m6A-centered Crosstalk Information

Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
Crosstalk ID
M6ACROT03130
 [1]
Histone modification H3K27ac HDAC11 ALKBH5 Indirect Inhibition m6A modification Htr3a Htr3a YTHDF2 : m6A sites
m6A Modification:
m6A Regulator YTH domain-containing family protein 2 (YTHDF2) READER
 Regulator Info 
m6A Target 5-hydroxytryptamine receptor 3A (HTR3A)
 Targert Gene 
Epigenetic Regulation that have Cross-talk with This m6A Modification:
Epigenetic Regulation Type Histone modification (HistMod)
Epigenetic Regulator Histone deacetylase 11 (HDAC11) ERASER View Details
Regulated Target Histone H3 lysine 27 acetylation (H3K27ac) View Details
Downstream Gene ALKBH5 View Details
Crosstalk Relationship Histone modification  →  m6A Inhibition
Crosstalk Mechanism histone modification indirectly regulates m6A modification through downstream signaling pathways
Crosstalk Summary HDAC11 downregulation induced by nerve injury increases Histone H3 lysine 27 acetylation (H3K27ac), facilitating the binding of the transcription factor forkhead box protein D3 (FOXD3) to the ALKBH5 promoter and promoting Alkbh5 transcription. The increased ALKBH5 erases m6A sites in 5-hydroxytryptamine receptor 3A (HTR3A) messenger RNA (mRNA), resulting in an inability of YT521-B homology domain 2 (YTHDF2) to bind to Htr3a mRNA, thus causing an increase in 5-HT3A protein expression and 5-HT3 channel currents.
Responsed Disease Neuropathic pain ICD-11: 8E43.0
 Disease Info 
In-vitro Model
 NCI-H1299 Lung large cell carcinoma Homo sapiens CVCL_0060
A-549 Lung adenocarcinoma Homo sapiens CVCL_0023
In-vivo Model Mice were randomly divided into different groups (at least n = 5 each group). H1299-RR cells or A549 cells (5 × 106) treated in different manners were harvested and inoculated subcutaneously into the left dorsal flank of mice.
Full List of Potential Compound(s) Related to This m6A-centered Crosstalk
5-hydroxytryptamine receptor 3A (HTR3A) 49 Compound(s) Regulating the Target Click to Show/Hide the Full List
 Compound Name Dolasetron Approved [2]
Synonyms
Dolasetronum; Dolasteron; Anzemet (TN); Dolasetron (INN); Dolasetron [INN:BAN]; Dolasetronum [INN-Latin]; 3-oxooctahydro-2h-2,6-methanoquinolizin-8-yl 1h-indole-3-carboxylate
    Click to Show/Hide
MOA Antagonist
External Link
CID: 3033818
TTD: D00YLW
DrugBank: DB00757
 Compound Name Palonosetron Approved [3]
Synonyms
Aloxi; Onicit; Palonosetron [INN]; Aloxi (TN); RS 25233-197; RS 25259-197; RS-25233-197; RS-25259-197; (S-(R*,R*))-2-(1-Azabicyclo(2.2.2)oct-3-yl)-2,3,3a,4,5,6-hexahydro-1H-benz(de)isoquinolin-1-one
    Click to Show/Hide
MOA Antagonist
Activity Ki = 0.03162 nM
External Link
CID: 6337614
TTD: D04FVU
DrugBank: DB00377
 Compound Name Alosetron Approved [4]
Synonyms
Lotronex; Lotrpnex; ALOSETRON HYDROCHLORIDE; Alosetron HCl; Alosetron hydrochloride [USAN]; Alosetron monohydrochloride; GR 68755; GR 68755X; GR 68755c; GR68755; Alosetron (INN); Alosetron [INN:BAN]; Alosetron hydrochloride (USAN); GR-68755C; Lotronex (TN); Lotrpnex (TN); 1H-Pyrido(4,3-b)indol-1-one, 2,3,4,5-tetrahydro-5-methyl-2((5-methyl-1H-imidazol-4-yl)methyl)-, monohydrochloride; 1H-Pyrido(4,3-b)indol-1-one, 2,3,4,5-tetrahydro-5-methyl-2-((5-methyl-1H-imidazol-4-yl)methyl)-, monohydrochloride; 1H-Pyrido[4,3-b]indol-1-one, 2,3,4,5-tetrahydro-5-methyl-2-[(4-methyl-1H-imidazol-5-yl)methyl]-, hydrochloride (1:1); 1H-Pyrido[4,3-b]indol-1-one, 2,3,4,5-tetrahydro-5-methyl-2-[(5-methyl-1H-imidazol; 1H-Pyrido[4,3-b]indol-1-one, 2,3,4,5-tetrahydro-5-methyl-2-[(5-methyl-1H-imidazol-4-yl)methyl]-(9CI); 2,3,4,5-Tetrahydro-5-methyl-2-((5-methyl-1H-imidazol-4-yl)methyl)-1H-pyrido(4,3-b)indol-1-one; 2,3,4,5-Tetrahydro-5-methyl-2-((5-methylimidazol-4-yl)methyl)-1H-pyrido(4,3-b)indol-1-one monohydrochloride; 2,3,4,5-tetrahydro-5-methyl-2-((5-methylimidazol-4-yl)methyl)-1H-pyridol(4,3-b)indol-1-one monohydrochloride; 2,3,4,5-tetrahydro-5-methyl-2-[(5-methyl-1H-imidazol-4-yl)methyl]-1H-pyrido[4,3-b]indol-1-one, monohydrochloride; 5-methyl-2-[(5-methyl-1H-imidazol-4-yl)methyl]-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indol-1-one; 5-methyl-2-[(5-methyl-1H-imidazol-4-yl)methyl]-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indol-1-one hydrochloride; 5-methyl-2-[(5-methyl-1H-imidazol-4-yl)methyl]-3,4-dihydropyrido[4,3-b]indol-1-one; 5-methyl-2-[(5-methyl-1H-imidazol-4-yl)methyl]-3,4-dihydropyrido[4,3-b]indol-1-one hydrochloride
    Click to Show/Hide
MOA Antagonist
Activity Ki = 0.5 nM
External Link
CID: 2099
TTD: D06GKN
DrugBank: DB00969
 Compound Name Tropisetron Approved [5]
Synonyms
Navoban; Novaban; TKT; ICS-205930; Navoban (TN); Tropisetron (INN); [(1R,5S)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl] 1H-indole-3-carboxylate; (3-endo)-8-methyl-8-azabicyclo[3.2.1]oct-3-yl 1H-indole-3-carboxylate
    Click to Show/Hide
MOA Antagonist
Activity Ki = 2.7 nM
External Link
CID: 656665
TTD: D0K0KH
DrugBank: DB11699
 Compound Name Procaine Approved [6]
Synonyms
Allocaine; Anticort; Anuject; Duracaine; Gerokit; Gerovital; Jenacain; Jenacaine; Nissocaine; Norocaine; Novocain; Novocaine; Procain; Procaina; Procainum; Scurocaine; Spinocaine; Solution of novocain; Factor H3; SP01; SP01A; Stoff H3; Vitamin H3; Anticort (TM); Diethylaminoethyl p-aminobenzoate; Gerovital H-3; Novocain (TN); P-Aminobenzoyldiethylaminoethanol; P-Aminobenzyoyldiethylaminoethanol; Procaina [INN-Spanish]; Procaine (INN); Procaine [INN:BAN]; Procaine, base; Procainum [INN-Latin]; SP-01A; Solution of novocain (TN); Beta-Diethylaminoethyl 4-aminobenzoate; P-Aminobenzoic acid 2-diethylaminoethyl ester; Beta-(Diethylamino)ethyl 4-aminobenzoate; Beta-(Diethylamino)ethyl p-aminobenzoate; BENZOIC ACID,4-AMINO,2-DIETHYLAMINOETHYL ESTER PROCAIN BASE; Benzoic acid, 4-amino-, 2-(diethylamino)ethyl ester; Benzoic acid, p-amino-, 2-(diethylamino)ethyl ester; 2-(Diethylamino)ethyl 4-aminobenzoate; 2-(Diethylamino)ethyl p-aminobenzoate; 2-(Diethylamino)ethyl-4-aminobenzoate; 2-Diethylaminoethyl 4-aminobenzoate; 2-Diethylaminoethyl p-aminobenzoate; 2-Diethylaminoethylester kyseliny p-aminobenzoove; 2-Diethylaminoethylester kyseliny p-aminobenzoove [Czech]; 4-Aminobenzoesaeure-beta-diethylaminoethylester; 4-Aminobenzoic acid 2-(diethylamino) ethyl ester; 4-Aminobenzoic acid diethylaminoethyl ester
    Click to Show/Hide
MOA Antagonist
External Link
CID: 4914
TTD: D0TZ1G
DrugBank: DB00721
 Compound Name Levetiracetam Approved [5]
Synonyms
102767-28-2; Keppra; (S)-2-(2-Oxopyrrolidin-1-yl)butanamide; Keppra XR; Levetiracetamum; ucb L059; (2S)-2-(2-oxopyrrolidin-1-yl)butanamide; UCB-L 059; UCB-L059; Spritam; (S)-alpha-Ethyl-2-oxo-1-pyrrolidineacetamide; (-)-(S)-alpha-Ethyl-2-oxo-1-pyrrolidineacetamide; SIB-S1; UNII-44YRR34555; 1-Pyrrolidineacetamide, alpha-ethyl-2-oxo-, (alphaS)-; UCB-22059; Levetiracetamum [INN-Latin]; Levetiractam; CHEBI:6437; ucb L060; Levetiracetam In Sodium Chloride; 44YRR34555; Levroxa; 1-Pyrrolidineacetamide, alpha-ethyl-2-oxo-,; Leviteracetam; Torleva; Levetiracetam [INN]; Etiracetam levo-isomer; Keppra (TN); L-059; Etiracetam, S-isomer; Keppra, Keppra XR),Levetiracetam; Levetriacetam
    Click to Show/Hide
MOA Antagonist
External Link
CID: 5284583
TTD: D0E1XL
DrugBank: DB01202
 Compound Name Palonosetron + fosnetupitant Approved [7]
MOA Antagonist
External Link
TTD: D0K5IP
 Compound Name Cilansetron Phase 3 [8]
Synonyms
Calmactin; DU-123265; KC-9946; Cilansetron (USAN/INN)
    Click to Show/Hide
MOA Modulator
External Link
CID: 6918107
TTD: D0Z2MB
DrugBank: DB04885
 Compound Name BEMESETRON Discontinued in Phase 3 [9]
Synonyms
3-Tropanyl-3,5-dichlorobenzoate; MDL 72222; MDL-72222; C15H17Cl2NO2; CHEMBL376379; 40796-97-2; Tropyl 3,5-dichlorobenzoate; 8-Methyl-8-azabicyclo[3.2.1]oct-3-yl 3,5-dichlorobenzoate; Bemesetron [USAN:INN]; Bemesetronum [INN-Latin]; 3,5-Dichloro-benzoic acid 8-methyl-8-aza-bicyclo[3.2.1]oct-3-yl ester; SR-01000075587; Tropanyl 3,5-dichlorobenzoate; 1alphaH,5alphaH-Tropan-3alpha-yl 3,5-dichlorobenzoate; endo-8-Methyl-8-azabicyclo(3.2.1)oct-3-yl 3,5-dichlorobenzoate; (8-methyl-8-azabicyclo[3.2.1]octan-3-yl) 3,5-dichlorobenzo
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 2.5 nM
External Link
CID: 671690
TTD: D0V3GT
 Compound Name YM-114 Discontinued in Phase 2 [10]
Synonyms
KAE-393; (R)-5-(2,3-Dihydro-1H-indol-1-ylcarbonyl)-4,5,6,7-tetrahydro-1H-benzimidazole hydrochloride
    Click to Show/Hide
MOA Antagonist
External Link
CID: 132963
TTD: D02WGN
 Compound Name Norcisapride Discontinued in Phase 2 [11]
Synonyms
84946-16-7; CHEMBL1748; 4-Amino-5-chloro-2-methoxy-N-(3-methoxy-4-piperidyl)benzamide; 4-amino-5-chloro-2-methoxy-N-(3-methoxy-4-piperidinyl)benzamide; (4-Amino-5-chloro-2-methoxy)-N-[3-methoxy(4-piperidyl)]benzamide; 4-amino-5-chloro-2-methoxy-N-(3-methoxypiperidin-4-yl)benzamide; Benzamide,4-amino-5-chloro-2-methoxy-N-[(3S,4R)-3-methoxy-4-piperidinyl]-, hydrochloride(1:1); EINECS 284-619-3; AC1MI81F; SCHEMBL593405; CTK4E8653; OMLDMGPCWMBPAN-UHFFFAOYSA-N; BDBM50301927; AKOS030254741; API0006151; DB-076176
    Click to Show/Hide
MOA Inhibitor
Activity EC50 = 2300 nM
External Link
CID: 3019427
TTD: D0K1SZ
 Compound Name ATI-17000 Preclinical [12]
Synonyms
CompB; J-113397; UNII-00M5444DIY; CHEMBL357076; 00M5444DIY; J113397; 1-[(3R,4R)-1-(cyclooctylmethyl)-3-(hydroxymethyl)piperidin-4-yl]-3-ethylbenzimidazol-2-one; 1-[(3R,4R)-1-cyclooctylmethyl-3-hydroxymethyl-4-piperidyl]-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one; AC1NSK6N; J-113,397; 1-(1-cyclooctylmethyl-3-hydroxymethyl-4-piperidyl)-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one; 256640-45-6; SCHEMBL875219; J 113397; GTPL1691; (+)-J-113397; ZINC1483900; BDBM50083230; NCGC00344513-02; 2H-Benzimidazol-2-one,
    Click to Show/Hide
MOA Antagonist
External Link
CID: 5311194
TTD: D0M1YN
 Compound Name AS-8112 Terminated [13]
MOA Antagonist
External Link
TTD: D08KDP
 Compound Name BP4.879a Terminated [14]
MOA Antagonist
External Link
CID: 5311254
TTD: D0V1SD
 Compound Name 5-hydroxyindole Investigative [15]
Synonyms
1H-Indol-5-ol; 1953-54-4; INDOL-5-OL; 5-Hydroxy-1H-indole; Hydroxy-5 indole; 5-Indolol; UNII-320UN7XZYN; Hydroxy-5-indole; Hydroxy-5 indole [French]; CCRIS 4422; 5-Hydroxyindole, 97%; EINECS 217-782-6; MFCD00005677; NSC 87503; BRN 0112349; 320UN7XZYN; CHEBI:89649; LMIQERWZRIFWNZ-UHFFFAOYSA-N; NSC-87503; 5-hydroxy-indole; Hydroxy-5 indole [French]; 5-hydroxylindole; 5-hydroxy-indol; 5-hydroxy indole; 3fuh; 5H1; zlchem 359; 5Hydroxy-1H-indole; PubChem7263; 1-H-indol-5-ol; 1H-indol-5-ol.; 4b3c; ACMC-1BQT3; WLN: T56 BMJ GQ
    Click to Show/Hide
MOA Modulator (allosteric modulator)
External Link
CID: 16054
TTD: D00EJS
 Compound Name TMB-8 Investigative [16]
Synonyms
8-(Diethylamino)octyl 3,4,5-trimethoxybenzoate; TMB 8; 57818-92-5; TM-8; 8-(N,N-Diethylamino)octyl-3,4,5-trimethoxybenzoate; 3,4,5-Trimethoxybenzoic acid, 8-(diethylamino)octyl ester; C22H37NO5; AC1L1KGS; AC1Q67GP; Lopac-861804; Lopac0_000022; BSPBio_001503; GTPL4323; CHEMBL258764; SCHEMBL2173737; CTK5A7496; DTXSID70206532; CHEBI:107633; HMS1989L05; HMS1791L05; HMS3402L05; 53464-72-5 (hydrochloride); ZINC3875139; EI-110; AKOS030559942; MCULE-5343453436; CCG-204118; NCGC00162047-03; NCGC00162047-01; NCGC00014998-06
    Click to Show/Hide
MOA Blocker (channel blocker)
External Link
CID: 5494
TTD: D01WXA
 Compound Name 1-(biphenyl-4-yl)-3-(4-(piperidin-1-yl)butyl)urea Investigative [17]
Synonyms
CHEMBL1086332; SCHEMBL13527422
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 7900 nM
External Link
CID: 46831055
TTD: D02OYL
 Compound Name 10,11-dihydro-5H-dibenzo[b,f]azepine Investigative [18]
Synonyms
Iminodibenzyl; 494-19-9; 10,11-Dihydro-5H-dibenz[b,f]azepine; Iminobibenzyl; 2,2'-Iminodibenzyl; 2,2'-Iminobibenzyl; 5H-Dibenz[b,f]azepine, 10,11-dihydro-; RP 23669; UNII-262BX7OE3U; NSC 72110; 10,11-Dihydro-5-dibenz(b,f)azepine; 6,11-dihydro-5H-benzo[b][1]benzazepine; 10,11-Dihydrodibenz(b,f)azepine; EINECS 207-787-1; 10,11-Dihydro-5H-dibenz(b,f)azepine; BRN 0152732; CHEMBL63054; 5H-Dibenz(b,f)azepine, 10,11-dihydro-; AI3-39165; 262BX7OE3U; ZSMRRZONCYIFNB-UHFFFAOYSA-N
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 10308
TTD: D04KGK
 Compound Name 4-Benzoxazo-2-yl-1,4-diazabicyclo[3.2.2]nonane Investigative [19]
Synonyms
CHEMBL611082; SCHEMBL373021; CXJLWJAYGMWLRR-UHFFFAOYSA-N; BDBM50309862
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 13 nM
External Link
CID: 9794818
TTD: D07ZZD
 Compound Name 3alpha-(2'-Indolecarbonyloxy)-nortropane Investigative [20]
Synonyms
CHEMBL596256; BDBM50304333
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 46226582
TTD: D0C3AJ
 Compound Name FLUPENTIXOLE Investigative [18]
Synonyms
(E)-Flupenthixol; beta-Flupenthixol; trans-flupenthixol; trans-(E)-Flupentixol; trans-Flupentixol; 53772-85-3; EINECS 258-759-0; UNII-895OJP78MJ; Flupentiol; 2709-56-0; 895OJP78MJ; Flupenthixol, Beta; FLUPENTHIXOL, Alpha; 1-Piperazineethanol, 4-(3-(2-(trifluoromethyl)-9H-thioxanthen-9-ylidene)propyl)-, (E)-; (E)-4-(3-(2-(Trifluoromethyl)-9H-thioxanthen-9-ylidene)propyl)-1-piperazineethanol; 2-[4-[(3E)-3-[2-(trifluoromethyl)thioxanthen-9-ylidene]propyl]piperazin-1-yl]ethanol
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 5281878
TTD: D0M4RW
 Compound Name [3H]ramosetron Investigative [21]
MOA Antagonist
External Link
CID: 91827343
TTD: D0O5PQ
 Compound Name 3alpha-(1'-Methyl-2'-Indolecarbonyloxy)-tropane Investigative [20]
Synonyms
CHEMBL593963; BDBM50304334
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 46226590
TTD: D0S8ZJ
 Compound Name [3H]GR65630 Investigative [22]
Synonyms
[3H]-GR65630
    Click to Show/Hide
MOA Antagonist
External Link
CID: 5311136
TTD: D0T3QZ
 Compound Name [3H](S)-zacopride Investigative [23]
Synonyms
GTPL4074
    Click to Show/Hide
MOA Antagonist
External Link
CID: 53321935
TTD: D0UV6L
 Compound Name BRL-24682 Investigative [24]
Synonyms
Brl 24682; SCHEMBL7292676; CHEMBL301039; BDBM82519; PDSP2_001249; PDSP1_001265; 76272-78-1; CAS_76272-78-1; 4-amino-5-chloro-2-methoxy-N-(8-methyl-8-azabicyclo[3.2.1]octan-3-yl)benzamide; Benzamide, 4-amino-5-chloro-2-methoxy-N-(8-methyl-8-azabicyclo(3.2.1)oct-3-yl)-, endo-
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 9797313
TTD: D00PCE
 Compound Name 6-(4-Methyl-piperazin-1-yl)-phenanthridine Investigative [25]
Synonyms
CHEMBL43193; 23441-13-6; 6-(4-methylpiperazin-1-yl)phenanthridine; CTK0I7937; DTXSID50433889; ZINC13778637; BDBM50063258; 6-(4-Methylpiperazino)phenanthridine; Phenanthridine, 6-(4-methyl-1-piperazinyl)-
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 9993659
TTD: D04AXY
 Compound Name trichloroethanol Investigative [26]
Synonyms
2,2,2-TRICHLOROETHANOL; 115-20-8; Trichlorethanol; Trichloroethyl alcohol; Ethanol, 2,2,2-trichloro-; 2,2,2-Trichloro-1-ethanol; (Hydroxymethyl)trichloromethane; 2,2,2-Trichloroethyl alcohol; 2,2,2-Trichloroethan-1-ol; C2H3Cl3O; UNII-AW835AJ62N; NSC 66407; beta-trichloroethanol; CCRIS 6763; CCl3CH2OH; EINECS 204-071-0; 2,2,2-trichloro-ethanol; 2,2,2-tris-chloroethanol; BRN 1697495; AW835AJ62N; CHEBI:28094; KPWDGTGXUYRARH-UHFFFAOYSA-N; .beta.,.beta.,.beta-Trichloroethanol; 2,2,2-Trichloroethanol, 99%; 4yas
    Click to Show/Hide
MOA Modulator (allosteric modulator)
External Link
CID: 8259
TTD: D06IRE
 Compound Name (4-Quinolin-2-ylpiperazin-1-yl)acetic Acid Investigative [27]
Synonyms
CHEMBL468498; AC1LEONH; SCHEMBL13780710; A3329/0141355; BDBM50258497; AKOS009544966; 2-(4-quinolin-2-ylpiperazin-1-yl)acetic acid
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 715494
TTD: D0G3MD
 Compound Name 1-phenylbiguanide Investigative [28]
Synonyms
phenylbiguanide; Phenyl biguanide; 102-02-3; Phenyldiguanide; Phenylguanide; phenyl diguanide; N-Phenyl-N'-guanylguanidine; N-phenylimidodicarbonimidic diamide; Biguanide, phenyl-; Imidodicarbonimidic diamide, N-phenyl-; UNII-W8PKA3T2I3; BIGUANIDE, 1-PHENYL-; C8H11N5; N-Phenyl-imidocarbonimidic diamide; EINECS 202-998-5; W8PKA3T2I3; CHEMBL13791; CHEBI:75377; P 1426; Imidodicarbonimidicdiamide, N-phenyl-; 1-(diaminomethylidene)-2-phenylguanidine; SR-01000075565; N-phenylbiguanide; N'-phenylbiguanide
    Click to Show/Hide
MOA Agonist
External Link
CID: 4780
TTD: D0H4NK
 Compound Name (S)-zacopride Investigative [29]
Synonyms
CHEMBL28992; Tocris-1795; NCGC00025295-01; AC1O7H1O; SCHEMBL5373467; ZINC3961; GTPL2289; SCHEMBL16233195; PDSP2_001618; PDSP1_001634; BDBM50056419; UNII-9GN3OT4156 component FEROPKNOYKURCJ-CYBMUJFWSA-N; 4-Amino-N-(S)-1-aza-bicyclo[2.2.2]oct-3-yl-5-chloro-2-methoxy-benzamide; 4-amino-N-[(3S)-1-azabicyclo[2.2.2]octan-3-yl]-5-chloro-2-methoxybenzamide; 4-amino-N-[(8S)-1-azabicyclo[2.2.2]octan-8-yl]-5-chloro-2-methoxybenzamide
    Click to Show/Hide
MOA Antagonist
Activity Ki = 0.182 nM
External Link
CID: 6604914
TTD: D0I4BZ
 Compound Name PH-709829 Investigative [30]
Synonyms
PTGWFYYEAUFEAS-ZYHUDNBSSA-N; CHEMBL403858; PHA-709829; SCHEMBL844377; GTPL3997; BDBM50377050
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 10107234
TTD: D0IP9V
 Compound Name 2-(4-Benzyl-piperazin-1-yl)-benzothiazole Investigative [31]
Synonyms
2-(4-benzylpiperazin-1-yl)-1,3-benzothiazole; CHEMBL282234; 2-(4-benzylpiperazino)-1,3-benzothiazole; 35463-75-3; AC1LSALZ; Oprea1_030694; MLS001166194; SCHEMBL7760900; KS-00003DHQ; MolPort-002-878-239; HMS2852D05; ZINC20405012; BDBM50041381; AKOS005101332; MCULE-9582396226; 7P-339S; 1-(2-Benzothiazolyl)-4-benzylpiperazine; SMR000550026; 2-(4-benzylpiperazin-1-yl)benzo[d]thiazole; Z86230191
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 1484933
TTD: D0L1NS
 Compound Name [3H]granisetron Investigative [32]
Synonyms
[3H]-granisetron; [3H]-BRL-43694
    Click to Show/Hide
MOA Antagonist
Activity Ki = 1.45 nM
External Link
CID: 3510
TTD: D0P2HR
 Compound Name meta-chlorphenylbiguanide Investigative [33]
Synonyms
m-Chlorophenylbiguanide; mCPBG; 1-(3-Chlorophenyl)biguanide; 1-(m-Chlorophenyl)biguanide; N-(3-Chlorophenyl)imidodicarbonimidic diamide; 48144-44-1; Imidodicarbonimidic diamide, N-(3-chlorophenyl)-; UNII-910A4X901V; M-Chlorophenylbiguanidine; 3-Chloro-Phenyl biguanide; 2-(3-chlorophenyl)-1-(diaminomethylidene)guanidine; CHEMBL13790; CHEBI:32347; N-(3-chlorophenyl)-N'-(diaminomethylene)guanidine; 910A4X901V; C8H10ClN5; Imidodicarbonimidicdiamide, N-(3-chlorophenyl)-; 1-carbamimidamido-N-(3-chlorophenyl)methanimidamide; 3-chlorophenyl-biguanide; [3H]meta-chlorophenylbiguanide
    Click to Show/Hide
MOA Agonist
Activity EC50 = 3800 nM
External Link
CID: 1354
TTD: D0SA4A
 Compound Name 2-(1H-Imidazol-4-ylmethyl)-4-phenyl-thiazole Investigative [34]
Synonyms
CHEMBL289060; BDBM50014174
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 14742545
TTD: D0TJ6Z
 Compound Name CP-810123 Investigative [19]
Synonyms
UNII-E6G4550EC4; CHEMBL604798; E6G4550EC4; BSNKYWSMUAGMDO-UHFFFAOYSA-N; 439608-12-5; SCHEMBL1459339; BDBM50309861; 1,4-Diazabicyclo(3.2.2)nonane, 4-(5-methyloxazolo(4,5-b)pyridin-2-yl)-; 4-(5-methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane; 4-(5-Methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]-nonane; 4-(5-methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diaza-bicyclo[3.2.2]nonane
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 5 nM
External Link
CID: 11184481
TTD: D0X7HD
 Compound Name bilobalide Investigative [35]
Synonyms
33570-04-6; Bilobalid; (-)-Bilobalide; UNII-M81D2O8H7U; CHEBI:3103; M81D2O8H7U; Bilobalide A; 4H,5aH,9H-Furo(2,3-b)furo(3',2':2,3)cyclopenta(1,2-c)furan-2,4,7(3H,8H)-trione, 9-(1,1-dimethylethyl)-10,10a-dihydro-8,9-dihydroxy-, (5aR-(3aS*,5aalpha,8beta,8aS*,9alpha,10aalpha))-; (3aS,8R,8aS,9R,10aS)-9-tert-butyl-8,9-dihydroxydihydro-9H-furo[2,3-b]furo[3',2':2,3]cyclopenta[1,2-c]furan-2,4,7(3H,8H)-trione; tert-butyl(dihydroxy)[ ]trione; C15H18O8; Bilobalide;; Bilobalide A;; ( )-Bilobalide; AC1L2K4G; MLS000563448
    Click to Show/Hide
MOA Blocker (channel blocker)
External Link
CID: 73581
TTD: D0B0TK
 Compound Name 2-(4-Methyl-piperazin-1-yl)-quinoline Investigative [25]
Synonyms
N-methylquipazine; 2-(4-methylpiperazin-1-yl)quinoline; UNII-0YV1ZIR6S0; 0YV1ZIR6S0; CHEMBL288591; CHEBI:64164; quinoline, 2-(4-methyl-1-piperazinyl)-; Tocris-0566; Lopac-Q-107; Biomol-NT_000084; AC1L1JF3; Oprea1_654246; Lopac0_001000; SCHEMBL606721; BPBio1_001081; DTXSID8043731; CTK6I3065; HOMWNUXPSJQSSU-UHFFFAOYSA-N; MolPort-006-384-975; ZINC403653; 2-(4-Methylpiperazinyl)-quinoline; 1-(2-Quinolyl)-4-methylpiperazine; STK362919; BDBM50053631; AKOS005453926; MCULE-4786527390; CCG-205080
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 0.4571 nM
External Link
CID: 5013
TTD: D0G2BS
 Compound Name 4-((naphthalen-2-yloxy)methyl)piperidine Investigative [36]
Synonyms
4-[(2-Naphthyloxy)methyl]piperidine; CHEMBL453996; 946680-75-7; 4-[(naphthalen-2-yloxy)methyl]piperidine; CTK7D1529; ZINC14631494; BDBM50278526; AKOS000172158
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 311 nM
External Link
CID: 24691160
TTD: D01FFX
 Compound Name MESULERGINE Investigative [37]
Synonyms
Mesulerginum; Mesulergina; Mesulergine [INN]; Mesulerginum [INN-Latin]; UNII-SML95FK06I; Mesulergina [INN-Spanish]; 64795-35-3; N'-(1,6-Dimethylergolin-8alpha-yl)-N,N-dimethylsulfamide; SML95FK06I; CQ 32085; CHEMBL12314; C18H26N4O2S; CHEBI:73378; 3-(1,6-Dimethyl-8alpha-ergolinyl)-1,1-dimethylsulfamid; NCGC00163168-01; DSSTox_RID_81540; DSSTox_CID_26324; DSSTox_GSID_46324; CU-32085; N'-[(8alpha)-1,6-dimethylergolin-8-yl]-N,N-dimethylsulfuric diamide; CAS-64795-35-3; AC1L2AKM; Biomol-NT_000077; AC1Q6V4R; GTPL206
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 68848
TTD: D0K5NZ
 Compound Name 7-(piperidin-4-ylmethoxy)-2-naphthonitrile Investigative [36]
Synonyms
CHEMBL444985
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 404 nM
External Link
CID: 44592241
TTD: D06QIQ
 Compound Name QUIPAZINE Investigative [38]
Synonyms
4774-24-7; 2-(piperazin-1-yl)quinoline; 2-Piperazin-1-yl-quinoline; 2-Piperazin-1-ylquinoline; Quinoline, 2-(1-piperazinyl)-; 2-(1-Piperazinyl)quinoline; Quipazine [INN]; 1-(2-Quinolinyl)piperazine; Quipazinum [INN-Latin]; Quipazina [INN-Spanish]; UNII-4WCY05C0SJ; 1-(2-Quinolyl)piperazine; 2-(1-Piperazinyl)chinolin; BRN 0196945; 4WCY05C0SJ; CHEMBL18772; 2-quinolylpiperazine; F3306-0004; Quipazinum; Quipazina; TPC-A004; MA-1291; Spectrum_001733; Tocris-0629; piperazin-1-yl-quinoline; AC1L1JEX; AC1Q4WAV; Spectrum4_001259
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 3.7 nM
External Link
CID: 5011
TTD: D08BCF
 Compound Name 5-chloro-3,4-dihydroquinazolin-2-amine Investigative [39]
Synonyms
CHEMBL401541; 2-Amino-5-chlor-3,4-dihydrochinazolin; 109319-86-0
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 1051 nM
External Link
CID: 13702393
TTD: D0Y9TL
 Compound Name 2-methyl-5-HT Investigative [40]
Synonyms
2-methyl-5-hydroxytryptamine; 2-Me-5-HT; 2-methylserotonin
    Click to Show/Hide
MOA Agonist
Activity Ki = 1200 nM
External Link
CID: 1574
TTD: D00CRA
 Compound Name 5,6-dichloro-3,4-dihydroquinazolin-2-amine Investigative [39]
Synonyms
Anagrelide impurity 5; 2-Amino-5,6-dichloro-3,4-dihydroquinazoline; 444904-63-6; CHEMBL1548; 2-Quinazolinamine, 5,6-dichloro-1,4-dihydro-; W-202785; SCHEMBL1569300; CTK1D2410; DTXSID80432648; VBKOTIVQMCTTAQ-UHFFFAOYSA-N; ZINC29130869; BDBM50371434; AKOS030254941; 5,6-Dichloro-1,4-dihydro-2-quinazolinamine; 2-amino-5,6-dichloro-3,4dihydroquinazoline; FT-0722369
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 172 nM
External Link
CID: 9904281
TTD: D08VGJ
 Compound Name SEROTONIN Investigative [25]
Synonyms
5-HYDROXYTRYPTAMINE; 3-(2-Aminoethyl)-1H-indol-5-ol; 50-67-9; Enteramine; 5-HT; Serotonine; Thrombotonin; Thrombocytin; Antemovis; Ds substance; Hippophain; Antemoqua; Substance DS; Substanz DS; 1H-Indol-5-ol, 3-(2-aminoethyl)-; 5-Hta; Tryptamine, 5-hydroxy-; 3-(2-Aminoethyl)indol-5-ol; Enteramin; UNII-333DO1RDJY; Indol-5-ol, 3-(2-aminoethyl)-; 5-Hydroxy-3-(beta-aminoethyl)indole; 3-(beta-Aminoethyl)-5-hydroxyindole; EINECS 200-058-9; 3-(2-Amino-ethyl)-1H-indol-5-ol; BRN 0143524; 333DO1RDJY; CHEBI:28790
    Click to Show/Hide
MOA Inhibitor
Activity EC50 = 141 nM
External Link
CID: 5202
TTD: D0F6CD
DrugBank: DB08839
 Compound Name A-987306 Investigative [41]
Synonyms
SCHEMBL604437; CHEMBL519240; BDBM26226; MolPort-023-276-880; DJKJVWJQAVGLHJ-YPMHNXCESA-N; ZINC42887577; AKOS024457726; NCGC00370852-01; UNII-6BVK16R925 component DJKJVWJQAVGLHJ-YPMHNXCESA-N; (12S,17S)-6-(piperazin-1-yl)-11-oxa-3,5-diazatetracyclo[8.7.0.0^{2,7}.0^{12,17}]heptadeca-1(10),2(7),3,5-tetraen-4-amine; (-)-(7aS*,11aS*)-4-piperazin-1-yl-5,6,7a,8,9,10,11,11a-octahydro[1]benzofuro[2,3h]quinazolin-2-amine; (+/-)-(7aR*,11aR*)-5,6,7a,8,9,10,11,11a-Octahydro-4-(1-piperazinyl)-benzofuran[2,3-h]quinazolin-2-amine
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 44538833
TTD: D0F9QT
 Compound Name 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Investigative [42]
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
    Click to Show/Hide
MOA Inhibitor
Activity Ki >= 1000 nM
External Link
CID: 9948320
TTD: D0T2RY
Histone deacetylase 11 (HDAC11) 7 Compound(s) Regulating the Target Click to Show/Hide the Full List
 Compound Name PMID29671355-Compound-36 Patented [43]
MOA Inhibitor
Activity IC50 = 110 nM
External Link
TTD: D04JWR
 Compound Name PMID29671355-Compound-23 Patented [43]
MOA Inhibitor
Activity IC50 = 10500 nM
External Link
CID: 118884610
TTD: D00HXJ
 Compound Name PMID29671355-Compound-44 Patented [43]
MOA Inhibitor
Activity IC50 < 150 nM
External Link
CID: 72710871
TTD: D0N2DK
 Compound Name PMID29671355-Compound-21 Patented [43]
MOA Inhibitor
Activity IC50 = 8420 nM
External Link
CID: 86295624
TTD: D0LP1K
 Compound Name PMID29671355-Compound-62 Patented [43]
MOA Inhibitor
Activity IC50 = 100 to 500 nM
External Link
TTD: D07WAT
 Compound Name PMID29671355-Compound-43 Patented [43]
MOA Inhibitor
Activity IC50 = 12 nM
External Link
CID: 118515590
TTD: D0BP8I
 Compound Name PMID29671355-Compound-25 Patented [43]
MOA Inhibitor
Activity IC50 = 2840 nM
External Link
CID: 126569528
TTD: D0RA0D
8E43: Pain disorders 1 Compound(s) Regulating the Disease Click to Show/Hide the Full List
 Compound Name FMX104 Phase 2 [44]
External Link
TTD: D0Z8EA
References
Ref 1 FOXD3-mediated transactivation of ALKBH5 promotes neuropathic pain via m(6)A-dependent stabilization of 5-HT3A mRNA in sensory neurons. Proc Natl Acad Sci U S A. 2024 Feb 6;121(6):e2312861121. doi: 10.1073/pnas.2312861121. Epub 2024 Jan 29.
Ref 2 Palonosetron plus dexamethasone versus granisetron plus dexamethasone for prevention of nausea and vomiting during chemotherapy: a double-blind, do... Lancet Oncol. 2009 Feb;10(2):115-24.
Ref 3 Management of postoperative nausea and vomiting: focus on palonosetron. Ther Clin Risk Manag. 2009 Feb;5(1):21-34.
Ref 4 Efficacy of 5-HT3 antagonists and 5-HT4 agonists in irritable bowel syndrome: systematic review and meta-analysis. Am J Gastroenterol. 2009 Jul;104(7):1831-43; quiz 1844.
Ref 5 Emerging therapies for fibromyalgia. Expert Opin Emerg Drugs. 2008 Mar;13(1):53-62.
Ref 6 Local anesthetics have different mechanisms and sites of action at recombinant 5-HT3 receptors. Reg Anesth Pain Med. 2007 Nov-Dec;32(6):462-70.
Ref 7 2018 FDA drug approvals. Nat Rev Drug Discov. 2019 Feb;18(2):85-89. doi: 10.1038/d41573-019-00014-x.
Ref 8 Cilansetron: a new serotonergic agent for the irritable bowel syndrome with diarrhoea.Expert Opin Investig Drugs.2005 Feb;14(2):185-93.
Ref 9 Zatosetron, a potent, selective, and long-acting 5HT3 receptor antagonist: synthesis and structure-activity relationships. J Med Chem. 1992 Jan 24;35(2):310-9.
Ref 10 Effect of serotonin (5-HT)3-receptor antagonists YM060, YM114 (KAE-393), ondansetron and granisetron on 5-HT4 receptors and gastric emptying in rodents. Jpn J Pharmacol. 1995 Nov;69(3):205-14.
Ref 11 mu-Opioid/5-HT4 dual pharmacologically active agents-efforts towards an effective opioid analgesic with less GI and respiratory side effects (Part I). Bioorg Med Chem Lett. 2009 Oct 1;19(19):5679-83.
Ref 12 Emerging drugs for irritable bowel syndrome. Expert Opin Emerg Drugs. 2006 May;11(2):293-313.
Ref 13 Emerging drugs for chemotherapy-induced emesis. Expert Opin Emerg Drugs. 2006 Mar;11(1):137-51.
Ref 14 Pharmacological and regional characterization of [3H]LY278584 binding sites in human brain. J Neurochem. 1993 Feb;60(2):730-7.
Ref 15 The 5-HT3B subunit confers spontaneous channel opening and altered ligand properties of the 5-HT3 receptor. J Biol Chem. 2008 Mar 14;283(11):6826-31.
Ref 16 Characterization of interaction of 3,4,5-trimethoxybenzoic acid 8-(diethylamino)octyl ester with Torpedo californica nicotinic acetylcholine receptor and 5-hydroxytryptamine3 receptor. J Pharmacol Exp Ther. 1999 Jul;290(1):129-35.
Ref 17 Novel alpha-7 nicotinic acetylcholine receptor agonists containing a urea moiety: identification and characterization of the potent, selective, and... J Med Chem. 2010 Jun 10;53(11):4379-89.
Ref 18 Molecular properties of psychopharmacological drugs determining non-competitive inhibition of 5-HT3A receptors. Eur J Med Chem. 2009 Jun;44(6):2667-72.
Ref 19 Discovery of 4-(5-methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane (CP-810,123), a novel alpha 7 nicotinic acetylcholine receptor ag... J Med Chem. 2010 Feb 11;53(3):1222-37.
Ref 20 Synthesis of heteroaromatic tropeines and heterogeneous binding to glycine receptors. Bioorg Med Chem. 2009 Oct 1;17(19):6872-8.
Ref 21 Molecular cloning of human 5-hydroxytryptamine3 receptor: heterogeneity in distribution and function among species. Mol Pharmacol. 1995 Sep;48(3):407-16.
Ref 22 Evaluation of the pharmacological profile of ramosetron, a novel therapeutic agent for irritable bowel syndrome. J Pharmacol Sci. 2007 Jul;104(3):263-73.
Ref 23 Autoradiographic distribution of [3H]-(S)-zacopride-labelled 5-HT3 receptors in human brain. J Neurol Sci. 1996 Dec;144(1-2):119-27.
Ref 24 Synthesis and structure-affinity relationships of novel N-(1-ethyl-4-methylhexahydro-1,4-diazepin-6-yl)pyridine-3-carboxamides with potent serotoni... J Med Chem. 2003 Feb 27;46(5):702-15.
Ref 25 Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 2. Molecular basis of the intrinsic efficacy ... J Med Chem. 1999 May 6;42(9):1556-75.
Ref 26 Arginine 246 of the pretransmembrane domain 1 region alters 2,2,2-trichloroethanol action in the 5-hydroxytryptamine3A receptor. J Pharmacol Exp Ther. 2008 Mar;324(3):1011-8.
Ref 27 Specific targeting of peripheral serotonin 5-HT(3) receptors. Synthesis, biological investigation, and structure-activity relationships. J Med Chem. 2009 Jun 11;52(11):3548-62.
Ref 28 Allosteric interactions among agonists and antagonists at 5-hydroxytryptamine3 receptors. J Neurochem. 1995 Jul;65(1):104-10.
Ref 29 Pharmacological comparison of human homomeric 5-HT3A receptors versus heteromeric 5-HT3A/3B receptors. Neuropharmacology. 2001 Aug;41(2):282-4.
Ref 30 Discovery of N-[(3R,5R)-1-azabicyclo[3.2.1]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide as an agonist of the alpha7 nicotinic acetylcholine receptor:... Bioorg Med Chem Lett. 2008 Jun 15;18(12):3611-5.
Ref 31 Synthesis of 2-piperazinylbenzothiazole and 2-piperazinylbenzoxazole derivatives with 5-HT3 antagonist and 5-HT4 agonist properties. J Med Chem. 1994 Apr 29;37(9):1320-5.
Ref 32 Characterization of a human 5-hydroxytryptamine3 receptor type A (h5-HT3R-AS) subunit stably expressed in HEK 293 cells. Br J Pharmacol. 1996 Jul;118(5):1237-45.
Ref 33 Different efficacy of specific agonists at 5-HT3 receptor splice variants: the role of the extra six amino acid segment. Br J Pharmacol. 1998 Feb;123(4):661-6.
Ref 34 Aromatic thiazole derivatives: structurally novel and selective serotonin-3 receptor antagonists. J Med Chem. 1990 Jan;33(1):13-6.
Ref 35 Binding sites for bilobalide, diltiazem, ginkgolide, and picrotoxinin at the 5-HT3 receptor. Mol Pharmacol. 2011 Jul;80(1):183-90.
Ref 36 Design and optimization of selective serotonin re-uptake inhibitors with high synthetic accessibility. Part 1. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2329-32.
Ref 37 Novel and highly potent 5-HT3 receptor agonists based on a pyrroloquinoxaline structure. J Med Chem. 1997 Oct 24;40(22):3670-8.
Ref 38 Novel, potent, and selective quinoxaline-based 5-HT(3) receptor ligands. 1. Further structure-activity relationships and pharmacological characteri... J Med Chem. 2009 Nov 12;52(21):6946-50.
Ref 39 Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation. Bioorg Med Chem Lett. 2008 Jan 1;18(1):256-61.
Ref 40 Pharmacological profile of YM-31636, a novel 5-HT3 receptor agonist, in vitro. Eur J Pharmacol. 2000 Dec 8;409(2):195-201.
Ref 41 cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia. J Med Chem. 2008 Nov 27;51(22):7094-8. doi: 10.1021/jm8007618.
Ref 42 Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential. J Med Chem. 2010 Sep 9;53(17):6386-97. doi: 10.1021/jm100697g.
Ref 43 HDAC inhibitors: a 2013-2017 patent survey. Expert Opin Ther Pat. 2018 Apr 19:1-17. doi: 10.1080/13543776.2018.1459568. Online ahead of print.
Ref 44 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)