m6A-centered Crosstalk Information

Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation

m6A Modification:
Crosstalk ID	M6ACROT02218				[1], [2]
DNA methylation DNMT3B METTL14 Direct Inhibition m⁶A modification GSK3B GSK3B METTL14 Methylation : m⁶A sites
m6A Regulator	Methyltransferase-like 14 (METTL14)			WRITER	Regulator Info
m6A Target	Glycogen synthase kinase-3 beta (GSK3Beta/GSK3B)				Targert Gene
Epigenetic Regulation that have Cross-talk with This m6A Modification:
Epigenetic Regulation Type	DNA methylation (DNAMeth)
Epigenetic Regulator	DNA (cytosine-5)-methyltransferase 3B (DNMT3B)			WRITER	View Details
Regulated Target	Methyltransferase-like protein 14 (METTL14)				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	lncRNA UCA1 recruited DNA methyltransferase (DNMT1, DNMT3A, and DNMT3B) to the METTL14 promoter region to inhibit METTL14 expression in breast cancer. m6A-hypomethylation regulated FGFR4 phosphorylates Glycogen synthase kinase-3 beta (GSK3Beta/GSK3B) and activates beta-catenin/TCF4-SLC7A11/FPN1 signaling to drive anti-HER2 resistance. Knockdown of METTL14 significantly increased the expression level of FGFR4 in HER2-positive breast cancer cells. FGFR4 reduced the sensitivity of HER2-positive breast cancer to trastuzumab plus pertuzumab or tucatinib. These results pinpoint a mechanism of anti-HER2 resistance and provide a strategy for overcoming resistance via FGFR4 inhibition in recalcitrant HER2-positive breast cancer.
Responsed Disease	Breast cancer		ICD-11: 2C60		Disease Info
Responsed Drug	Tucatinib				Drug Info
Pathway Response	Wnt signaling pathway				hsa04310
Cell Process	Glutathione synthesis
In-vitro Model	MDA-MB-453	Breast adenocarcinoma	Homo sapiens		CVCL_0418
	MDA-MB-361	Breast adenocarcinoma	Homo sapiens		CVCL_0620
	SK-BR-3	Breast adenocarcinoma	Homo sapiens		CVCL_0033
	BT-474	Invasive breast carcinoma	Homo sapiens		CVCL_0179
	AU565	Breast adenocarcinoma	Homo sapiens		CVCL_1074
	MCF-7	Invasive breast carcinoma	Homo sapiens		CVCL_0031
	T-47D	Invasive breast carcinoma	Homo sapiens		CVCL_0553
	ZR-75-1	Invasive breast carcinoma	Homo sapiens		CVCL_0588
	MDA-MB-231	Breast adenocarcinoma	Homo sapiens		CVCL_0062
	BT-549	Invasive breast carcinoma	Homo sapiens		CVCL_1092
	MDA-MB-468	Breast adenocarcinoma	Homo sapiens		CVCL_0419
	SUM159PT	Breast pleomorphic carcinoma	Homo sapiens		CVCL_5423
	MCF-10A	Normal	Homo sapiens		CVCL_0598
	HEK293T	Normal	Homo sapiens		CVCL_0063
In-vivo Model	Luciferase-labeled rSKBR3 and MDA-MB-361 cells (1 × 10⁷ cells) mixed with 1:1 Matrigel (Corning, 356237) were subcutaneously injected into the fat pads of mice. After a tumor was palpable, the mice were randomized into four groups (five mice per group), and they were treated with vehicle, trastuzumab (20 mg/kg, intraperitoneal administration), roblitinib (30 mg/kg, oral administration), or a combination of both drugs.

Full List of Potential Compound(s) Related to This m6A-centered Crosstalk

DNA (cytosine-5)-methyltransferase 3B (DNMT3B)		22 Compound(s) Regulating the Target	Click to Show/Hide the Full List
Compound Name	Curcumin		Phase 3	[3]
Synonyms	458-37-7; Diferuloylmethane; Natural yellow 3; Turmeric yellow; Turmeric; Curcuma; Kacha haldi; Gelbwurz; Indian saffron; Curcumin I; Souchet; Halud; Halad; Haidr; Haldar; Merita earth; Yellow Ginger; Terra Merita; Yellow Root; Safran d'Inde; Yo-Kin; Golden seal; Curcuma oil; Orange Root; Oils, curcuma; CI Natural Yellow 3; Curcumine; Hydrastis; Indian turmeric; Yellow puccoon; Turmeric extract; Diferaloylmethane; Kurkumin [Czech]; (1E,6E)-1,7-Bis(4-hydroxy-3-methoxyphenyl)hepta-1,6-diene-3,5-dione; Tumeric yellow; Turmeric oil Click to Show/Hide
MOA	Inhibitor
External Link	CID: 969516 TTD: D07SDQ DrugBank: DB11672
Compound Name	PMID27376512-Compound-MTC-424		Patented	[4]
MOA	Inhibitor
Activity	IC50 = 1940 nM
External Link	TTD: D02WRM
Compound Name	PMID27376512-Compound-MTC-427		Patented	[4]
MOA	Inhibitor
Activity	IC50 = 295 nM
External Link	TTD: D0HA0J
Compound Name	PMID27376512-Compound-MTC-422		Patented	[4]
MOA	Inhibitor
Activity	IC50 = 1430 nM
External Link	TTD: D0QY0N
Compound Name	PMID27376512-Compound-MTC-423		Patented	[4]
MOA	Inhibitor
Activity	IC50 = 363 nM
External Link	TTD: D0W9VZ
Compound Name	NSC-622444		Investigative	[3]
Synonyms	NSC622444; CHEMBL116347; AC1Q3LXD; AC1L7GK5; SCHEMBL9755151; dichlorinated diacylmethane fragment; ZINC1616868; BDBM50048522; 5,3'-dicarboxy-4,4'-dihydrodiphenylmethane; 5,5''-methylenebis(3-chloro-2-hydroxybenzoic acid); 5,5'-Methylenebis(3-chloro-2-hydroxybenzoic acid); 3,3'-methanediylbis(5-chloro-6-hydroxybenzoic acid); 5-(3-carboxy-5-chloro-4-hydroxybenzyl)-3-chloro-2-hydroxybenzoic acid; 3',3-Dichloro-4',4-dimethoxy-5',5-bis(methoxycarbonyl)-1,1-diphenylmethane Click to Show/Hide
MOA	Inhibitor
External Link	CID: 360384 TTD: D01VNN
Compound Name	NSC-138419		Investigative	[3]
Synonyms	NSC138419; n-[4-(methylamino)benzoyl]glutamic acid; AC1Q5SG8; AC1L5YW4; SCHEMBL5925511; CHEMBL591443; CTK1H0013; 2-[(4-methylaminobenzoyl)amino]pentanedioic acid; A816490; 2-[[4-(methylamino)benzoyl]amino]pentanedioic acid; 2-[[4-(methylamino)phenyl]carbonylamino]pentanedioic acid; 2-[[[4-(methylamino)phenyl]-oxomethyl]amino]pentanedioic acid Click to Show/Hide
MOA	Inhibitor
External Link	CID: 283555 TTD: D03PWU
Compound Name	NSC-319745		Investigative	[3]
Synonyms	61629-60-5; HB 093; BRN 2168571; 4-(2-((5-Chloro-2-methoxybenzoyl)amino)ethyl)hydrocinnamic acid; 3-[4-[2-[(5-CHLORO-2-METHOXY-BENZOYL)AMINO]ETHYL]PHENYL]PROPANOIC ACID; 3-(4-(2-(5-Chlor-2-methoxy-benzamido)-aethyl)phenyl)-propionsaeure [German]; 3-[4-[2-[(5-chloro-2-methoxybenzoyl)amino]ethyl]phenyl]propanoic acid; HYDROCINNAMIC ACID, 4-(2-((5-CHLORO-2-METHOXYBENZOYL)AMINO)ETHYL)-; AC1L2AFL; CHEMBL597112; SCHEMBL11481071; CTK5B3505; DTXSID00210642; AIEFQKOARQRACO-UHFFFAOYSA-N; ZINC1572211; HB-093; NSC319745 Click to Show/Hide
MOA	Inhibitor
External Link	CID: 43709 TTD: D06RGX
Compound Name	NSC-348926		Investigative	[3]
Synonyms	NSC348926; 2-phthalimidoadipic acid; AC1L7IP1; SCHEMBL9741723; CHEMBL599367; 2-(1,3-dioxoisoindol-2-yl)hexanedioic acid Click to Show/Hide
MOA	Inhibitor
External Link	CID: 336008 TTD: D06VVV
Compound Name	NSC-401077		Investigative	[3]
Synonyms	NSC401077; MLS000757170; DNA Methyltransferase Inhibitor; CHEMBL383475; 32675-71-1; 2-(1,3-Dioxo-1,3-dihydro-isoindol-2-yl)-3-(1H-indol-3-yl)-propionic acid; 2-(1,3-dioxo-2,3-dihydro-1H-isoindol-2-yl)-3-(1H-indol-3-yl)propanoic acid; 2-(1,3-Dioxo-1,3-dihydro-2H-isoindol-2-yl)-3-(1H-indol-3-yl)propanoic acid; 2-(1,3-Dioxo-1,3-dihydro-2H-isoindol-2-yl)-3-(1H-indol-3-yl)propionic acid; SMR000413613; AC1Q71QA; Oprea1_475901; Oprea1_410805; MLS000777218; MLS006011919; SCHEMBL562060 Click to Show/Hide
MOA	Inhibitor
External Link	CID: 344265 TTD: D07VWC
Compound Name	S-tubercidinylhomocysteine		Investigative	[5]
Synonyms	CHEMBL552309; 57344-98-6; AC1L3YAS; AC1Q5QMO; (S)-7-(5-S-(3-amino-3-carboxypropyl)-5-thio-beta-D-ribofuranosyl)-7H-pyrrolo(2,3-d)pyrimidin-4-amine; (2s)-2-amino-4-({[(2s,3s,4r,5r)-5-(4-amino-7h-pyrrolo[2,3-d]pyrimidin-7-yl)-3,4-dihydroxytetrahydrofuran-2-yl]methyl}sulfanyl)butanoic acid(non-preferred name); BDBM50294482; (2S)-2-amino-4-[[(2S,3S,4R,5R)-5-(4-aminopyrrolo[2,3-d]pyrimidin-7-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]butanoic acid Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 300 nM
External Link	CID: 124349 TTD: D08TGQ
Compound Name	NSC-106084		Investigative	[3]
Synonyms	CHEMBL597113; NSC106084; AC1L6H8Q; CTK7J5419; ZINC1868549; BDBM50308983; {4-[5-bromo-2-(carboxymethoxy)benzoyl]phenoxy}acetic acid; 2-(4-bromo-2-(4-(carboxymethoxy)benzoyl)phenoxy)acetic acid; 2-[4-[5-bromo-2-(carboxymethyloxy)benzoyl]phenoxy]acetic acid Click to Show/Hide
MOA	Inhibitor
External Link	CID: 266989 TTD: D0A2ZH
Compound Name	NSC-154957		Investigative	[3]
Synonyms	NSC154957; AC1L6EF2; CHEMBL586418; 3-benzhydrylsulfanyl-2-formamidopropanoic acid Click to Show/Hide
MOA	Inhibitor
External Link	CID: 290753 TTD: D0C4NA
Compound Name	NSC-54162		Investigative	[3]
Synonyms	NSC54162; AC1Q5WTA; AC1L6CM2; CHEMBL611994; 2,2'-{[(2-hydroxyphenyl)methanediyl]disulfanediyl}diacetic acid; ZINC1685025; Acetic acid, (salicylidenedithio)di-; 4265-51-4; Acetic acid, [(o-hydroxybenzylidene)dithio]di-; Acetic acid,2'-[[(2-hydroxyphenyl)methylene]bis(thio)]bis-; 2-[carboxymethylsulfanyl-(2-hydroxyphenyl)methyl]sulfanylacetic acid Click to Show/Hide
MOA	Inhibitor
External Link	CID: 243918 TTD: D0FN7C
Compound Name	NSC-57893		Investigative	[3]
Synonyms	MLS002667915; 7399-94-2; 4-[(1h-benzimidazol-2-ylmethyl)(formyl)amino]benzoic acid; NSC57893; AC1L6GFK; AC1Q5TWY; NCIOpen2_002368; CHEMBL599366; 4-[1H-benzimidazol-2-ylmethyl(formyl)amino]benzoic acid; CTK5D9099; DTXSID30288854; HMS3089M13; ZINC1688755; AKOS030547711 Click to Show/Hide
MOA	Inhibitor
External Link	CID: 245689 TTD: D0G9NS
Compound Name	NSC-56071		Investigative	[3]
Synonyms	32230-52-7; NSC56071; AC1L6EJV; AC1Q7ES0; NCIOpen2_007380; CHEMBL596910; CTK4G8394; DTXSID80288485; ZINC1686711; 2,2'-[piperazine-1,4-diylbis(carbonothioylsulfanediyl)]diacetic acid; AKOS030574801; Acetic acid,2,2'-[1,4-piperazinediylbis(carbonothioylthio)]bis- (9CI); 2-[4-(carboxymethylsulfanylcarbothioyl)piperazine-1-carbothioyl]sulfanylacetic acid Click to Show/Hide
MOA	Inhibitor
External Link	CID: 244824 TTD: D0H1YK
Compound Name	NSC-137546		Investigative	[3]
Synonyms	NSC137546; CHEMBL591202; AC1L5Y49; AKOS008984447; 2-[(2,6-dichlorobenzoyl)amino]pentanedioic acid Click to Show/Hide
MOA	Inhibitor
External Link	CID: 283188 TTD: D0I5JP
Compound Name	NSC-623548		Investigative	[3]
Synonyms	2581-36-4; NSC 408488; o-Cresotic acid, 5,5'-methylenedi-; 2,3-CRESOTIC ACID, 5,5'-METHYLENEDI-; UNII-S3D8KC88KC; 5,5'-Methylenedi-2,3-cresotic acid; NSC 623548; BRN 3433298; S3D8KC88KC; CHEMBL113835; 5,5'-Methylenedi-o-cresotic acid; NSC623548; NSC408488; 5,5'-Methylenebis(2-hydroxy-3-methylbenzoic acid); 2, 5,5'-methylenedi-; AC1L29YK; Oprea1_231968; 2-10-00-00398 (Beilstein Handbook Reference); SCHEMBL9755153; CTK4F6504; DTXSID90180466; o-Cresotic acid,5'-methylenedi-; MolPort-000-698-522; ZINC4028795; STL511095 Click to Show/Hide
MOA	Inhibitor
External Link	CID: 17413 TTD: D0LS2U
Compound Name	NSC-345763		Investigative	[3]
Synonyms	7-(8-hydroxyquinolin-5-yl)-4,7-dioxoheptanoic acid; NSC345763; AC1L7HSU; CHEMBL597114 Click to Show/Hide
MOA	Inhibitor
External Link	CID: 335596 TTD: D0MP7N
Compound Name	NSC-158324		Investigative	[3]
Synonyms	Acediasulfone; UNII-30YP2YHH8W; 30YP2YHH8W; CHEMBL48396; N-[4-[(4-AMINOPHENYL)SULPHONYL]PHENYL]GLYCINE; 2-[4-(4-aminophenyl)sulfonylanilino]acetic acid; Acediasulfonum; N-(4-((4-Aminophenyl)sulphonyl)phenyl)glycine; EINECS 201-243-7; AC1L25EF; ZINC862; SCHEMBL143660; CTK5E7379; DTXSID00229991; CHEBI:135300; BDBM50099670; AKOS027327086; DB08926; Glycine,N-[4-[(4-aminophenyl)sulfonyl]phenyl]-; {4-[(4-aminophenyl)sulfonyl]anilino}acetic acid; 2-(4-(4-aminophenylsulfonyl)phenylamino)acetic acid Click to Show/Hide
MOA	Inhibitor
External Link	CID: 24193827 TTD: D0W5SZ
Compound Name	(L-)-S-adenosyl-L-homocysteine		Investigative	[6]
Synonyms	S-Adenosyl-L-homocysteine; S-adenosylhomocysteine; 979-92-0; AdoHcy; S-(5'-adenosyl)-L-homocysteine; adenosylhomocysteine; Formycinylhomocysteine; Adenosyl-L-homocysteine; S-(5'-deoxyadenosin-5'-yl)-L-homocysteine; 2-S-adenosyl-L-homocysteine; 5'-Deoxy-S-adenosyl-L-homocysteine; S-adenosyl-homocysteine; S-Adenosyl Homocysteine; L-S-Adenosylhomocysteine; L-Homocysteine, S-(5'-deoxyadenosin-5'-yl)-; adenosylhomo-cys; adenosyl-homo-cys; UNII-8K31Q2S66S; (S)-5'-(S)-(3-Amino-3-carboxypropyl)-5'-thioadenosine; BRN 5166233; SAH Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 200 nM
External Link	CID: 439155 TTD: D09CLP DrugBank: DB01752
Compound Name	NSC-622445		Investigative	[3]
Synonyms	5,5'-Methylenedisalicylic acid; 122-25-8; 5,5'-Methylenebis(2-hydroxybenzoic acid); Methylenebis(salicylic acid); 5,5-Methylenebis(salicylic acid); UNII-2KF4FVV76N; 5,5-Methylenedisalicylic acid; 5-(3-Carboxy-4-hydroxybenzyl)salicylic acid; 4,4'-Dihydroxy-3,3'-dicarboxydiphenylmethane; 3,3'-Dicarboxy-4,4'-dihydroxydiphenylmethane; NSC 14778; 2KF4FVV76N; 4,4'-Dihydroxydiphenylmethane-3,3'-dicarboxylic acid; 3,3'-Methylenebis(6-hydroxybenzoic acid); CHEMBL115145; Benzoic acid, 3,3'-methylenebis[6-hydroxy- Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 17000 nM
External Link	CID: 67145 TTD: D0J5VK
Glycogen synthase kinase-3 beta (GSK3Beta/GSK3B)		88 Compound(s) Regulating the Target	Click to Show/Hide the Full List
Compound Name	AMO-02		Phase 2/3	[7]
MOA	Inhibitor
External Link	TTD: D0BS5E
Compound Name	Tideglusib		Phase 2	[8]
Synonyms	NP-031112; NP-12; NP031112; Tideglusib(NP-031112) Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 78 nM
External Link	CID: 11313622 TTD: D0UT7X DrugBank: DB12129
Compound Name	9-ING-41		Phase 2	[9]
Synonyms	1034895-42-5; ND1SOF0DLU; UNII-ND1SOF0DLU; CHEMBL483465; 3-(5-fluoro-1-benzofuran-3-yl)-4-(5-methyl-[1,3]dioxolo[4,5-f]indol-7-yl)pyrrole-2,5-dione; 3-(5-fluorobenzofuran-3-yl)-4-(5-methyl-5H-[1,3]dioxolo[4,5-f]indol-7-yl)-1H-pyrrole-2,5-dione; elraglusib; SCHEMBL3152351; GTPL11412; EX-A4074; BDBM50267716; s9602; SB19735; compound 26 [PMID: 19338355]; HY-113914; CS-0063319; 1H-Pyrrole-2,5-dione, 3-(5-fluoro-3-benzofuranyl)-4-(5-methyl-5H-1,3-dioxolo(4,5-F)indol-7-yl)-; 3-(5-Fluoro-benzofuran-3-yl)-4-(5-methyl-5H-(1,3)dioxolo(4,5-F)indol-7-yl)-pyrrole-2,5-dione; 3-(5-Fluorobenzofuran-3-yl)-4-(5-methyl-5H-[1,3]dioxolo[4,5-f]indol-7-yl)pyrrole-2,5-dione; 4-(5-methyl-5H-[1,3]dioxolo[4,5-f]-indol-7-yl)-3-(5-fluoro-1-benzofuran-3-yl)-1 h-pyrrole-2,5-dione Click to Show/Hide
MOA	Inhibitor
External Link	CID: 44582816 TTD: D4USX5
Compound Name	LY2090314		Phase 2	[10]
Synonyms	603288-22-8; LY-2090314; UNII-822M3GYM67; Kinome_3681; LY 2090314; CHEMBL362558; 822M3GYM67; 3-(9-Fluoro-2-(piperidine-1-carbonyl)-1,2,3,4-tetrahydro-[1,4]diazepino[6,7,1-hi]indol-7-yl)-4-(imidazo[1,2-a]pyridin-3-yl)-1H-pyrrole-2,5-dione; SCHEMBL633455; GTPL7958; DTXSID90209085; MolPort-035-944-332; EX-A2214; ZINC3817327; BCP07855; s7063; BDBM50150699; AKOS032950045; AKOS026750195; CS-1633; DB11913; SB16558; NCGC00378942-05; NCGC00378942-02; BC600682; QC-11735; HY-16294; KB-78238; FT-0698670; LY2090314, &gt Click to Show/Hide
MOA	Modulator
Activity	IC50 = 0.9 nM
External Link	CID: 10029385 TTD: D0Z1DH DrugBank: DB11913
Compound Name	Lithium		Phase 2	[11]
Synonyms	7439-93-2; Li; litio; UNII-9FN79X2M3F; 9FN79X2M3F; CHEBI:30145; MFCD00134051; Litium; Lithium, metallic; Lithium, elemental; Lithium, 99+%, granular, dry; Lithium compounds; 3Li; HSDB 647; EINECS 231-102-5; UN1415; monolithium; Lithium standard solution, for AAS, 1 mg-ml Li in 2% HCl; Hydrure de lithium [French]; Lithium ribbon; Lithium rod; HSDB 549; Lithium granules; EINECS 231-484-3; UN1414; UN2805; Normothymin-E (TN); Epitope ID:114079; EC 231-102-5; Lithium, 99%, low sodium; Lithium, 99%, high sodium; CHEMBL2146126; DTXSID5036761; HSDB 6900; 7321AH; AKOS015833388; AKOS015902481; HSD6900000; Lithium wire, 3.2mm (0.125in) dia; Lithium [UN1415] [Dangerous when wet]; Lithium granules, 1-6mm (0.04-0.2in); Lithium, granular, 99% trace metals basis; FT-0627905; C15473; D08133; EC 231-484-3; Lithium hydride [UN1414] [Dangerous when wet]; Lithium, shot, 99%, 4-16 mesh, in mineral oil; Lithium, wire, diam. 3.2 mm, in mineral oil, >=98%; Lithium, ~25 wt % dispersion in mineral oil, high sodium; Lithium, AAS standard solution, Specpure?, Li 1000?g/ml; Lithium, ingot, diam. 5.7 cm, 99.9% trace metals basis; Lithium, rod, diam. 12.7 mm, 99.9% trace metals basis; Lithium foil, 0.75mm (0.03in) thick x 19mm (0.75in) wide; Lithium hydride, fused solid [UN2805] [Dangerous when wet]; Lithium ingot, 5.7cm (2.2in) dia x 8.6cm (3.4in) long; Lithium, Oil based standard solution, Specpure, Li 5000g/g; Lithium, plasma standard solution, Specpure?, Li 10,000?g/ml; Lithium, plasma standard solution, Specpure?, Li 1000?g/ml; Lithium, rod, 12.7 mm diameter, length 165 mm, purity 99%; Lithium, rod, 12.7 mm diameter, length 200 mm, purity 99%; Lithium, foil, 25x100mm, thickness 0.6mm, as rolled, 99.9%; Lithium, Oil based standard solution, Specpure(R), Li 1000?g/g; Lithium, foil, thickness 0.6 mm, size 25 x 300 mm, purity 99.9%; Lithium, Ion chromatography standard solution, Specpure, Li+ 1000?g/ml; Lithium, wire (in mineral oil), diam. 3.2 mm, 99.9% trace metals basis; Lithium, foil, not light tested, 38x200mm, thickness 0.20mm, as rolled, 99.9%; Lithium, foil, not light tested, 38x500mm, thickness 0.20mm, as rolled, 99.9%; Lithium, foil, not light tested, 45x200mm, thickness 0.12mm, as rolled, 99.9%; Lithium, granular, 4-10 mesh particle size, high sodium, 99% (metals basis); Lithium, ribbon, thickness x W 0.38 mm x 23 mm, 99.9% trace metals basis; Lithium, ribbon, thickness x W 0.75 mm x 19 mm, 99.9% trace metals basis; Lithium, ribbon, thickness x W 0.75 mm x 45 mm, 99.9% trace metals basis; Lithium, ribbon, thickness x W 1.5 mm x 100 mm, 99.9% trace metals basis Click to Show/Hide
MOA	Inhibitor
External Link	CID: 3028194 TTD: D5MF8Y
Compound Name	Neu-120		Phase 1/2	[12]
Synonyms	Neu-108; NMDA receptor modulators (Parkinson's Disease), Neurim Click to Show/Hide
MOA	Modulator
External Link	TTD: D0D1UQ
Compound Name	TDZD-8		Patented	[13]
Synonyms	327036-89-5; 4-Benzyl-2-methyl-1,2,4-thiadiazolidine-3,5-dione; GSK-3beta Inhibitor I; TDZD 8; 1,2,4-Thiadiazolidine-3,5-dione, 2-methyl-4-(phenylmethyl)-; MFCD04973552; NP 01139; AK-48153; 4-Benzyl-2-methyl-[1,2,4]thiadiazolidine-3,5-dione; 1,2,4-Thiadiazolidine-3,5-dione,2-methyl-4-(phenylmethyl)-; GSK-3 Inhibitor I; SCHEMBL139834; GTPL5977; CHEMBL284861; BDBM7781; CTK4G9152; ZINC27361; AOB6176; EX-A109; DTXSID30399590; JDSJDASOXWCHPN-UHFFFAOYSA-N; MolPort-003-844-896; HMS3229G12; A Inhibitor I, TDZD-8 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 690 nM
External Link	CID: 4124851 TTD: D06KNK
Compound Name	AR-A014418		Patented	[14]
Synonyms	487021-52-3; GSK-3beta Inhibitor VIII; 1-(4-methoxybenzyl)-3-(5-nitrothiazol-2-yl)urea; 1-[(4-methoxyphenyl)methyl]-3-(5-nitro-1,3-thiazol-2-yl)urea; A Inhibitor VIII; N-(4-METHOXYBENZYL)-N'-(5-NITRO-1,3-THIAZOL-2-YL)UREA; UNII-87KSH90Q6D; AR-AO 14418; SN 4521; AR-A 014418; CHEMBL259850; 87KSH90Q6D; N-[(4-Methoxyphenyl)methyl]-N'-(5-nitro-2-thiazolyl)urea; AK175829; C12H12N4O4S; N-(4-Methoxybenzyl)-N& -(5-nitro-1,3-thiazol-2-yl)urea; AR 014418; GSK 3be Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 2.07 nM
External Link	CID: 448014 TTD: D0A3MV DrugBank: DB01950
Compound Name	PMID26161698-Compound-18		Patented	[15]
MOA	Inhibitor
Activity	IC50 = high nM
External Link	CID: 136273305 TTD: D0F7DS
Compound Name	CHIR-99021		Patented	[16]
Synonyms	CHIR99021; CHIR 99021; CT-99021; CT99021 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 30 nM
External Link	CID: 9956119 TTD: D0YK9D
Compound Name	KENPAULLONE		Patented	[17]
Synonyms	142273-20-9; 9-Bromopaullone; NSC 664704; 9-Bromo-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one; NSC-664704; NSC664704; MLS002702152; CHEMBL296586; 9-Bromo-7,12-dihydroindolo(3,2-d)(1)benzazepin-6(5H)-one; Indolo[3,2-d][1]benzazepin-6(5H)-one,9-bromo-7,12-dihydro-; QQUXFYAWXPMDOE-UHFFFAOYSA-N; 9-Bromo-7,12-dihydro-indolo[3,2-d][1]benzazepin-6(5H)-one; 9-bromo-7,12-dihydro-5H-indolo[3,2-d][1]benzazepin-6-one; 9-Bromo-7,12-dihydro-indolo-[3,2-d]-[1]benzazepin-6(5H)-one Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 23 nM
External Link	CID: 3820 TTD: D00PWQ
Compound Name	AZD-1080		Discontinued in Phase 1	[18]
MOA	Modulator
Activity	IC50 = 31 nM
External Link	CID: 135564570 TTD: D0MC0O
Compound Name	SAN-61		Terminated	[19]
Synonyms	SAN-AL-61; Oral beta amyloid inhibitor (Alzheimer's disease), Sanomune Click to Show/Hide
MOA	Inhibitor
External Link	TTD: D07YNH
Compound Name	RO-320432		Terminated	[20]
Synonyms	ro 32-0432; Ro-32-0432; CHEMBL26501; (S)-3-(8-(Dimethylaminomethyl)-6,7,8,9-tetrahydropyrido(1,2-a)indol-10-yl)-4-(1-methyl-3-indolyl)-1H-pyrrole-2,5-dione hydrochloride; (S)-3-(8-((Dimethylamino)methyl)-6,7,8,9-tetrahydropyrido(1,2-a)indol-10-yl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrol-2,5-dione; (S)-3-(8-((Dimethylamino)methyl)-6,7,8,9-tetrahydropyrido(1,2-a)indol-10-yl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione; 151342-35-7; 1H-Pyrrole-2,5-dione, 3-(8-((dimethylamino)methyl)-6,7,8,9-tetrahydropyrido(1,2-a)in Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 20 nM
External Link	CID: 127757 TTD: D0R5ZR
Compound Name	8-O-(4-chlorobenzenesulfonyl)manzamine F		Investigative	[21]
Synonyms	CHEMBL400717 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 7200 nM
External Link	CID: 23643731 TTD: D00AAN
Compound Name	N,8-diphenyl-9H-purin-6-amine		Investigative	[22]
Synonyms	CHEMBL1210175; N,8-Diphenyl-9H-purine-6-amine; BDBM50322830; SR-01000661492 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 16 nM
External Link	CID: 46894037 TTD: D00HUP
Compound Name	N-(8-(3-cyanophenyl)-9H-purin-6-yl)pentanamide		Investigative	[22]
Synonyms	CHEMBL1210476 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 1220 nM
External Link	CID: 49863103 TTD: D00XUF
Compound Name	N-(6-(3-hydroxyphenyl)-1H-indazol-3-yl)butyramide		Investigative	[23]
Synonyms	CHEMBL1086639; SCHEMBL6485118; UKQRPDHIQLHFNS-UHFFFAOYSA-N; BDBM50313706 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 94 nM
External Link	CID: 22319573 TTD: D01IPF
Compound Name	GSK-3beta inhibitor II		Investigative	[24]
Synonyms	GSK-3b inhibitor II Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 390 nM
External Link	CID: 6539732 TTD: D01MEP
Compound Name	3-phenyl-4-(phenylamino)-1H-pyrrole-2,5-dione		Investigative	[25]
Synonyms	SKF-62604; 4-arylmaleimide deriv. 6a; phenyl anilino-maleimide; AC1O6ZNQ; BDBM8218; SCHEMBL5682682; CHEMBL346551; HMS3303J01; HMS3305A03; 2-(Phenylamino)-3-phenylmaleimide; 3-anilino-4-phenylpyrrole-2,5-dione; NCGC00241898-01; AB01092118-01 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 520 nM
External Link	CID: 6539451 TTD: D01OJG
Compound Name	8-O-(4-bromobenzenesulfonyl)manzamine F		Investigative	[21]
Synonyms	CHEMBL414128 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 23000 nM
External Link	CID: 23643732 TTD: D01RKI
Compound Name	I-5		Investigative	[26]
Synonyms	SB-409513; 2-CHLORO-5-[4-(3-CHLORO-PHENYL)-2,5-DIOXO-2,5-DIHYDRO-1H-PYRROL-3-YLAMINO]-BENZOIC ACID; 2-chloro-5-{[4-(3-chlorophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino}benzoic acid; AC1L9LHU; 4-arylmaleimide deriv. 6-z; CHEMBL156987; BDBM8269; SCHEMBL10059345; HMS3303B04; HMS3305M22; DB01793; NCGC00241937-01; AB01092116-01; 2-(3-Carboxy-4-chlorophenylamino)-3-(3-chlorophenyl)maleimide; 2-chloro-5-[[4-(3-chlorophenyl)-2,5-dioxopyrrol-3-yl]amino]benzoic acid Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 76 nM
External Link	CID: 448008 TTD: D02OPH DrugBank: DB01793
Compound Name	GSK-3beta inhibitor XI		Investigative	[27]
Synonyms	GSK-3b inhibitor XI Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 5 nM
External Link	CID: 10020713 TTD: D02ZIY
Compound Name	Manzamine E		Investigative	[28]
MOA	Inhibitor
External Link	CID: 6474830 TTD: D03GQF
Compound Name	N-(6-(4-fluorophenyl)-1H-indazol-3-yl)butyramide		Investigative	[23]
Synonyms	CHEMBL1084681; SCHEMBL4488738; ORRUGYIZWSJRJU-UHFFFAOYSA-N; BDBM50313680 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 5008 nM
External Link	CID: 22319694 TTD: D03OED
Compound Name	N-(6-(2-chlorophenyl)-1H-indazol-3-yl)butyramide		Investigative	[23]
Synonyms	CHEMBL1086175; N-[6-(2-chlorophenyl)-1H-indazol-3-yl]butanamide; SCHEMBL6485112; WPJGFQOEGTUKTE-UHFFFAOYSA-N Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 1353 nM
External Link	CID: 10380885 TTD: D04ACJ
Compound Name	N-(6-bromo-1H-indazol-3-yl)butyramide		Investigative	[23]
Synonyms	CHEMBL1086780; N-[6-bromo-1H-indazol-3-yl]butanamide; 599191-53-4; butanamide,n-(6-bromo-1h-indazol-3-yl)-; SCHEMBL6490286; QQVNXRROZHWJNS-UHFFFAOYSA-N; ZINC38816494; BDBM50313708 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 198 nM
External Link	CID: 10423871 TTD: D04VBD
Compound Name	Manzamine Y		Investigative	[28]
Synonyms	CHEBI:66668; (4aR,7S,7aR,13Z,14aR,15aR,18Z)-5-(6-hydroxy-9H-beta-carbolin-1-yl)-4,4a,9,10,11,12,14a,15-octahydro-3H-7,2-oct[3]enoazocino[1',2':1,5]pyrrolo[2,3-i]isoquinolin-7(1H,7aH)-ol Click to Show/Hide
MOA	Inhibitor
External Link	CID: 10393120 TTD: D05GIC
Compound Name	IM-12		Investigative	[29]
Synonyms	1129669-05-1; CHEMBL1254896; 3-(4-Fluorophenylethylamino)-1-methyl-4-(2-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione; 3-(4-fluorophenethylamino)-1-methyl-4-(2-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione; 3-[2-(4-fluorophenyl)ethylamino]-1-methyl-4-(2-methyl-1H-indol-3-yl)pyrrole-2,5-dione; IM 12; GTPL8017; SCHEMBL17378682; DTXSID20649091; AOB4090; MolPort-035-789-694; CHEBI:125616; HMS3653F15; BCP10769; EX-A2071; ZINC59086693; s7566; BDBM50326901; 2472AH; AKOS026750397; SB19269; CS-3399; CCG-208085; NCGC00386352-05; BC600587 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 53 nM
External Link	CID: 25209788 TTD: D05SXF
Compound Name	N-(6-phenethyl-1H-indazol-3-yl)butyramide		Investigative	[23]
Synonyms	CHEMBL1084684; SCHEMBL6489338 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 8525 nM
External Link	CID: 22319484 TTD: D06YMZ
Compound Name	N-(6-benzyl-1H-indazol-3-yl)butyramide		Investigative	[23]
Synonyms	CHEMBL1077260; SCHEMBL6490520 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 4140 nM
External Link	CID: 10266409 TTD: D07IVD
Compound Name	(2'Z,3'E)-7-Azaindirubin-3'-oxime		Investigative	[30]
MOA	Inhibitor
External Link	CID: 44614397 TTD: D07MZD
Compound Name	N-(6-phenyl-1H-indazol-3-yl)butyramide		Investigative	[31]
Synonyms	CHEMBL1086174; SCHEMBL4493121 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 390 nM
External Link	CID: 10085013 TTD: D07PTD
Compound Name	Neo-kauluamine		Investigative	[28]
MOA	Inhibitor
External Link	CID: 44448144 TTD: D09AEV
Compound Name	(E)-N-(6-(prop-1-enyl)-1H-indazol-3-yl)butyramide		Investigative	[23]
Synonyms	CHEMBL1086176 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 2459 nM
External Link	CID: 22319483 TTD: D09BQY
Compound Name	8-OH-MANZAMINE A		Investigative	[28]
Synonyms	8-Hydroxymanzamine A; 154466-37-2; (4aR,7S,7aR,13Z,14aR,15aR,18Z)-5-(8-hydroxy-9H-beta-carbolin-1-yl)-4,4a,9,10,11,12,14a,15-octahydro-3H-7,2-oct[3]enoazocino[1',2':1,5]pyrrolo[2,3-i]isoquinolin-7(1H,7aH)-ol; (+)8-Hydroxymanzamine A; CHEBI:66669 Click to Show/Hide
MOA	Inhibitor
External Link	CID: 5270765 TTD: D09ITI
Compound Name	6-deoxymanzamine X		Investigative	[21]
MOA	Inhibitor
External Link	CID: 44445400 TTD: D09RYG
Compound Name	N-(6-(4-aminophenyl)-1H-indazol-3-yl)butyramide		Investigative	[23]
Synonyms	CHEMBL1086638; N-[6-(4-aminophenyl)-1H-indazol-3-yl]butanamide; SCHEMBL6478145; DCCRABAZYMVLJU-UHFFFAOYSA-N Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 76 nM
External Link	CID: 10085818 TTD: D0A9MY
Compound Name	N-(6-(trifluoromethyl)-1H-indazol-3-yl)butyramide		Investigative	[23]
Synonyms	N-[6-(trifluoromethyl)-1H-indazol-3-yl]butanamide; CHEMBL1086640; 599191-49-8; SCHEMBL1462440; RVYSDAGRNRYYML-UHFFFAOYSA-N Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 195 nM
External Link	CID: 10265187 TTD: D0C9OT
Compound Name	PAULLONE		Investigative	[20]
Synonyms	142273-18-5; 7,12-Dihydroindolo[3,2-d][1]benzazepin-6(5H)-one; CHEMBL430574; NSC641166; NSC 641166; 7,12-dihydro-5H-indolo[3,2-d][1]benzazepin-6-one; 8,18-diazatetracyclo[9.7.0.0; {12,17}]octadeca-1(11),2,4,6,12(17),13,15-heptaen-9-one; AC1Q6O0K; AC1L7YZ4; BDBM7287; SCHEMBL3178594; CTK4C3026; DTXSID30327277; CHEBI:138487; ZINC1626613; AKOS024113922; NSC-641166; NCI60_013826; RT-014947; FT-0673529 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 4 nM
External Link	CID: 369401 TTD: D0D5ZL
Compound Name	12,13-DEHYDRO-8-O-ACETYLMANZAMINE A		Investigative	[21]
Synonyms	CHEMBL252520 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 4800 nM
External Link	CID: 23643836 TTD: D0E2XM
Compound Name	N-(6-(pyridin-4-yl)-1H-indazol-3-yl)butyramide		Investigative	[23]
Synonyms	CHEMBL1086782; SCHEMBL1460286; BBNQSWZLWJBJIN-UHFFFAOYSA-N; BDBM50313652 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 661 nM
External Link	CID: 10085059 TTD: D0E6GC
Compound Name	4-(5-bromo-1H-indol-3-yl)pyrimidin-2-amine		Investigative	[14]
Synonyms	Meridianin C; 213473-00-8; 2-Pyrimidinamine, 4-(5-bromo-1H-indol-3-yl)-; CHEMBL44541; SCHEMBL1612228; CTK0J7680; BDBM10840; DTXSID50434275; PKQJCYXKRNGUKQ-UHFFFAOYSA-N; AKOS027469387; AS-49872 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 2000 nM
External Link	CID: 10017019 TTD: D0F5EI
Compound Name	9-N-METHYL-8-METHOXY-MANZAMINE A		Investigative	[21]
MOA	Inhibitor
External Link	CID: 23643639 TTD: D0I3US
Compound Name	N-(6-(furan-3-yl)-1H-indazol-3-yl)butyramide		Investigative	[23]
Synonyms	CHEMBL1086781; SCHEMBL1461525; ZGQZPFJWHPTRAH-UHFFFAOYSA-N; BDBM50313709 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 260 nM
External Link	CID: 9993220 TTD: D0IL0G
Compound Name	N-(6-chloro-5-p-tolyl-1H-indazol-3-yl)butyramide		Investigative	[23]
Synonyms	CHEMBL1097694; SCHEMBL1461361; REESNWQQNIKZJK-UHFFFAOYSA-N; BDBM50313666 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 14000 nM
External Link	CID: 22319511 TTD: D0M3SC
Compound Name	12,13-DEHYDROMANZAMINE A		Investigative	[21]
Synonyms	CHEMBL268202 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 5400 nM
External Link	CID: 23643835 TTD: D0NL1F
Compound Name	CT-98024		Investigative	[20]
Synonyms	556813-39-9; N2-(2-((4-(2,4-Dichlorophenyl)-5-(1H-imidazol-2-yl)pyrimidin-2-yl)amino)ethyl)-5-nitropyridine-2,6-diamine; CHEMBL1080901; CHIR-98024; N6-[2-[[4-(2,4-Dichlorophenyl)-5-(1H-imidazol-2-yl)-2-pyrimidinyl]amino]ethyl]-3-nitro-2,6-pyridinediamine; NDFXSHIIGXVOKT-UHFFFAOYSA-N; SCHEMBL4394521; CTK8E8250; DTXSID90433308; MolPort-006-393-166; BCP13710; BDBM50313013; ABP000489; ZINC44136098; AKOS016011284; KB-76042; CHIR98014(CT98014)/; AK120785; RT-011992; AX8246201; AJ-109287; FT-0664506; Z-3284 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 0.56 nM
External Link	CID: 9957049 TTD: D0Q3KS
Compound Name	N-(6-(pyridin-3-yl)-1H-indazol-3-yl)butyramide		Investigative	[31]
Synonyms	CHEMBL1085918; SCHEMBL6489919; CZTAWAQITKVBNQ-UHFFFAOYSA-N; BDBM50313686 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 5900 nM
External Link	CID: 10016510 TTD: D0R5EF
Compound Name	N-(6-chloro-1H-indazol-3-yl)butyramide		Investigative	[23]
Synonyms	CHEMBL1082235; N-(6-chloro-1H-indazol-3-yl)butanamide; SCHEMBL4497072; VHQZZDZWVQELLJ-UHFFFAOYSA-N Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 354 nM
External Link	CID: 10421683 TTD: D0R6TL
Compound Name	9-N-ETHYL-8-ETHOXY-MANZAMINE A		Investigative	[21]
Synonyms	CHEMBL403562 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 10400 nM
External Link	CID: 23643537 TTD: D0R7QL
Compound Name	N-(6-(4-hydroxyphenyl)-1H-indazol-3-yl)butyramide		Investigative	[23]
MOA	Inhibitor
Activity	IC50 = 44 nM
External Link	CID: 135458003 TTD: D0S3RP
Compound Name	N-(6-(thiophen-3-yl)-1H-indazol-3-yl)butyramide		Investigative	[23]
Synonyms	CHEMBL1083208; SCHEMBL1462380; KEXXQGBZRBKVRC-UHFFFAOYSA-N; BDBM50313653 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 935 nM
External Link	CID: 22319580 TTD: D0T1CE
Compound Name	CP-70949		Investigative	[32]
Synonyms	PFI-367; PFI-856; GSK-3-beta inhibitor, Pfizer; Glycogen synthase kinase-3-beta inhibitor, Pfizer Click to Show/Hide
MOA	Inhibitor
External Link	TTD: D0T8CQ
Compound Name	3-(6-(phenylamino)-9H-purin-8-yl)benzonitrile		Investigative	[22]
Synonyms	CHEMBL1210236; BDBM50322829 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 26 nM
External Link	CID: 46894038 TTD: D0V6HG
Compound Name	DM-204		Investigative	[32]
Synonyms	Anti-GSK-3beta mAbs, DiaMedica; Anti-GSK-3beta mAbs, Sanomune; Anti-GSK-3beta monoclonal antibodies, DiaMedica; Anti-GSK-3beta monoclonal antibodies, Sanomune Click to Show/Hide
External Link	TTD: D0WN1N
Compound Name	CHIR-98023		Investigative	[14]
Synonyms	CT-98014 Click to Show/Hide
MOA	Inhibitor
Activity	Ki = 0.09 nM
External Link	CID: 9847557 TTD: D0X4CO
Compound Name	8-O-(4-toluenesulfonyl)manzamine A		Investigative	[21]
Synonyms	CHEMBL403561 Click to Show/Hide
MOA	Inhibitor
External Link	CID: 101437199 TTD: D0X4KR
Compound Name	N-(6-chloro-5-phenyl-1H-indazol-3-yl)butyramide		Investigative	[31]
Synonyms	CHEMBL1095040; N-(6-chloro-5-phenyl-1H-indazol-3-yl)butanamide; 3lfs; SCHEMBL1461347; WGVVIVGNBSSANI-UHFFFAOYSA-N; BDBM50313661; N-(5-phenyl-6-chloro-1H-indazol-3-yl)butanamide Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 80 nM
External Link	CID: 22319604 TTD: D0YM4A
Compound Name	CHIR-98014		Investigative	[16]
Synonyms	CHIR98014; CHIR 98014 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 0.6 nM
External Link	CID: 53396311 TTD: D04ZWF
Compound Name	alsterpaullone 2-cyanoethyl		Investigative	[33]
Synonyms	alsterpaullone derivative7 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 0.8 nM
External Link	CID: 16760286 TTD: D05NKG
Compound Name	indirubin deriv. 8a		Investigative	[34]
MOA	Inhibitor
External Link	CID: 135398521 TTD: D0B3ZB
Compound Name	LEUCETTAMINE B		Investigative	[35]
Synonyms	CHEMBL485053; SCHEMBL13219029 Click to Show/Hide
MOA	Inhibitor
External Link	CID: 10037501 TTD: D0K1DR
Compound Name	SB-415286		Investigative	[14]
Synonyms	SB 415286; 264218-23-7; SB415286; 3-(3-chloro-4-hydroxyphenylamino)-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione; 3-(3-chloro-4-hydroxyphenylamino)-4-(4-nitrophenyl)-1H-pyrrole-2,5-dione; CHEMBL322970; 3-(3-chloro-4-hydroxyanilino)-4-(2-nitrophenyl)pyrrole-2,5-dione; 3-[(3-chloro-4-hydroxyphenyl)amino]-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione; 1H-Pyrrol-2,5-dione, 3-((3-chloro-4-hydroxyphenyl)amino)-4-(2-nitrophenyl)-; SMR000568415; SR-01000075855 Click to Show/Hide
MOA	Inhibitor
Activity	Ki = 24 nM
External Link	CID: 4210951 TTD: D0N4WB
Compound Name	MANZAMINE A		Investigative	[36]
Synonyms	104196-68-1; CHEMBL611781; SCHEMBL11915472 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 8400 nM
External Link	CID: 6509753 TTD: D0Q4QF
Compound Name	PYRAZOLOPYRIDAZINE 1		Investigative	[37]
Synonyms	551920-54-8; GW810576X; n-(3-methoxyphenyl)-4-pyrazolo[1,5-b]pyridazin-3-yl-2-pyrimidinamine; pyrazolo[1,5-b]pyridazine deriv. 19; AC1O6ZIQ; CHEMBL187081; BDBM8128; SCHEMBL4489357; CTK1F7320; DTXSID60424889; HMS3305F24; HMS3303K24; ZINC13582569; NCGC00242229-01; DA-42106; FT-0707969; AB01092291-01; 2-Pyrimidinamine, N-(3-methoxyphenyl)-4-pyrazolo[1,5-b]pyridazin-3-yl-; N-(3-methoxyphenyl)-4-pyrazolo[1,5-b]pyridazin-3-ylpyrimidin-2-amine Click to Show/Hide
MOA	Inhibitor
Activity	Ki = 10 nM
External Link	CID: 6539361 TTD: D02DLC
Compound Name	RGB-286147		Investigative	[33]
Synonyms	pyrazolopyrimidone analog, RGB-286147 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 754 nM
External Link	CID: 135473382 TTD: D0J4ON
Compound Name	PYRAZOLOPYRIDAZINE 2		Investigative	[37]
Synonyms	pyrazolo[1,5-b]pyridazine deriv. 25; AC1O6ZJ2; BDBM8134; CHEMBL186054; N-(3,4-dimethoxyphenyl)-4-pyrazolo[1,5-b]pyridazin-3-ylpyrimidin-2-amine Click to Show/Hide
MOA	Inhibitor
Activity	Ki = 10 nM
External Link	CID: 6539367 TTD: D0O0VP
Compound Name	K00244		Investigative	[38]
Synonyms	GSK-3 Inhibitor XIII; N-(5-methyl-1H-pyrazol-3-yl)-2-phenylquinazolin-4-amine; GSK3-XIII; 404828-08-6; CHEMBL359482; (5-Methyl-1H-pyrazol-3-yl)-(2-phenylquinazolin-4-yl)amine; CHEBI:78544; AC1O4WD1; SCHEMBL462877; GTPL5976; CTK4I3154; HMS3229I06; BDBM228657; BCP12434; BDBM50162083; ZINC16052235; IN1311; AKOS025394676; DB08454; CCG-101293; NCGC00387776-01; ACM404828086; RT-013126; N-(3-methyl-1H-pyrazol-5-yl)-2-phenylquinazolin-4-amine; (5-Methyl-1H-pyrazol-3-yl)-(2-phenyl-quinazolin-4-yl)-amine Click to Show/Hide
MOA	Inhibitor
Activity	Ki = 22 nM
External Link	CID: 6419766 TTD: D0Q7TO DrugBank: DB08454
Compound Name	Quinoxaline1		Investigative	[33]
MOA	Inhibitor
Activity	IC50 = 1000 nM
External Link	CID: 438981 TTD: D0R5FH
Compound Name	TWS-119		Investigative	[39]
Synonyms	TWS119; 601514-19-6; 3-[[6-(3-Aminophenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]oxy]phenol; TWS 119; GSK inhibitor XII; GSK-3beta Inhibitor XII, TWS119; Neurogenesis Inducer, TWS119; CHEMBL405759; 3-(6-(3-aminophenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yloxy)phenol; 3-((6-(3-AMINOPHENYL)-7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)OXY)PHENOL; 3-{[6-(3-aminophenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]oxy}phenol; Phenol, 3-[[6-(3-aminophenyl)-1H-pyrrolo[2,3-d]pyrimidin-4-yl]oxy]-; K00245; MLS006011018; GTPL5980; SCHEMBL5559045; GSK-3BETA INHIB Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 30 nM
External Link	CID: 9549289 TTD: D0T8KR
Compound Name	AS-601245		Investigative	[40]
Synonyms	JNK Inhibitor V; SAPK Inhibitor V; 1,3-Benzothiazol-2-yl-(2-((2-(3-pyridinyl)ethyl)amino)-4-pyrimidinyl)acetonitrile; GTPL5997; SCHEMBL12242792; MolPort-044-724-552; HMS3229I20; CCG-206858; RT-013405; J-019673 Click to Show/Hide
MOA	Inhibitor
External Link	CID: 10109823 TTD: D04QCF
Compound Name	AZAKENPAULLONE		Investigative	[17]
Synonyms	1-Azakenpaullone; 676596-65-9; 9-bromo-7,12-dihydropyrido[3',2':2,3]azepino[4,5-b]indol-6(5H)-one; C15H10BrN3O; Kinome_3492; 1-AKP; SCHEMBL378920; GTPL8018; CHEMBL336961; BDBM7497; DTXSID8042686; NOCAS_42686; CTK8F0375; MolPort-003-844-675; CHEBI:131490; HMS3653A17; HMS3229B07; BCP21061; ZINC13588927; s7193; 2138AH; 1-Azakenpaullone, > AKOS030240424; SB19270; TRA0006688; NCGC00386322-01; RT-006179; FT-0662368; SW220021-1; KS-00001866 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 18 nM
External Link	CID: 6538897 TTD: D0DR8N
Compound Name	Thieno analogue of kenpaullone		Investigative	[17]
Synonyms	Paullone Analogue 71; CHEMBL323657; SCHEMBL5688610; BDBM7336; NSC 703058; 8-Bromo-6,11-dihydro-thieno[3 ,2 :2,3]azepino[4,5-b]indol-5(4H)-one; 9-Bromo-5,4-(epithioetheno)-1,2,3,6-tetrahydroazepino[4,5-b]indole-2-one Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 119.95 nM
External Link	CID: 6538761 TTD: D0TF9P
Compound Name	L-779450		Investigative	[41]
Synonyms	303727-31-3; L-779,450; 2-chloro-5-(2-phenyl-5-(pyridin-4-yl)-1H-imidazol-4-yl)phenol; L779450; CHEMBL373011; 2-chloro-5-(2-phenyl-5-pyridin-4-yl-1H-imidazol-4-yl)phenol; 2-(Phenyl)-4-(3-hydroxy-4-chlorophenyl)-5-(4-pyridyl)-1H-imidazole; 2-Chloro-5-[2-phenyl-5-(4-pyridinyl)-1H-imidazol-4-yl]phenol; C20H14ClN3O; L 779450; 2-chloro-5-[2-phenyl-5-(pyridin-4-yl)-1H-imidazol-4-yl]phenol; 2-chloro-5-[2-phenyl-4-(pyridin-4-yl)-1H-imidazol-5-yl]phenol; 2-chloro-5-(2-phenyl-4-(pyridin-4-yl)-1H-imidazol-5-yl)phenol Click to Show/Hide
MOA	Inhibitor
External Link	CID: 9950176 TTD: D06WJA
Compound Name	NU-6102		Investigative	[42]
Synonyms	nu6102; 444722-95-6; NU 6102; O6-CYCLOHEXYLMETHOXY-2-(4'-SULPHAMOYLANILINO) PURINE; Cdk1/2 Inhibitor II, NU6102; 6-Cyclohexylmethoxy-2-(4& -sulfamoylanilino)purine; 4-{[6-(cyclohexylmethoxy)-9H-purin-2-yl]amino}benzenesulfonamide; 4SP; 1h1s; 4-[[6-(cyclohexylmethoxy)-7H-purin-2-yl]amino]benzenesulfonamide; 4-{[6-(cyclohexylmethoxy)-7h-purin-2-yl]amino}benzenesulfonamide; 4-[[6-(cyclohexylmethoxy)-9h-purin-2-yl]amino]benzenesulfonamide; 4eor; 4eok; 2iw9; 2c6o; 2iw8; AC1L1IGA; SCHEMBL2170816; CHEMBL319467 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 40 nM
External Link	CID: 4566 TTD: D0Y5RO DrugBank: DB07126
Compound Name	PF-228		Investigative	[43]
Synonyms	869288-64-2; PF-573228; PF 573228; PF573228; CHEMBL514554; 3,4-Dihydro-6-[[4-[[[3-(methylsulfonyl)phenyl]methyl]amino]-5-(trifluoromethyl)-2-pyrimidinyl]amino]-2(1H)-quinolinone; 6-((4-((3-(Methylsulfonyl)benzyl)amino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)-3,4-dihydroquinolin-2(1H)-one; 6-(4-(3-(methylsulfonyl)benzylamino)-5-(trifluoromethyl)pyrimidin-2-ylamino)-3,4-dihydroquinolin-2(1H)-one; 6-[4-(3-Methanesulfonyl-benzylamino)-5-trifluoromethyl-pyrimidin-2-ylamino]-3,4-dihydro-1H-quinolin-2-one Click to Show/Hide
MOA	Inhibitor
Activity	IC50 > 1000 nM
External Link	CID: 11612883 TTD: D02QAZ
Compound Name	BX-912		Investigative	[44]
Synonyms	BX 912; BX912 Click to Show/Hide
MOA	Inhibitor
External Link	CID: 11754511 TTD: D0IX7Y
Compound Name	BX-795		Investigative	[44]
Synonyms	BX795; BX 795 Click to Show/Hide
MOA	Inhibitor
External Link	CID: 10077147 TTD: D0RG0Z
Compound Name	PMID19115845C89S		Investigative	[45]
Synonyms	3du8; GTPL8114; BDBM27380; DB07149 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 146 nM
External Link	CID: 16757525 TTD: D0T8NU DrugBank: DB07149
Compound Name	STAUROSPORINONE		Investigative	[46]
MOA	Inhibitor
External Link	TTD: D0GB4V
Compound Name	Ro31-8220		Investigative	[46]
Synonyms	Bisindolylmaleimide IX; ro 31-8220; 125314-64-9; Ro 31 8220; Ro 318220; UNII-W9A0B5E78O; Ro-318220; Ro-31-8220; CHEMBL6291; W9A0B5E78O; CHEBI:38912; 3-{3-[4-(1-methyl-1H-indol-3-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]-1H-indol-1-yl}propyl carbamimidothioate; 3-{3-[4-(1-methyl-1H-indol-3-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]-1H-indol-1-yl}propyl imidothiocarbamate; CHEMBL1591531; Carbamimidothioic acid, 3-(3-(2,5-dihydro-4-(1-methyl-1H-indol-3-yl)-2,5-dioxo-1H-pyrrol-3-yl)-1H-indol-1-yl)propyl; bisindolymaleimide IX Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 2.8 nM
External Link	CID: 5083 TTD: D0M5FF
Compound Name	AMP-PNP		Investigative	[47]
Synonyms	Phosphoaminophosphonic acid-adenylate ester; gamma-Imino-ATP; ADENYLYL IMIDODIPHOSPHATE; AMPPNP; Adenyl imidodiphosphate; 25612-73-1; adenyl-5'-yl imidodiphosphate; CHEBI:47785; App(NH)p; O(5')-(1,2-dihydroxy-2-phosphonoaminodiphosphoryl)adenosine; 5'-O-(hydroxy{[hydroxy(phosphonoamino)phosphoryl]oxy}phosphoryl)adenosine; [[[[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-hydroxyphosphoryl]amino]phosphonic acid; p(NH)Ppf; beta,gamma-Imido-ATP; beta,gamma-Imidoadenosine Click to Show/Hide
MOA	Inhibitor
External Link	CID: 33113 TTD: D00ICA
Compound Name	ELLAGIC ACID		Investigative	[48]
Synonyms	476-66-4; Benzoaric acid; Lagistase; Eleagic acid; Alizarine Yellow; Elagostasine; 2,3,7,8-Tetrahydroxychromeno[5,4,3-cde]chromene-5,10-dione; Ellagic acid dihydrate; Llagic acid; Acide ellagique; Acido elagico; Acidum ellagicum; C.I. 55005; Gallogen (VAN); Gallogen (astringent); C.I. 75270; Ellagate; Ellagic acid [INN:DCF]; UNII-19YRN3ZS9P; Acido elagico [INN-Spanish]; CCRIS 774; Gallogen, astringent; Acide ellagique [INN-French]; Acidum ellagicum [INN-Latin]; MLS000069632; C14H6O8; EINECS 207-508-3; NSC407286; NSC 40728 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 7500 nM
External Link	CID: 5281855 TTD: D0A1CM DrugBank: DB08846
Compound Name	CI-1040		Investigative	[46]
MOA	Inhibitor
External Link	CID: 6918454 TTD: D0B9BU DrugBank: DB12429
Compound Name	4,5,6,7-tetrabromo-1H-benzo[d][1,2,3]triazole		Investigative	[49]
Synonyms	4,5,6,7-tetrabromobenzotriazole Click to Show/Hide
MOA	Inhibitor
External Link	CID: 1694 TTD: D0O1YH DrugBank: DB04462
Compound Name	4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol		Investigative	[50]
MOA	Inhibitor
External Link	CID: 9859248 TTD: D0A5RM
Compound Name	Bisindolylmaleimide-I		Investigative	[46]
Synonyms	Bisindolylmaleimide i; 133052-90-1; GF 109203X; GF109203X; Go 6850; GF-109203X; RBT205 INHIBITOR; Go-6850; UNII-L79H6N0V6C; Bisindolylmaleimide I (GF 109203X); CHEMBL7463; 3-{1-[3-(DIMETHYLAMINO)PROPYL]-1H-INDOL-3-YL}-4-(1H-INDOL-3-YL)-1H-PYRROLE-2,5-DIONE; 3-(1-(3-(Dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione; L79H6N0V6C; QMGUOJYZJKLOLH-UHFFFAOYSA-N; 2-[1-(3-dimethylaminopropyl)indol-3-yl]-3-(indol-3-yl)maleimide; GF-109203; Go6850 Click to Show/Hide
MOA	Inhibitor
Activity	IC50 = 190.55 nM
External Link	CID: 2396 TTD: D0TO6S DrugBank: DB03777
2C60: Breast cancer		2 Compound(s) Regulating the Disease	Click to Show/Hide the Full List
Compound Name	Entrectinib		Approved	[51]
Synonyms	1108743-60-7; RXDX-101; UNII-L5ORF0AN1I; Entrectinib (RXDX-101); L5ORF0AN1I; Benzamide, N-[5-[(3,5-difluorophenyl)methyl]-1H-indazol-3-yl]-4-(4-methyl-1-piperazinyl)-2-[(tetrahydro-2H-pyran-4-yl)amino]-; Benzamide, N-(5-((3,5-difluorophenyl)methyl)-1H-indazol-3-yl)-4-(4-methyl-1-piperazinyl)-2-((tetrahydro-2H-pyran-4-yl)amino)-; Entrectinib [USAN:INN]; YMX; Kinome_2659; Entrectinib(rxdx-101); Entrectinib (USAN/INN); SCHEMBL3512601; GTPL8290; CHEMBL1983268; KS-00000TSK Click to Show/Hide
External Link	CID: 25141092 TTD: D0O0LS DrugBank: DB11986
Compound Name	Everolimus		Approved	[52]
External Link	CID: 6442177 TTD: D09ZSC DrugBank: DB01590

References

Ref 1	LncRNA UCA1 promotes SOX12 expression in breast cancer by regulating m(6)A modification of miR-375 by METTL14 through DNA methylation. Cancer Gene Ther. 2022 Jul;29(7):1043-1055. doi: 10.1038/s41417-021-00390-w. Epub 2022 Jan 13.
Ref 2	N6-methyladenosine regulated FGFR4 attenuates ferroptotic cell death in recalcitrant HER2-positive breast cancer. Nat Commun. 2022 May 13;13(1):2672. doi: 10.1038/s41467-022-30217-7.
Ref 3	Novel and selective DNA methyltransferase inhibitors: Docking-based virtual screening and experimental evaluation. Bioorg Med Chem. 2010 Jan 15;18(2):822-9. doi: 10.1016/j.bmc.2009.11.050. Epub 2009 Nov 27.
Ref 4	DNA methyltransferase inhibitors: an updated patent review (2012-2015). Expert Opin Ther Pat. 2016 Sep;26(9):1017-30. doi: 10.1080/13543776.2016.1209488. Epub 2016 Jul 18.
Ref 5	SAR around (l)-S-adenosyl-l-homocysteine, an inhibitor of human DNA methyltransferase (DNMT) enzymes. Bioorg Med Chem Lett. 2009 May 15;19(10):2747-51. doi: 10.1016/j.bmcl.2009.03.113. Epub 2009 Mar 28.
Ref 6	Constrained (l-)-S-adenosyl-l-homocysteine (SAH) analogues as DNA methyltransferase inhibitors. Bioorg Med Chem Lett. 2009 May 15;19(10):2742-6.
Ref 7	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
Ref 8	Evidence for irreversible inhibition of glycogen synthase kinase-3Beta by tideglusib. J Biol Chem. 2012 Jan 6;287(2):893-904. doi: 10.1074/jbc.M111.306472. Epub 2011 Nov 18.
Ref 9	9-ING-41, a small molecule inhibitor of GSK-3beta, potentiates the effects of anticancer therapeutics in bladder cancer. Sci Rep. 2019 Dec 27;9(1):19977. doi: 10.1038/s41598-019-56461-4.
Ref 10	Glycogen synthase kinase 3 (GSK-3) inhibitors: a patent update (2014-2015). Expert Opin Ther Pat. 2017 Jun;27(6):657-666. doi: 10.1080/13543776.2017.1259412. Epub 2016 Nov 21.
Ref 11	The GSK3 kinase inhibitor lithium produces unexpected hyperphosphorylation of Beta-catenin, a GSK3 substrate, in human glioblastoma cells. Biol Open. 2018 Jan 26;7(1):bio030874. doi: 10.1242/bio.030874.
Ref 12	Company report (Neurim Pharmaceuticals)
Ref 13	Identification of novel scaffold of benzothiazepinones as non-ATP competitive glycogen synthase kinase-3Beta inhibitors through virtual screening. Bioorg Med Chem Lett. 2012 Dec 1;22(23):7232-6. doi: 10.1016/j.bmcl.2012.09.043. Epub 2012 Sep 23.
Ref 14	Fragment and knowledge-based design of selective GSK-3beta inhibitors using virtual screening models. Eur J Med Chem. 2009 Jun;44(6):2361-71. doi: 10.1016/j.ejmech.2008.08.012. Epub 2008 Sep 16.
Ref 15	Cyclin-dependent kinase inhibitors for cancer therapy: a patent review (2009 - 2014). Expert Opin Ther Pat. 2015;25(9):953-70. doi: 10.1517/13543776.2015.1045414. Epub 2015 Jul 13.
Ref 16	Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo. Diabetes. 2003 Mar;52(3):588-95. doi: 10.2337/diabetes.52.3.588.
Ref 17	1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta. Bioorg Med Chem Lett. 2004 Jan 19;14(2):413-6. doi: 10.1016/j.bmcl.2003.10.062.
Ref 18	AZD1080, a novel GSK3 inhibitor, rescues synaptic plasticity deficits in rodent brain and exhibits peripheral target engagement in humans. J Neurochem. 2013 May;125(3):446-56. doi: 10.1111/jnc.12203. Epub 2013 Mar 11.
Ref 19	Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029796)
Ref 20	Discovery of potent and bioavailable GSK-3beta inhibitors. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1693-6. doi: 10.1016/j.bmcl.2010.01.038. Epub 2010 Jan 25.
Ref 21	Glycogen synthase kinase-3 (GSK-3) inhibitory activity and structure-activity relationship (SAR) studies of the manzamine alkaloids. Potential for Alzheimer's disease. J Nat Prod. 2007 Sep;70(9):1397-405. doi: 10.1021/np060092r. Epub 2007 Aug 21.
Ref 22	Novel 8-arylated purines as inhibitors of glycogen synthase kinase. Eur J Med Chem. 2010 Aug;45(8):3389-93. doi: 10.1016/j.ejmech.2010.04.026. Epub 2010 Apr 28.
Ref 23	Rational design of potent GSK3beta inhibitors with selectivity for Cdk1 and Cdk2. Bioorg Med Chem Lett. 2010 Mar 15;20(6):1985-9. doi: 10.1016/j.bmcl.2010.01.114. Epub 2010 Jan 25.
Ref 24	Scaffold hopping and optimization towards libraries of glycogen synthase kinase-3 inhibitors. Bioorg Med Chem Lett. 2002 Jun 3;12(11):1525-8. doi: 10.1016/s0960-894x(02)00169-5.
Ref 25	Novel GSK-3beta inhibitors from sequential virtual screening. Bioorg Med Chem. 2008 Jan 15;16(2):636-43. doi: 10.1016/j.bmc.2007.10.047. Epub 2007 Oct 22.
Ref 26	How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
Ref 27	Design, synthesis, and biological evaluation of novel 7-azaindolyl-heteroaryl-maleimides as potent and selective glycogen synthase kinase-3beta (GSK-3beta) inhibitors. Bioorg Med Chem. 2004 Jun 15;12(12):3167-85. doi: 10.1016/j.bmc.2004.04.010.
Ref 28	Manzamine B and E and ircinal A related alkaloids from an Indonesian Acanthostrongylophora sponge and their activity against infectious, tropical parasitic, and Alzheimer's diseases. J Nat Prod. 2006 Jul;69(7):1034-40. doi: 10.1021/np0601399.
Ref 29	Novel indolylmaleimide acts as GSK-3beta inhibitor in human neural progenitor cells. Bioorg Med Chem. 2010 Sep 15;18(18):6785-95. doi: 10.1016/j.bmc.2010.07.045. Epub 2010 Jul 25.
Ref 30	Synthesis and antiproliferative activity of 7-azaindirubin-3'-oxime, a 7-aza isostere of the natural indirubin pharmacophore. J Nat Prod. 2009 Dec;72(12):2199-202. doi: 10.1021/np9003905.
Ref 31	Design of potent and selective GSK3beta inhibitors with acceptable safety profile and pharmacokinetics. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2344-9. doi: 10.1016/j.bmcl.2010.01.132. Epub 2010 Feb 2.
Ref 32	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. (Target id: 2030).
Ref 33	A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. Proc Natl Acad Sci U S A. 2007 Dec 18;104(51):20523-8. doi: 10.1073/pnas.0708800104. Epub 2007 Dec 11.
Ref 34	Structural basis for the synthesis of indirubins as potent and selective inhibitors of glycogen synthase kinase-3 and cyclin-dependent kinases. J Med Chem. 2004 Feb 12;47(4):935-46. doi: 10.1021/jm031016d.
Ref 35	Synthesis and preliminary biological evaluation of new derivatives of the marine alkaloid leucettamine B as kinase inhibitors. Eur J Med Chem. 2010 Feb;45(2):805-10. doi: 10.1016/j.ejmech.2009.10.009. Epub 2009 Oct 12.
Ref 36	2-N-Methyl modifications and SAR studies of manzamine A. Bioorg Med Chem. 2008 Jul 15;16(14):6702-6. doi: 10.1016/j.bmc.2008.05.079. Epub 2008 Jun 5.
Ref 37	N-Phenyl-4-pyrazolo[1,5-b]pyridazin-3-ylpyrimidin-2-amines as potent and selective inhibitors of glycogen synthase kinase 3 with good cellular efficacy. J Med Chem. 2004 Sep 9;47(19):4716-30. doi: 10.1021/jm040063i.
Ref 38	The discovery of the potent aurora inhibitor MK-0457 (VX-680). Bioorg Med Chem Lett. 2009 Jul 1;19(13):3586-92. doi: 10.1016/j.bmcl.2009.04.136. Epub 2009 May 3.
Ref 39	Diversity-oriented synthesis: exploring the intersections between chemistry and biology. Nat Chem Biol. 2005 Jul;1(2):74-84. doi: 10.1038/nchembio0705-74.
Ref 40	The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315. doi: 10.1042/BJ20070797.
Ref 41	The identification of potent and selective imidazole-based inhibitors of B-Raf kinase. Bioorg Med Chem Lett. 2006 Jan 15;16(2):378-81. doi: 10.1016/j.bmcl.2005.09.072. Epub 2005 Nov 2.
Ref 42	Triazolo[1,5-a]pyrimidines as novel CDK2 inhibitors: protein structure-guided design and SAR. Bioorg Med Chem Lett. 2006 Mar 1;16(5):1353-7. doi: 10.1016/j.bmcl.2005.11.048. Epub 2005 Dec 1.
Ref 43	Cellular characterization of a novel focal adhesion kinase inhibitor. J Biol Chem. 2007 May 18;282(20):14845-52. doi: 10.1074/jbc.M606695200. Epub 2007 Mar 28.
Ref 44	Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. J Biol Chem. 2005 May 20;280(20):19867-74. doi: 10.1074/jbc.M501367200. Epub 2005 Mar 16.
Ref 45	First Cdc7 kinase inhibitors: pyrrolopyridinones as potent and orally active antitumor agents. 2. Lead discovery. J Med Chem. 2009 Jan 22;52(2):293-307. doi: 10.1021/jm800977q.
Ref 46	Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105. doi: 10.1042/0264-6021:3510095.
Ref 47	The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. doi: 10.1093/nar/28.1.235.
Ref 48	Identification of ellagic acid as potent inhibitor of protein kinase CK2: a successful example of a virtual screening application. J Med Chem. 2006 Apr 20;49(8):2363-6. doi: 10.1021/jm060112m.
Ref 49	Optimization of protein kinase CK2 inhibitors derived from 4,5,6,7-tetrabromobenzimidazole. J Med Chem. 2004 Dec 2;47(25):6239-47. doi: 10.1021/jm049854a.
Ref 50	4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. J Med Chem. 2006 Nov 2;49(22):6500-9. doi: 10.1021/jm0605740.
Ref 51	Safety and Antitumor Activity of the Multitargeted Pan-TRK, ROS1, and ALK Inhibitor Entrectinib: Combined Results from Two Phase I Trials (ALKA-372... Cancer Discov. 2017 Apr;7(4):400-409.
Ref 52	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015

m6A-centered Crosstalk Information

Cite M6AREG

Correspondence

Prof. Feng ZHU

Prof. Shuiping Liu

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