; ACM447406782; FT-0743554; D06647; 406S782; Propanoic ac
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MOA Agonist
External Link
CID: 9805950
TTD: D01JGG
 Compound Name Indeglitazar Discontinued in Phase 2 [33]
Synonyms
PLX-204
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MOA Agonist
External Link
CID: 11395145
TTD: D09OHP
DrugBank: DB07724
 Compound Name GSK-677954 Discontinued in Phase 2 [34]
Synonyms
SCHEMBL2065429
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MOA Agonist
External Link
CID: 56603715
TTD: D0S6KX
 Compound Name AR-H049020 Discontinued in Phase 1 [35]
MOA Agonist
External Link
TTD: D04FTB
 Compound Name LG-101280 Discontinued in Phase 1 [36]
Synonyms
LSN-862; LY-WWW; LY-YYY; PPAR modulators, Ligand/Lilly
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MOA Modulator
External Link
TTD: D09SLU
 Compound Name DRF 10945 Discontinued in Phase 1 [37]
MOA Agonist
External Link
TTD: D0W3YW
 Compound Name MP-136 Discontinued in Phase 1 [38]
MOA Agonist
External Link
TTD: D0Z3XO
 Compound Name E-3030 Discontinued in Phase 1 [39]
Synonyms
Dual PPAR alpha/gamma agonists, Eisai
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MOA Modulator
External Link
CID: 11949481
TTD: D06PHO
 Compound Name LY-929 Discontinued in Phase 1 [40]
Synonyms
LY-510929; Dual PPAR-alpha/PPAR-gamma agonists
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MOA Agonist
Activity EC50 = 8.913 nM
External Link
CID: 9890585
TTD: D0B0EB
 Compound Name MC-3001 Preclinical [41]
Synonyms
MC-3004; PPAR-alpha agonists, MaxoCore
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MOA Agonist
External Link
TTD: D04PBS
 Compound Name PIRINIXIC ACID Preclinical [42]
Synonyms
50892-23-4; WY-14643; [4-Chloro-6-(2,3-xylidino)-2-pyrimidinylthio]acetic acid; WY-14,643; WY14643; Wyeth 14,643; Wy 14643; Pirinixic acid [INN]; WY-14643 (Pirinixic Acid); (4-Chloro-6-(2,3-xylidino)-2-pyrimidinylthio)acetic acid; UNII-86C4MRT55A; C14H14ClN3O2S; CCRIS 133; Acidum pirinixicum [INN-Latin]; Acide pirinixique [INN-French]; Acido pirinixico [INN-Spanish]; NSC310038; NSC-310038; NSC 310038; BRN 0759945; ((4-Chloro-6-((2,3-dimethylphenyl)amino)-2-pyrimidinyl)thio)acetic acid; Acetic acid, ((4-chloro-6-(
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MOA Inhibitor
Activity EC50 = 130 nM
External Link
CID: 5694
TTD: D09XCX
 Compound Name Romazarit Preclinical [43]
Synonyms
ORE-5007; Metabolic modulator (obesity/hyperlipidemia), Ore Pharmaceuticals
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MOA Modulator
External Link
CID: 71321
TTD: D0U2FN
 Compound Name MC-3002 Preclinical [18]
Synonyms
PPAR dual agonists, MaxoCore
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MOA Modulator
External Link
TTD: D08WOE
 Compound Name CS-207 Terminated [44]
Synonyms
CS-307; PPAR alpha agonists (cardiovascular disease associated with dyslipidemia); PPAR alpha agonists (cardiovascular disease associated with dyslipidemia), Chipscreen Biosciences
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MOA Agonist
External Link
TTD: D03CUS
 Compound Name KRP-105 Terminated [45]
MOA Agonist
External Link
TTD: D0BB1X
 Compound Name BVT-142 Terminated [46]
Synonyms
BVT-13; BVT-142 analogs, Biovitrum; Dual PPAR alpha/gamma agonists (type II diabetes); Dual PPAR alpha/gamma agonists (type II diabetes), Biovitrum
    Click to Show/Hide
MOA Agonist
External Link
TTD: D0I0RF
 Compound Name Sipoglitazar Terminated [12]
Synonyms
TAK-654
    Click to Show/Hide
MOA Modulator
External Link
CID: 9825652
TTD: D0OW6Z
 Compound Name CS-204 Terminated [47]
Synonyms
CS-00088; PPAR alpha/gamma/delta agonist (type 2 diabetes), Chipscreen Bioscience
    Click to Show/Hide
MOA Agonist
External Link
TTD: D0V0TT
 Compound Name GW7647 Investigative [48]
Synonyms
GW-7647; GW 7647
    Click to Show/Hide
MOA Agonist
Activity Ki = 0.0541 nM
External Link
CID: 3392731
TTD: D00TFA
 Compound Name CP-775146 Investigative [49]
Synonyms
CP775146
    Click to Show/Hide
MOA Agonist
External Link
CID: 10410059
TTD: D01KPN
 Compound Name GSK-9578 Investigative [5]
Synonyms
KYQNYMXQHLMADB-UHFFFAOYSA-N; GW 9578; GW9578; 247923-29-1; GW-9578; UNII-H32ABL87X4; H32ABL87X4; CHEMBL278590; SCHEMBL68327; GTPL2673; BDBM28799; CTK8E7867; GSK9578; DTXSID10179493; MolPort-009-019-367; ZINC14115100; Propanoic acid, 2-((4-(2-((((2,4-difluorophenyl)amino)carbonyl)heptylamino)ethyl)phenyl)thio)-2-methyl-; RT-013144; J-015674; 289722-11-8; 2-{[4-(2-{[(2,4-difluorophenyl)carbamoyl](heptyl)amino}ethyl)phenyl]sulfanyl}-2-methylpropanoic acid; 2-[4-[2-[(2,4-difluorophenyl)carbamoyl-heptylamino]ethyl]phenyl]sulfanyl-2-methylpropanoic
    Click to Show/Hide
MOA Inhibitor
Activity EC50 = 6 nM
External Link
CID: 9870304
TTD: D05CLM
 Compound Name Fibrates Investigative [50]
Synonyms
clofibric acid; 882-09-7; 2-(4-Chlorophenoxy)-2-methylpropanoic acid; Chlorofibrinic acid; Clofibrinic acid; Chlorfibrinic acid; Clofibrin; 2-(4-CHLOROPHENOXY)-2-METHYLPROPIONIC ACID; Chlorophibrinic acid; PCIB; Clofibrate free acid; Clofibrinsaeure; Regulipid; Regadrin; PCPIB; 2-(p-Chlorophenoxy)-2-methylpropionic acid; 2-(4-Chlorophenoxy)isobutyric Acid; 4-CPIB; 2-(p-Chlorophenoxy)isobutyric acid; Propanoic acid, 2-(4-chlorophenoxy)-2-methyl-; alpha-(p-Chlorophenoxy)isobutyric acid; Acido clofibrico; Acide clofibrique; Acidum c
    Click to Show/Hide
MOA Agonist
Activity EC50 = 39600 nM
External Link
CID: 2797
TTD: D06RRD
 Compound Name BMS-687453 Investigative [51]
Synonyms
1000998-59-3; UNII-39TL5L7XDX; BMS 687453; 39TL5L7XDX; 2-{[(3-{[2-(4-chlorophenyl)-5-methyl-1,3-oxazol-4-yl]methoxy}phenyl)methyl](methoxycarbonyl)amino}acetic acid; SCHEMBL2742714; CHEMBL1089501; BDBM28800; EX-A592; BCP14808; ZINC44460341; AKOS030526188; CS-5523; DA-48472; HY-10678; FT-0749275; J-690001; 2-[[3-[[2-(4-chlorophenyl)-5-methyl-1,3-oxazol-4-yl]methoxy]phenyl]methyl-methoxycarbonylamino]acetic acid; 7HA; N-(3-{[2-(4-chlorophenyl)-5-methyl-1,3-oxazol-4-yl]methoxy}benzyl)-N-(methoxycarbonyl)glycine
    Click to Show/Hide
MOA Inhibitor
Activity EC50 = 9.6 nM
External Link
CID: 16725047
TTD: D08UWZ
 Compound Name pristanic acid Investigative [52]
Synonyms
UNII-6P06977L1A; 6P06977L1A; (2S,6R,10R)-2,6,10,14-tetramethylpentadecanoic acid; L,d,D-pristanic acid; GTPL2676; Pristanic acid, (2S,6R,10R)-; UNII-5FMQ2908AP component PAHGJZDQXIOYTH-KURKYZTESA-N; Pentadecanoic acid, 2,6,10,14-tetramethyl-, (2S,6R,10R)-
    Click to Show/Hide
MOA Agonist
External Link
CID: 123929
TTD: D0EN7T
 Compound Name eicosatetranoic acid Investigative [53]
Synonyms
ETYA; 5,8,11,14-eicosatetraynoic acid; 1191-85-1; icosa-5,8,11,14-tetraynoic acid; Octadehydroarachidonic acid; MLS000069514; SMR000058640; MLS-0002886.0001; Ro 31428; Ro 3-1428; Opera_ID_402; AC1Q5VYB; Spectrum5_001952; cid_1780; CBiol_001864; SCHEMBL68751; KBioSS_000169; BSPBio_001449; KBioGR_000169; GTPL2669; CHEMBL458328; BML2-F04; AC1L1C80; CTK0H5766; CHEBI:94483; KBio3_000338; KBio2_002737; KBio3_000337; KBio2_005305; KBio2_000169; BDBM31752; DTXSID20152318; MGLDCXPLYOWQRP-UHFFFAOYSA-N; HMS3402I11; Bio1_001128
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MOA Agonist
External Link
CID: 1780
TTD: D0G9IP
 Compound Name 8S-HETE Investigative [54]
Synonyms
8-hydroxyeicosatetraenoic acid
    Click to Show/Hide
MOA Agonist
External Link
CID: 5283154
TTD: D0K6TI
 Compound Name LL-6531 Investigative [38]
Synonyms
PPAR modulators (diabetes), Lupin
    Click to Show/Hide
MOA Modulator
External Link
TTD: D0K8HA
 Compound Name Deoxy-Bigchap Investigative [55]
Synonyms
Big CHAP, Deoxy; N,N-bis-(3-D-Gluconamidopropyl)deoxycholamide; AC1MTX5H; DTXSID70394140; AN-35629; FT-0629429; N,N -Bis(3-D -gluconamidopropyl)- deoxy-cholamide; N-[3-[4-(3,12-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl)pentanoyl-[3-(2,3,4,5,6-pentahydroxyhexanoylamino)propyl]amino]propyl]-2,3,4,5,6-pentahydroxyhexanamide
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 446320
TTD: D0S4GK
DrugBank: DB01890
 Compound Name (E)-4-(3,5-dimethoxystyryl)phenol Investigative [38]
Synonyms
Pterostilbene; 537-42-8; 4-(3,5-Dimethoxystyryl)phenol; 3',5'-Dimethoxy-4-stilbenol; trans-pterostilbene; 4-[(E)-2-(3,5-dimethoxyphenyl)ethenyl]phenol; pterostilben; 4-[(E)-2-(3,5-dimethoxyphenyl)vinyl]phenol; UNII-26R60S6A5I; 3,5-Dimethoxy-4'-hydroxy-trans-stilbene; 3,5-Dimethoxy-4'-hydroxystilbene; 18259-15-9; trans-3,5-dimethoxy-4'-hydroxystilbene; CHEMBL83527; CHEBI:8630; VLEUZFDZJKSGMX-ONEGZZNKSA-N; 4-((E)-2-(3,5-dimethoxyphenyl)ethenyl)phenol; 26R60S6A5I; Pterostilbene, Pterocarpus
    Click to Show/Hide
MOA Agonist
External Link
CID: 5281727
TTD: D00AII
 Compound Name AD-5061 Investigative [13]
Synonyms
AD-7057; AD7057; AD 7057; AD5061; AD 5061
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MOA Agonist
External Link
CID: 9953271
TTD: D00EOP
 Compound Name GW-2331 Investigative [56]
Synonyms
190844-95-2; PPAR ligand, Glaxo Wellcome
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MOA Modulator
Activity EC50 < 20 nM
External Link
CID: 657048
TTD: D01POG
 Compound Name TZD18 Investigative [57]
Synonyms
TZD 18; TZD-18
    Click to Show/Hide
MOA Agonist
External Link
CID: 9827261
TTD: D04JOG
 Compound Name (9Z,12E)-12-nitrooctadeca-9,12-dienoic acid Investigative [58]
Synonyms
12-Nitrolinoleic acid; 12-Nitro-9Z,12Z-octadecadienoic acid; CHEMBL554608; CHEBI:34150; AC1NQZV1; C13958; SCHEMBL2371323; BDBM50295045; LMFA01120002; 12-Nitro-9-cis,12-cis-octadecadienoic acid; (9Z,12Z)-12-Nitrooctadeca-9,12-dienoic acid
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 9600 nM
External Link
CID: 5282316
TTD: D06GYO
 Compound Name reglitazar Investigative [59]
Synonyms
JTT-501
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MOA Agonist
External Link
CID: 154000
TTD: D08XGH
DrugBank: DB04971
 Compound Name DRF 2519 Investigative [60]
Synonyms
5-[[4-[2-(4-Oxo-2H-1,3-benzoxazin3(4H)-yl)ethoxy]phenyl]methyl2,4-thiazolidinedione; SCHEMBL6953746; GTPL2671; CHEMBL1491825; DTXSID5040754; NOCAS_40754; CTK8F9377; API0008459; NCGC00165785-01; NCGC00164420-01; SR-05000000444; SR-05000000444-2
    Click to Show/Hide
MOA Agonist
External Link
CID: 9908833
TTD: D0M8VN
 Compound Name (E)-12-Nitrooctadec-12-enoic Acid Investigative [58]
Synonyms
CHEMBL549351; BDBM50295043; (E)-12-Nitro-12-octadecenoic acid
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1600 nM
External Link
CID: 44221100
TTD: D0M9LL
 Compound Name (E)-13-Nitrooctadec-12-enoic Acid Investigative [58]
Synonyms
CHEMBL540732
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MOA Inhibitor
Activity IC50 = 1100 nM
External Link
CID: 44221101
TTD: D0P5QM
 Compound Name ZY H2 Investigative [61]
Synonyms
ZYH2
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MOA Modulator
External Link
TTD: D0Z4MH
 Compound Name LY-465608 Investigative [62]
Synonyms
LY465608; LY 465608
    Click to Show/Hide
MOA Agonist
Activity EC50 = 149.5 nM
External Link
CID: 9890319
TTD: D0Z7OX
 Compound Name DB-900 Investigative [63]
MOA Agonist
External Link
TTD: D01ARG
 Compound Name L-796449 Investigative [64]
Synonyms
UNII-O937X0Z5EM; CHEMBL278994; O937X0Z5EM; 194608-80-5; KAPDPGZDHUCILF-UHFFFAOYSA-N; GTPL2689; SCHEMBL4296303; BDBM50085040; Benzeneacetic acid, 3-chloro-4-((3-((3-phenyl-7-propyl-6-benzofuranyl)oxy)propyl)thio)-; L796449; L 796449; L-796,449; 3-chloro-4-(3-(3-phenyl-7-propylbenzofuran-6-yloxy)propylthio)-phenylacetic acid; {3-Chloro-4-[3-(3-phenyl-7-propyl-benzofuran-6-yloxy)-propylsulfanyl]-phenyl}-acetic acid; 2-[3-chloro-4-[3-[(3-phenyl-7-propyl-1-benzofuran-6-yl)oxy]propylsulfanyl]phenyl]acetic acid
    Click to Show/Hide
MOA Inhibitor
Activity EC50 = 4.1 nM
External Link
CID: 9891946
TTD: D09JII
 Compound Name L-165461 Investigative [64]
Synonyms
CHEMBL279053; SCHEMBL6753428; GTPL2690; BDBM50126016; AKOS027321335; L165461; L 165461; 3-Chloro-4-[3-(3-ethyl-7-propyl-1,2-benzisoxazole-6-yloxy)propylthio]benzeneacetic acid; 2-(3-chloro-4-(3-(3-ethyl-7-propylbenzo[d]isoxazol-6-yloxy)propylthio)phenyl)acetic acid; {3-Chloro-4-[3-(3-ethyl-7-propyl-benzo[d]isoxazol-6-yloxy)-propylsulfanyl]-phenyl}-acetic acid; 2-[3-chloro-4-[3-[(3-ethyl-7-propyl-1,2-benzoxazol-6-yl)oxy]propylsulfanyl]phenyl]acetic acid
    Click to Show/Hide
MOA Inhibitor
Activity EC50 = 247 nM
External Link
CID: 9889841
TTD: D0F0MP
 Compound Name N-oleoylethanolamide Investigative [65]
Synonyms
n-Oleoylethanolamine; oleoylethanolamide; N-(2-Hydroxyethyl)oleamide; 111-58-0; Oleylethanolamide; N-oleoyl ethanolamine; Oleamide MEA; Oleoyl monoethanolamide; Oleoyl Ethanolamide; N-(2-Hydroxyethyl)-9-octadecenamide; N-(Hydroxyethyl)oleamide; UNII-1HI5J9N8E6; (Z)-N-(2-hydroxyethyl)octadec-9-enamide; Oleic acid ethanolamide; N-(9Z-octadecenoyl)-ethanolamine; EINECS 203-884-8; OEA; MLS002153155; CHEMBL280065; 1HI5J9N8E6; (9Z)-N-(2-hydroxyethyl)octadec-9-enamide; Monoethanolamine oleic acid amide; CHEBI:71466; NOE
    Click to Show/Hide
MOA Agonist
Activity EC50 = 110 nM
External Link
CID: 5283454
TTD: D07MBC
References
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Ref 46 A new class of peroxisome proliferator-activated receptor agonists with a novel binding epitope shows antidiabetic effects. J Biol Chem. 2004 Sep 24;279(39):41124-30. doi: 10.1074/jbc.M401552200. Epub 2004 Jul 15.
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Ref 58 Activation of peroxisome proliferator-activated receptor gamma (PPARgamma) by nitroalkene fatty acids: importance of nitration position and degree of unsaturation. J Med Chem. 2009 Aug 13;52(15):4631-9. doi: 10.1021/jm900326c.
Ref 59 Pharmacological profiles of a novel oral antidiabetic agent, JTT-501, an isoxazolidinedione derivative. Eur J Pharmacol. 1999 Jan 8;364(2-3):211-9. doi: 10.1016/s0014-2999(98)00832-2.
Ref 60 Antidiabetic and hypolipidemic potential of DRF 2519--a dual activator of PPAR-alpha and PPAR-gamma. Eur J Pharmacol. 2004 May 3;491(2-3):195-206. doi: 10.1016/j.ejphar.2004.03.034.
Ref 61 The ChEMBL database in 2017. Nucleic Acids Res. 2017 Jan 4;45(D1):D945-D954.
Ref 62 Design and synthesis of alpha-aryloxy-alpha-methylhydrocinnamic acids: a novel class of dual peroxisome proliferator-activated receptor alpha/gamma agonists. J Med Chem. 2004 May 6;47(10):2422-5. doi: 10.1021/jm0342616.
Ref 63 CN patent application no. 102459215, 3-(4-aminophenyl)-2-furancarboxylic acid derivative and pharmaceutically acceptable salt thereof.
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Ref 65 Oleoylethanolamide, an endogenous PPAR-alpha agonist, lowers body weight and hyperlipidemia in obese rats. Neuropharmacology. 2005 Jun;48(8):1147-53. doi: 10.1016/j.neuropharm.2005.02.013. Epub 2005 Apr 21.