Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
Crosstalk ID
M6ACROT05278
[1]
Non-coding RNA miR-6125 YTHDF2  lncRNA       miRNA   circRNA Direct Inhibition m6A modification GSK3B GSK3B YTHDF2 : m6A sites
m6A Modification:
m6A Regulator YTH domain-containing family protein 2 (YTHDF2) READER
m6A Target Glycogen synthase kinase-3 beta (GSK3Beta/GSK3B)
Epigenetic Regulation that have Cross-talk with This m6A Modification:
Epigenetic Regulation Type Non-coding RNA (ncRNA)
Epigenetic Regulator hsa-miR-6125 microRNA View Details
Regulated Target YTH domain-containing family protein 2 (YTHDF2) View Details
Crosstalk Relationship ncRNA  →  m6A Inhibition
Crosstalk Mechanism ncRNAs directly impacts m6A modification through modulating the expression level of m6A regulator
Crosstalk Summary hsa-miR-6125 targeted the 3'-UTR of YTHDF2 and downregulated the YTHDF2 protein, thereby increasing the stability of m6A-modified Glycogen synthase kinase-3 beta (GSK3Beta/GSK3B) mRNA.
Responsed Disease Colorectal cancer ICD-11: 2B91
In-vivo Model nude mice were randomly divided into four groups and injected subcutaneously with SW480 (Vector), SW480 (miR-6125), RKO (Vector) or RKO (miR-6125) cells on the back region (5.0 × 106 cells in 100 μl PBS/mouse).
Full List of Potential Compound(s) Related to This m6A-centered Crosstalk
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 [2]
MOA Inhibitor
External Link
 Compound Name Tideglusib Phase 2 [3]
Synonyms
NP-031112; NP-12; NP031112; Tideglusib(NP-031112)
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 78 nM
External Link
 Compound Name 9-ING-41 Phase 2 [4]
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
 Compound Name LY2090314 Phase 2 [5]
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
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MOA Modulator
Activity IC50 = 0.9 nM
External Link
 Compound Name Lithium Phase 2 [6]
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
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MOA Inhibitor
External Link
 Compound Name Neu-120 Phase 1/2 [7]
Synonyms
Neu-108; NMDA receptor modulators (Parkinson's Disease), Neurim
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MOA Modulator
External Link
 Compound Name TDZD-8 Patented [8]
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
 Compound Name AR-A014418 Patented [9]
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
 Compound Name PMID26161698-Compound-18 Patented [10]
MOA Inhibitor
Activity IC50 = high nM
External Link
 Compound Name CHIR-99021 Patented [11]
Synonyms
CHIR99021; CHIR 99021; CT-99021; CT99021
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MOA Inhibitor
Activity IC50 = 30 nM
External Link
 Compound Name KENPAULLONE Patented [12]
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
 Compound Name AZD-1080 Discontinued in Phase 1 [13]
MOA Modulator
Activity IC50 = 31 nM
External Link
 Compound Name SAN-61 Terminated [14]
Synonyms
SAN-AL-61; Oral beta amyloid inhibitor (Alzheimer's disease), Sanomune
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MOA Inhibitor
External Link
 Compound Name RO-320432 Terminated [15]
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
 Compound Name 8-O-(4-chlorobenzenesulfonyl)manzamine F Investigative [16]
Synonyms
CHEMBL400717
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MOA Inhibitor
Activity IC50 = 7200 nM
External Link
 Compound Name N,8-diphenyl-9H-purin-6-amine Investigative [17]
Synonyms
CHEMBL1210175; N,8-Diphenyl-9H-purine-6-amine; BDBM50322830; SR-01000661492
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MOA Inhibitor
Activity IC50 = 16 nM
External Link
 Compound Name N-(8-(3-cyanophenyl)-9H-purin-6-yl)pentanamide Investigative [17]
Synonyms
CHEMBL1210476
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MOA Inhibitor
Activity IC50 = 1220 nM
External Link
 Compound Name N-(6-(3-hydroxyphenyl)-1H-indazol-3-yl)butyramide Investigative [18]
Synonyms
CHEMBL1086639; SCHEMBL6485118; UKQRPDHIQLHFNS-UHFFFAOYSA-N; BDBM50313706
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MOA Inhibitor
Activity IC50 = 94 nM
External Link
 Compound Name GSK-3beta inhibitor II Investigative [19]
Synonyms
GSK-3b inhibitor II
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MOA Inhibitor
Activity IC50 = 390 nM
External Link
 Compound Name 3-phenyl-4-(phenylamino)-1H-pyrrole-2,5-dione Investigative [20]
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
 Compound Name 8-O-(4-bromobenzenesulfonyl)manzamine F Investigative [16]
Synonyms
CHEMBL414128
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MOA Inhibitor
Activity IC50 = 23000 nM
External Link
 Compound Name I-5 Investigative [21]
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
 Compound Name GSK-3beta inhibitor XI Investigative [22]
Synonyms
GSK-3b inhibitor XI
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MOA Inhibitor
Activity IC50 = 5 nM
External Link
 Compound Name Manzamine E Investigative [23]
MOA Inhibitor
External Link
 Compound Name N-(6-(4-fluorophenyl)-1H-indazol-3-yl)butyramide Investigative [18]
Synonyms
CHEMBL1084681; SCHEMBL4488738; ORRUGYIZWSJRJU-UHFFFAOYSA-N; BDBM50313680
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MOA Inhibitor
Activity IC50 = 5008 nM
External Link
 Compound Name N-(6-(2-chlorophenyl)-1H-indazol-3-yl)butyramide Investigative [18]
Synonyms
CHEMBL1086175; N-[6-(2-chlorophenyl)-1H-indazol-3-yl]butanamide; SCHEMBL6485112; WPJGFQOEGTUKTE-UHFFFAOYSA-N
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MOA Inhibitor
Activity IC50 = 1353 nM
External Link
 Compound Name N-(6-bromo-1H-indazol-3-yl)butyramide Investigative [18]
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
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MOA Inhibitor
Activity IC50 = 198 nM
External Link
 Compound Name Manzamine Y Investigative [23]
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
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MOA Inhibitor
External Link
 Compound Name IM-12 Investigative [24]
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
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MOA Inhibitor
Activity IC50 = 53 nM
External Link
 Compound Name N-(6-phenethyl-1H-indazol-3-yl)butyramide Investigative [18]
Synonyms
CHEMBL1084684; SCHEMBL6489338
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MOA Inhibitor
Activity IC50 = 8525 nM
External Link
 Compound Name N-(6-benzyl-1H-indazol-3-yl)butyramide Investigative [18]
Synonyms
CHEMBL1077260; SCHEMBL6490520
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MOA Inhibitor
Activity IC50 = 4140 nM
External Link
 Compound Name (2'Z,3'E)-7-Azaindirubin-3'-oxime Investigative [25]
MOA Inhibitor
External Link
 Compound Name N-(6-phenyl-1H-indazol-3-yl)butyramide Investigative [26]
Synonyms
CHEMBL1086174; SCHEMBL4493121
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MOA Inhibitor
Activity IC50 = 390 nM
External Link
 Compound Name Neo-kauluamine Investigative [23]
MOA Inhibitor
External Link
 Compound Name (E)-N-(6-(prop-1-enyl)-1H-indazol-3-yl)butyramide Investigative [18]
Synonyms
CHEMBL1086176
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MOA Inhibitor
Activity IC50 = 2459 nM
External Link
 Compound Name 8-OH-MANZAMINE A Investigative [23]
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
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MOA Inhibitor
External Link
 Compound Name 6-deoxymanzamine X Investigative [16]
MOA Inhibitor
External Link
 Compound Name N-(6-(4-aminophenyl)-1H-indazol-3-yl)butyramide Investigative [18]
Synonyms
CHEMBL1086638; N-[6-(4-aminophenyl)-1H-indazol-3-yl]butanamide; SCHEMBL6478145; DCCRABAZYMVLJU-UHFFFAOYSA-N
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MOA Inhibitor
Activity IC50 = 76 nM
External Link
 Compound Name N-(6-(trifluoromethyl)-1H-indazol-3-yl)butyramide Investigative [18]
Synonyms
N-[6-(trifluoromethyl)-1H-indazol-3-yl]butanamide; CHEMBL1086640; 599191-49-8; SCHEMBL1462440; RVYSDAGRNRYYML-UHFFFAOYSA-N
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MOA Inhibitor
Activity IC50 = 195 nM
External Link
 Compound Name PAULLONE Investigative [15]
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
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MOA Inhibitor
Activity IC50 = 4 nM
External Link
 Compound Name 12,13-DEHYDRO-8-O-ACETYLMANZAMINE A Investigative [16]
Synonyms
CHEMBL252520
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MOA Inhibitor
Activity IC50 = 4800 nM
External Link
 Compound Name N-(6-(pyridin-4-yl)-1H-indazol-3-yl)butyramide Investigative [18]
Synonyms
CHEMBL1086782; SCHEMBL1460286; BBNQSWZLWJBJIN-UHFFFAOYSA-N; BDBM50313652
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MOA Inhibitor
Activity IC50 = 661 nM
External Link
 Compound Name 4-(5-bromo-1H-indol-3-yl)pyrimidin-2-amine Investigative [9]
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
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MOA Inhibitor
Activity IC50 = 2000 nM
External Link
 Compound Name 9-N-METHYL-8-METHOXY-MANZAMINE A Investigative [16]
MOA Inhibitor
External Link
 Compound Name N-(6-(furan-3-yl)-1H-indazol-3-yl)butyramide Investigative [18]
Synonyms
CHEMBL1086781; SCHEMBL1461525; ZGQZPFJWHPTRAH-UHFFFAOYSA-N; BDBM50313709
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MOA Inhibitor
Activity IC50 = 260 nM
External Link
 Compound Name N-(6-chloro-5-p-tolyl-1H-indazol-3-yl)butyramide Investigative [18]
Synonyms
CHEMBL1097694; SCHEMBL1461361; REESNWQQNIKZJK-UHFFFAOYSA-N; BDBM50313666
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MOA Inhibitor
Activity IC50 = 14000 nM
External Link
 Compound Name 12,13-DEHYDROMANZAMINE A Investigative [16]
Synonyms
CHEMBL268202
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MOA Inhibitor
Activity IC50 = 5400 nM
External Link
 Compound Name CT-98024 Investigative [15]
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
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MOA Inhibitor
Activity IC50 = 0.56 nM
External Link
 Compound Name N-(6-(pyridin-3-yl)-1H-indazol-3-yl)butyramide Investigative [26]
Synonyms
CHEMBL1085918; SCHEMBL6489919; CZTAWAQITKVBNQ-UHFFFAOYSA-N; BDBM50313686
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MOA Inhibitor
Activity IC50 = 5900 nM
External Link
 Compound Name N-(6-chloro-1H-indazol-3-yl)butyramide Investigative [18]
Synonyms
CHEMBL1082235; N-(6-chloro-1H-indazol-3-yl)butanamide; SCHEMBL4497072; VHQZZDZWVQELLJ-UHFFFAOYSA-N
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MOA Inhibitor
Activity IC50 = 354 nM
External Link
 Compound Name 9-N-ETHYL-8-ETHOXY-MANZAMINE A Investigative [16]
Synonyms
CHEMBL403562
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 10400 nM
External Link
 Compound Name N-(6-(4-hydroxyphenyl)-1H-indazol-3-yl)butyramide Investigative [18]
MOA Inhibitor
Activity IC50 = 44 nM
External Link
 Compound Name N-(6-(thiophen-3-yl)-1H-indazol-3-yl)butyramide Investigative [18]
Synonyms
CHEMBL1083208; SCHEMBL1462380; KEXXQGBZRBKVRC-UHFFFAOYSA-N; BDBM50313653
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 935 nM
External Link
 Compound Name CP-70949 Investigative [27]
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
 Compound Name 3-(6-(phenylamino)-9H-purin-8-yl)benzonitrile Investigative [17]
Synonyms
CHEMBL1210236; BDBM50322829
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 26 nM
External Link
 Compound Name DM-204 Investigative [27]
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
 Compound Name CHIR-98023 Investigative [9]
Synonyms
CT-98014
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 0.09 nM
External Link
 Compound Name 8-O-(4-toluenesulfonyl)manzamine A Investigative [16]
Synonyms
CHEMBL403561
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name N-(6-chloro-5-phenyl-1H-indazol-3-yl)butyramide Investigative [26]
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
 Compound Name CHIR-98014 Investigative [11]
Synonyms
CHIR98014; CHIR 98014
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 0.6 nM
External Link
 Compound Name alsterpaullone 2-cyanoethyl Investigative [28]
Synonyms
alsterpaullone derivative7
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 0.8 nM
External Link
 Compound Name indirubin deriv. 8a Investigative [29]
MOA Inhibitor
External Link
 Compound Name LEUCETTAMINE B Investigative [30]
Synonyms
CHEMBL485053; SCHEMBL13219029
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name SB-415286 Investigative [9]
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
 Compound Name MANZAMINE A Investigative [31]
Synonyms
104196-68-1; CHEMBL611781; SCHEMBL11915472
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 8400 nM
External Link
 Compound Name PYRAZOLOPYRIDAZINE 1 Investigative [32]
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
 Compound Name RGB-286147 Investigative [28]
Synonyms
pyrazolopyrimidone analog, RGB-286147
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 754 nM
External Link
 Compound Name PYRAZOLOPYRIDAZINE 2 Investigative [32]
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
 Compound Name K00244 Investigative [33]
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
 Compound Name Quinoxaline1 Investigative [28]
MOA Inhibitor
Activity IC50 = 1000 nM
External Link
 Compound Name TWS-119 Investigative [34]
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
 Compound Name AS-601245 Investigative [35]
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
 Compound Name AZAKENPAULLONE Investigative [12]
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
 Compound Name Thieno analogue of kenpaullone Investigative [12]
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
 Compound Name L-779450 Investigative [36]
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
 Compound Name NU-6102 Investigative [37]
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
 Compound Name PF-228 Investigative [38]
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
 Compound Name BX-912 Investigative [39]
Synonyms
BX 912; BX912
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name BX-795 Investigative [39]
Synonyms
BX795; BX 795
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name PMID19115845C89S Investigative [40]
Synonyms
3du8; GTPL8114; BDBM27380; DB07149
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 146 nM
External Link
 Compound Name STAUROSPORINONE Investigative [41]
MOA Inhibitor
External Link
 Compound Name Ro31-8220 Investigative [41]
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
 Compound Name AMP-PNP Investigative [42]
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
 Compound Name ELLAGIC ACID Investigative [43]
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
 Compound Name CI-1040 Investigative [41]
MOA Inhibitor
External Link
 Compound Name 4,5,6,7-tetrabromo-1H-benzo[d][1,2,3]triazole Investigative [44]
Synonyms
4,5,6,7-tetrabromobenzotriazole
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol Investigative [45]
MOA Inhibitor
External Link
 Compound Name Bisindolylmaleimide-I Investigative [41]
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
2B91: Colorectal cancer 25 Compound(s) Regulating the Disease Click to Show/Hide the Full List
 Compound Name Retifanlimab Approved [46]
Synonyms
INCMGA0012; Retifanlimab
    Click to Show/Hide
External Link
 Compound Name Aflibercept Approved [47]
Synonyms
Ziv-Aflibercept; Zaltrap (TN); VEGF Trap; VEGF Trap-Eye
    Click to Show/Hide
External Link
 Compound Name Regorafenib Approved [48]
Synonyms
755037-03-7; BAY 73-4506; Regorafenibum; Stivarga; 4-(4-(3-(4-Chloro-3-(trifluoromethyl)phenyl)ureido)-3-fluorophenoxy)-N-methylpicolinamide; BAY73-4506; Regorafenib (BAY 73-4506); UNII-24T2A1DOYB; 4-[4-({[4-Chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide; BAY-73-4506; 24T2A1DOYB; CHEMBL1946170; CHEBI:68647; Stivarga (TN); BAY73-4506 hydrochloride; Regorafenib [USAN:INN]
    Click to Show/Hide
External Link
 Compound Name Bevacizumab Approved [49]
Synonyms
Bevacizumab (ophthalmic slow-release tissue tablet)
    Click to Show/Hide
External Link
 Compound Name SYM-004 Phase 3 [49]
Synonyms
Chimeric IgG1 antibody 1024 (cancer), Symphogen; Chimeric IgG1 antibody 992 (cancer), Symphogen; Chimeric IgG1 antibodies992 + 1024 (cancer), Symphogen
    Click to Show/Hide
External Link
 Compound Name Bevacizumab + Erlotinib Phase 3 [50]
External Link
 Compound Name CPI-613 Phase 3 [49]
Synonyms
95809-78-2; 6,8-bis(benzylthio)octanoic acid; CPI 613; MLS006010202; SCHEMBL1062218; 6,8-Bis(benzylsulfanyl)octanoic acid; Octanoic acid, 6,8-bis((phenylmethyl)thio)-; Octanoic acid, 6,8-bis[(phenylMethyl)thio]-; 6,8-Bis[(phenylmethyl)thio]octanoic acid; CPI613; CHEMBL3186849; QCR-193; AOB1058; MolPort-023-219-128; HMS3656L06; C22H28O2S2; BCP04663; EX-A2043; s2776; AKOS025142095; BCP9000552; DB12109; RL06062; CS-0961; NCGC00344764-01; SMR004701300; AS-16613; BC261916; AK174899; HY-15453; BCP0726000030; KB-293127; AB0035874
    Click to Show/Hide
External Link
 Compound Name Bevacizumab Approved [47]
External Link
 Compound Name AlloStim Phase 2/3 [51]
Synonyms
AlloStim (TN)
    Click to Show/Hide
External Link
 Compound Name Sibrotuzumab Phase 2 [52]
External Link
 Compound Name CV301 Phase 2 [53]
External Link
 Compound Name Efatutazone Phase 2 [54]
Synonyms
Inolitazone; 223132-37-4; 5-[[4-[[6-(4-amino-3,5-dimethylphenoxy)-1-methyl-1H-benzimidazol-2-yl]methoxy]phenyl]methyl]-2,4-Thiazolidinedione; Efatutazone [INN]; RS5444; CS-7017; SCHEMBL3246054; CHEMBL3545280; JCYNMRJCUYVDBC-UHFFFAOYSA-N; Efatutazone;CS-7017;RS5444; BCP07478; AKOS030526729; DB11894; CS-0778; KB-77905; DA-07988; HY-14792; QC-10456; 4CA-1384; FT-0737589; 5-[4-[6-(4-amino-3 ,5-dimethylphenoxy)-1-methyl-1H-benzimidazol-2-ylmethoxy]benzyl]thiazolidine-2,4-dione
    Click to Show/Hide
External Link
 Compound Name LOR-2040 Phase 2 [55]
External Link
 Compound Name RG7221 Phase 2 [56]
External Link
 Compound Name PEG-SN38 Phase 2 [57]
Synonyms
EZN-2208
    Click to Show/Hide
External Link
 Compound Name MEGF0444A Phase 2 [58]
External Link
 Compound Name Encapsulated cell therapy Phase 1/2 [59]
External Link
 Compound Name AB928 Phase 1/2 [60]
External Link
 Compound Name MGD007 Phase 1 [56]
External Link
 Compound Name BNC-101 Phase 1 [61]
External Link
 Compound Name Navicixizumab Phase 1 [49]
External Link
 Compound Name RG7160 Discontinued in Phase 2 [62]
External Link
 Compound Name Nimesulide Terminated [63]
Synonyms
51803-78-2; N-(4-Nitro-2-phenoxyphenyl)methanesulfonamide; Mesulid; Flogovital; Sulidene; Nimed; R-805; 4-NITRO-2-PHENOXYMETHANESULFONANILIDE; Nisulid; Nimesulidum [INN-Latin]; Nimesulida [INN-Spanish]; R 805; UNII-V4TKW1454M; 4-Nitro-2-phenoxy-methanesulfonanilide; 4'-Nitro-2'-phenoxymethanesulfonanilide; Methanesulfonamide, N-(4-nitro-2-phenoxyphenyl)-; EINECS 257-431-4; 4'-Nitro-2'-phenoxymethansulfonanilid; BRN 2421175; CHEMBL56367; MLS000069680; V4TKW1454M; Methanesulfonanilide, 4'-nitro-2'-phenoxy-; CHEBI:44445; Dulanermin
    Click to Show/Hide
External Link
 Compound Name Saracatinib Phase 2 [64]
External Link
 Compound Name G3139 + Irinotecan Investigative [65]
External Link
References
Ref 1 Downregulation of microRNA-6125 promotes colorectal cancer growth through YTHDF2-dependent recognition of N6-methyladenosine-modified GSK3beta. Clin Transl Med. 2021 Oct;11(10):e602. doi: 10.1002/ctm2.602.
Ref 2 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
Ref 3 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 4 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 5 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 6 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 7 Company report (Neurim Pharmaceuticals)
Ref 8 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 9 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 10 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 11 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 12 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 13 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 14 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 15 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 16 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.
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