Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
Crosstalk ID
M6ACROT03618
[1], [2]
Histone modification H3K4me3 SMYD2 LINC01605 Indirect Enhancement m6A modification PLAU PLAU METTL3 Methylation : m6A sites
m6A Modification:
m6A Regulator Methyltransferase-like 3 (METTL3) WRITER
m6A Target Urokinase-type plasminogen activator (PLAU)
Epigenetic Regulation that have Cross-talk with This m6A Modification:
Epigenetic Regulation Type Histone modification (HistMod)
Epigenetic Regulator N-lysine methyltransferase SMYD2 (SMYD2) WRITER View Details
Regulated Target Histone H3 lysine 4 trimethylation (H3K4me3) View Details
Downstream Gene LINC01605 View Details
Crosstalk Relationship Histone modification  →  m6A Enhancement
Crosstalk Mechanism histone modification indirectly regulates m6A modification through downstream signaling pathways
Crosstalk Summary LINC01605 was regulated by SMYD2-EP300-mediated modifications of histone Histone H3 lysine 4 trimethylation (H3K4me3) as well as H3K27ac. LINC01605 was found to bind to METTL3 and promote the m6A modification of SPTBN2 mRNA, thereby facilitating the translation of SPTBN2. METTL3 upregulated Urokinase-type plasminogen activator (PLAU) mRNA in an m6A-dependent manner, and then participated in MAPK/ERK pathway to promote angiogenesis and metastasis in CRC.
Responsed Disease Colorectal cancer ICD-11: 2B91
Pathway Response MAPK signaling pathway hsa04010
Cell Process Cell proliferation and metastasis
Cell apoptosis
In-vitro Model
HT29 Colon cancer Mus musculus CVCL_A8EZ
LoVo Colon adenocarcinoma Homo sapiens CVCL_0399
In-vivo Model 1 × 106 cells in 100 uL PBS (shMETTL3-1 or shNC) were respectively injected into each mouse through the tail vein. Pulmonary metastases were monitored after fourteen days using the imaging system (IVIS) Spectrum (PerkinElmer, USA).
Full List of Potential Compound(s) Related to This m6A-centered Crosstalk
N-lysine methyltransferase SMYD2 (SMYD2) 6 Compound(s) Regulating the Target Click to Show/Hide the Full List
 Compound Name AZ505 Preclinical [3]
Synonyms
AZ 505; AZ-505
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 120 nM
External Link
 Compound Name LLY-507 Preclinical [4]
Synonyms
1793053-37-8; LLY507; CHEMBL3414623; 5-Cyano-2'-{4-[2-(3-Methyl-1h-Indol-1-Yl)ethyl]piperazin-1-Yl}-N-[3-(Pyrrolidin-1-Yl)propyl]biphenyl-3-Carboxamide; 3-cyano-5-(2-{4-[2-(3-methyl-1H-indol-1-yl)ethyl]piperazin-1-yl}phenyl)-N-[3-(pyrrolidin-1-yl)propyl]benzamide; 3-Cyano-5-[2-[4-[2-(3-methyl-1H-indol-1-yl)ethyl]piperazin-1-yl]phenyl]-N-[3-(pyrrolidin-1-yl)propyl]benzamide; GTPL8239; SCHEMBL19760400; EX-A899; LLY 507; MolPort-042-624-530; BCP17114; s7575; BDBM50075102; ZINC231558920; AKOS027470175; CS-5126
    Click to Show/Hide
MOA Inhibitor
Activity IC50 < 15 nM
External Link
 Compound Name EPZ032597 Preclinical [5]
MOA Inhibitor
External Link
 Compound Name EPZ033294 Preclinical [5]
MOA Inhibitor
External Link
 Compound Name A-893 Preclinical [6]
Synonyms
1868232-32-9; (R)-N-cyclohexyl-3-((3,4-dichlorophenethyl)amino)-N-(2-((2-hydroxy-2-(3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-8-yl)ethyl)amino)ethyl)propanamide; CHEMBL3590526; N-Cyclohexyl-N~3~-[2-(3,4-Dichlorophenyl)ethyl]-N-(2-{[(2r)-2-Hydroxy-2-(3-Oxo-3,4-Dihydro-2h-1,4-Benzoxazin-8-Yl)ethyl]amino}ethyl)-Beta-Alaninamide; SCHEMBL17476248; EX-A2769; BDBM50095537; AKOS030235552; ZINC230499113; ACN-037539; AC-29886; HY-19563; CS-0015655; Q27454706; 4GQ; N-Cyclohexyl-3-[2-(3,4-dichlorophenyl)ethylamino]-N-[2-[[(2R)-2-hydroxy-2-(3-oxo-4H-1,4-benzoxazin-8-yl)ethyl]amino]ethyl]propanamide
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name BAY 598 Preclinical [7]
Synonyms
BAY-598; 1906919-67-2; CHEMBL3818617; 1906919-67-2 (S-isomer); (S,E)-N-(1-(N'-cyano-N-(3-(difluoromethoxy)phenyl)carbamimidoyl)-3-(3,4-dichlorophenyl)-4,5-dihydro-1H-pyrazol-4-yl)-N-ethyl-2-hydroxyacetamide; BAY 598 - Bio-X; BAY598; GTPL8953; EX-A1835; BDBM50180955; ZINC504786915; AC-31567; BS-16389; HY-19546; CS-0015642; J3.601.000B; Q27074893; (S)-N-(1-(N'-Cyano-N-(3-(difluoromethoxy)phenyl)carbamimidoyl)-3-(3,4-dichlorophenyl)-4,5-dihydro-1H-pyrazol-4-yl)-N-ethyl-2-hydroxyacetamide; (S,E)-N-(1-(N-cyano-N'-(3-(difluoromethoxy)phenyl)carbamimidoyl)-3-(3,4-dichlorophenyl)-4,5-dihydro-1H-pyrazol-4-yl)-N-ethyl-2-hydroxyacetamide; (S,Z)-N-(1-(N-cyano-N'-(3-(difluoromethoxy)phenyl)carbamimidoyl)-3-(3,4-dichlorophenyl)-4,5-dihydro-1H-pyrazol-4-yl)-N-ethyl-2-hydroxyacetamide; N-[(4S)-1-[(Cyanoamino)[[3-(difluoromethoxy)phenyl]imino]methyl]-3-(3,4-dichlorophenyl)-4,5-dihydro-1H-pyrazol-4-yl]-N-ethyl-2-hydroxyacetamide; N-[(4S)-1-[(Z)-N'-cyano-N-[3-(difluoromethoxy)phenyl]carbamimidoyl]-3-(3,4-dichlorophenyl)-4,5-dihydro-1H-pyrazol-4-yl]-N-ethyl-2-hydroxyacetamide
    Click to Show/Hide
MOA Inhibitor
External Link
Urokinase-type plasminogen activator (PLAU) 42 Compound(s) Regulating the Target Click to Show/Hide the Full List
 Compound Name Pro-urokinase Approved [8]
Synonyms
Thrombolyse (TN)
    Click to Show/Hide
MOA Modulator
External Link
 Compound Name Urokinase Approved [9]
MOA Modulator
External Link
 Compound Name PAI-1 Phase 4 [10]
Synonyms
PA Autoinducer; Pseudomonas aeruginosa autoinducer; N-(3-Oxododecanoyl)homoserine lactone; 3-Oxo-N-(tetrahydro-2-oxo-3-furanyl)dodecanamide; 152833-54-0; CHEBI:29639; 3-oxo-N-(2-oxotetrahydrofuran-3-yl)dodecanamide; N-(3-ketododecanoyl)homoserine lactone; 3-oxo-C12-AHL; 3-oxo-N-(2-oxooxolan-3-yl)dodecanamide; AC1L2SRN; CHEMBL482476; SCHEMBL10076544; BCP19350; AN-30880; RT-014202; 3-(3-Oxododecanoylamino)tetrahydrofuran-2-one; C11840; Dodecanamide, 3-oxo-N-(tetrahydro-2-oxo-3-furanyl)-
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Amediplase Phase 3 [11]
Synonyms
Amediplase [INN]; Trans,trans-3,4:12,13-Tetrahydroxy-3,4,12,13-tetrahydro-dibenz(a,h)anthracene; (3S,4S,12S,13S)-3,4,12,13-tetrahydronaphtho[1,2-b]phenanthrene-3,4,12,13-tetrol
    Click to Show/Hide
MOA Activator
External Link
 Compound Name Upamostat Phase 2 [12]
Synonyms
WX-671
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 410 nM
External Link
 Compound Name Saruplase Phase 2 [13]
Synonyms
Rescupase; CG-4509; PUK, Grunenthal; Pro-urokinase, Grunenthal; Rscu-PA, Grunenthal
    Click to Show/Hide
MOA Activator
External Link
 Compound Name HTU-PA Phase 1/2 [14]
Synonyms
Human tissue urokinase type plasminogen activator, Global Biotech
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MOA Activator
External Link
 Compound Name PMID18163548C4 Clinical trial [15]
Synonyms
7IN; 1vja; AC1L9MNX; GTPL6545; BDBM50231520; US8476306, 6.12
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 20 nM
External Link
 Compound Name UK-356202 Clinical trial [16]
Synonyms
compound 13j [PMID: 15149680]; UK-356,202
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 37 nM
External Link
 Compound Name PAI-2 Discontinued in Phase 2 [17]
Synonyms
N-Butyryl-DL-homoserine lactone; N-butanoyl-lhomoserine lactone; N-(2-oxooxolan-3-yl)butanamide; N-(2-oxotetrahydrofuran-3-yl)butanamide; N-Butyrylhomoserine lactone; 98426-48-3; N-(2-Oxotetrahydro-3-furanyl)butanamide; AC1L9ENE; SCHEMBL787006; Homoserine lactone, N-butanoyl-; N-Butanoyl-DL-homoserine lactone; VFFNZZXXTGXBOG-UHFFFAOYSA-N; LMFA08030002; AN-38291; N-Butyryl-DL-homoserine lactone, &gt
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MOA Inhibitor
External Link
 Compound Name WX-UK1 Discontinued in Phase 1/2 [18]
Synonyms
UKI-1; UNII-00LOF6890B; CHEMBL107955; 00LOF6890B; 220355-63-5; Wx-uk1 free base; compound 2r-L; GTPL6498; BDBM23891; 3-amidinophenylalanine deriv., 35; ZINC4426028; AKOS030526723; CS-5726; HY-100415; 1-Piperazinecarboxylic acid, 4-((2S)-3-(3-(aminoiminomethyl)phenyl)-1-oxo-2-(((2,4,6-tris(1-methylethyl)phenyl)sulfonyl)amino)propyl)-, ethyl ester; ethyl 4-[(2S)-3-(3-carbamimidoylphenyl)-2-[[2,4,6-tri(propan-2-yl)phenyl]sulfonylamino]propanoyl]piperazine-1-carboxylate; ethyl 4-[(2S)-3-(3-carbamimidoylphenyl)-2-{[2,4,6
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 960 nM
External Link
 Compound Name B-428 Terminated [19]
MOA Inhibitor
Activity Ki = 79.43 nM
External Link
 Compound Name UPA-targeted oncolytic Sendai virus Investigative [8]
Synonyms
BioKnife; RSeV/Fct14(uPA2)dM; UPA-targeted oncolytic Sendai virus, DNAVEC
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name CRA_10655 Investigative [20]
Synonyms
AC1O4QGF
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MOA Inhibitor
Activity Ki = 220 nM
External Link
 Compound Name 5-Methylsulfanyl-thiophene-2-carboxamidine Investigative [21]
Synonyms
CHEMBL28890; 2-Thiophenecarboximidamide, 5-(methylthio)-; SCHEMBL5982145; AXSQTCBARFBKPH-UHFFFAOYSA-N; BDBM50099912; 5-methylthiothiophene-2-carboxamidine
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 6000 nM
External Link
 Compound Name ATN-658 Investigative [8]
Synonyms
ATN-291; ATN-292; HuATN-658; UPA mAbs, Attenuon; MAb (urokinase plasminogen activator system), Attenuon/Kyowa Hakko Kirin
    Click to Show/Hide
MOA Activator
External Link
 Compound Name (2R)-1-(2,6-dimethylphenoxy)propan-2-amine Investigative [20]
Synonyms
94991-73-8; (R)-1-(2,6-dimethylphenoxy)propan-2-amine; 2-Propanamine, 1-(2,6-dimethylphenoxy)-, (2R)-; CHEMBL147507; zlchem 1301; (R)-MEXILETINE; (R)-(-)-Mexiletine; AC1L47IL; SCHEMBL16082; BIDD:GT0498; ZINC20257; ZLE0076; DTXSID50241709; BDBM50135883; AKOS017529564; DB07129; AJ-08428; KB-209407; (2R)-1-(2,6-dimethylphenoxy)-2-propanamine; A821017; (R)-2-(2,6-Dimethyl-phenoxy)-1-methyl-ethylamine; UNII-1U511HHV4Z component VLPIATFUUWWMKC-SNVBAGLBSA-N
    Click to Show/Hide
MOA Inhibitor
Activity IC50 > 1000000 nM
External Link
 Compound Name B-623 Investigative [22]
Synonyms
149732-37-6
    Click to Show/Hide
MOA Modulator
Activity Ki = 530 nM
External Link
 Compound Name 4-chloro-1-guanidino-7-isoquinolinesulphonamide Investigative [23]
Synonyms
223671-02-1; 1-GUANIDINO-4-CHLORO-7-SULFAMOYL-ISOQUINOLINE; 2-(4-chloro-7-sulfamoylisoquinolin-1-yl)guanidine; CHEMBL227782; SCHEMBL6437735; CTK4E9305; BDBM16132; DTXSID90586545; FXVHAOFNNRNCRJ-UHFFFAOYSA-N; AKOS015966420; 1-guanidino-7-sulfonamidoisoquinoline 6; ACM223671021; 4-chloro-1-guanidino-7-sulphamoylisoquinoline
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 140 nM
External Link
 Compound Name 2-Amino-5-Hydroxy-Benzimidazole Investigative [24]
MOA Inhibitor
Activity IC50 = 200000 nM
External Link
 Compound Name 6-(N-Phenylcarbamyl)-2-Naphthalenecarboxamidine Investigative [24]
Synonyms
CHEMBL104937; 6-[(Z)-AMINO(IMINO)METHYL]-N-PHENYL-2-NAPHTHAMIDE; 6-carbamimidoyl-N-phenylnaphthalene-2-carboxamide; 1owe; uPa_7; AC1L9L6A; SCHEMBL4324160; ZINC2047486; BDBM50138670; 6-carbamimidoyl-N-phenyl-2-naphthamide; DB01977; 6-Carbamimidoyl-naphthalene-2-carboxylic acid phenylamide
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 630 nM
External Link
 Compound Name Thieno[2,3-B]Pyridine-2-Carboxamidine Investigative [20]
Synonyms
amino(thieno[2,3-b]pyridin-2-yl)methaniminium; [amino(thieno[2,3-b]pyridin-2-yl)methylidene]azanium; AC1L1KCT; BDBM14171; CTK7D1810; APC-7538
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Recombinant human pro-urokinase Investigative [8]
Synonyms
Recombinant human pro-urokinase (myocardial infarction)
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name N-(1-Adamantyl)-N'-(4-Guanidinobenzyl)Urea Investigative [24]
Synonyms
AGB; 1ejn; AC1L1HTN; SCHEMBL4328331; WX293T; SCHEMBL14524522; CTK7G4253; BDBM16176; WX-293T; DB03782; 3-adamantan-1-yl-1-[(4-carbamimidamidophenyl)methyl]urea; 3-(1-adamantyl)-1-[(4-carbamimidamidophenyl)methyl]urea; 3-(adamantan-1-yl)-1-[(4-carbamimidamidophenyl)methyl]urea; 1-(1-adamantyl)-3-[[4-(diaminomethylideneamino)phenyl]methyl]urea; 1-{4-[(diaminomethylidene)amino]benzyl}-3-tricyclo[3.3.1.13,7]dec-1-ylurea
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name (4-guanidino-benzyl)-carbamic acid benzyl ester Investigative [25]
Synonyms
CHEMBL391969
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 16000 nM
External Link
 Compound Name 1-[4-(2-oxo-2-phenylethyl)phenyl]guanidine Investigative [20]
Synonyms
SCHEMBL20553177; DB07122
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MOA Inhibitor
External Link
 Compound Name 4-methoxy-N'-(2-phenylacetyl)benzohydrazide Investigative [26]
Synonyms
4-methoxy-N'-(phenylacetyl)benzohydrazide; benzohydrazide, 15; AC1LEZHC; CHEMBL244921; ARONIS002261; BDBM23731; ZINC68809; KS-00003VJE; MolPort-000-681-545; STK056698; AKOS000492246; MCULE-6943344531; ST040019; 4-methoxy-N -(phenylacetyl)benzohydrazide; KB-115318; 4-methoxy-N''-(2-phenylacetyl)benzohydrazide
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MOA Inhibitor
Activity IC50 = 2500 nM
External Link
 Compound Name ATF-HI-8 Investigative [27]
Synonyms
urokinase/urinary trypsin inhibitor chimera, Nissin/Hamamatsu University
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MOA Modulator
External Link
 Compound Name 1-guanidino-7-isoquinolinesulphonamide Investigative [23]
Synonyms
SCHEMBL6436143; CHEMBL227583; 7-Isoquinolinesulfonamide, 1-[(aminoiminomethyl)amino]-; BDBM16130; NRVVFOKWKSWIIV-UHFFFAOYSA-N; 1-Guanidino-7-sulphamoylisoquinoline; 1-guanidino-7-sulfonamidoisoquinoline 4; 2-(7-sulfamoylisoquinolin-1-yl)guanidine
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 280 nM
External Link
 Compound Name CRA_8696 Investigative [20]
Synonyms
AC1O4QGN
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 8 nM
External Link
 Compound Name 1-guanidino-N-phenyl-7-isoquinolinesulphonamide Investigative [23]
Synonyms
SCHEMBL6435184; CHEMBL227781; BDBM16131; NNEJXIJKGKRBBF-UHFFFAOYSA-N; 1-guanidino-7-sulfonamidoisoquinoline 5; 1-guanidino-7-phenylsulphamoylisoquinoline
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 160 nM
External Link
 Compound Name (4-nitro-1H-pyrazol-1-yl)(o-tolyl)methanone Investigative [26]
Synonyms
BAS 02052986; AC1LDSC0; N-Benzoylpyrazole deriv., 20; CHEMBL244072; ZINC37170; BDBM23712; MolPort-001-971-782; AKOS000577347; 2-methylphenyl 4-nitropyrazolyl ketone; MCULE-4726161589; ST033205; (4-Nitro-pyrazol-1-yl)-o-tolyl-methanone; (2-methylphenyl)-(4-nitropyrazol-1-yl)methanone
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1300 nM
External Link
 Compound Name 4-iodobenzo[b]thiophene 2-carboxamidine Investigative [28]
Synonyms
amino(4-iodo-1-benzothiophen-2-yl)methaniminium; ESI; AC1L1C5C; CTK7C3490; BDBM14169; APC-6860; CRA-6860; DB03136; [amino-(4-iodo-1-benzothiophen-2-yl)methylidene]azanium
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name (4-nitro-1H-pyrazol-1-yl)(phenyl)methanone Investigative [26]
Synonyms
BAS 02052938; AC1LDSCA; N-Benzoylpyrazole deriv., 5; 4-nitropyrazolyl phenyl ketone; CHEMBL244908; 1-benzoyl-4-nitro-1H-pyrazole; ZINC37183; BDBM23703; AKOS000577075; (4-nitropyrazol-1-yl)-phenylmethanone; MCULE-3158742884; ST033219; (4-Nitro-pyrazol-1-yl)-phenyl-methanone; SR-01000312627
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MOA Inhibitor
Activity IC50 = 18200 nM
External Link
 Compound Name 2-nas-phe(3-am)-4-(2-guanidinoethyl)piperidine Investigative [29]
Synonyms
(S)-3-(3-(4-(2-GUANIDINOETHYL)PIPERIDIN-1-YL)-2-(NAPHTHALENE-2-SULFONAMIDO)-3-OXOPROPYL)BENZIMIDAMIDE; 2gv6; AC1OA9XW; CHEMBL210771; SCHEMBL12960819; BDBM23902; 3-amidinophenylalanine deriv., 8; 3-[(2S)-3-[4-(2-carbamimidamidoethyl)piperidin-1-yl]-2-(naphthalene-2-sulfonamido)-3-oxopropyl]benzene-1-carboximidamide; 3-{(2S)-3-[4-(2-carbamimidamidoethyl)piperidin-1-yl]-2-[(naphthalen-2-ylsulfonyl)amino]-3-oxopropyl}benzenecarboximidamide
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 1300 nM
External Link
 Compound Name (4-bromo-1H-pyrazol-1-yl)(p-tolyl)methanone Investigative [26]
Synonyms
AC1LDSCF; N-Benzoylpyrazole deriv., 7; CHEMBL244909; ZINC37188; BDBM23705; MolPort-002-174-815; AKOS000576906; 4-bromopyrazolyl 4-methylphenyl ketone; MCULE-8194486011; ST033225; AB00100488-01; (4-bromopyrazol-1-yl)-(4-methylphenyl)methanone; SR-01000521427; SR-01000521427-1
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1700 nM
External Link
 Compound Name Benzamidine Investigative [24]
Synonyms
Benzimidamide; Benzenecarboximidamide; 618-39-3; Phenylamidine; UNII-KUE3ZY3J1F; NSC 243704; CCRIS 2952; Benzamidine (Protonated); EINECS 210-546-3; KUE3ZY3J1F; CHEMBL20936; CHEBI:41033; PXXJHWLDUBFPOL-UHFFFAOYSA-N; BDN; 1oss; 2ast; 1bra; Benzenecarboxamidine; 1v2m; 1v2j; 1h4w; 1ce5; 1c5o; 2j9n; 1f5k; 1c5p; 1v2v; 1v2s; 1v2l; 1c5z; 1v2u; AC1L1DFX; Lopac-B-6506; ACMC-1B9LG; SCHEMBL9207; Lopac0_000203; MLS001066369; GTPL7566; AC1Q1U98; DTXSID8045012; 1670-14-0 (hydrochloride); ZINC36634; CTK2F5055; 1w80; 1j16; 1j15; MolPort-000-001-395
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 180000 nM
External Link
 Compound Name (3-nitro-1H-pyrazol-1-yl)(p-tolyl)methanone Investigative [26]
Synonyms
(4-methylphenyl)(3-nitro-1H-pyrazol-1-yl)methanone; AC1LF99H; N-Benzoylpyrazole deriv., 18; CHEMBL244939; ZINC78678; BDBM23710; A2012/0084499; MolPort-002-705-255; STK760276; AKOS001746005; 4-methylphenyl 3-nitropyrazolyl ketone; MCULE-9242110239; ST073763; (4-methylphenyl)-(3-nitropyrazol-1-yl)methanone; SR-01000524341; 1-[(4-methylphenyl)carbonyl]-3-nitro-1H-pyrazole
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MOA Inhibitor
Activity IC50 = 3100 nM
External Link
 Compound Name 1-benzoyl-N-phenyl-1H-pyrazole-3-carboxamide Investigative [26]
Synonyms
AC1LERN1; TimTec1_001906; Oprea1_174326; N-Benzoylpyrazole deriv., 6; CHEMBL388239; BDBM23704; MolPort-001-664-680; ZINC115253; HMS1539G14; STK398485; AKOS003748858; MCULE-1390939767; 1-benzoyl-N-phenylpyrazole-3-carboxamide; ST025783; N-phenyl[1-(phenylcarbonyl)pyrazol-3-yl]carboxamide
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1500 nM
External Link
 Compound Name (3,4-dichlorophenyl)(1H-pyrazol-1-yl)methanone Investigative [26]
Synonyms
AC1LDSBN; BAS 02052919; N-Benzoylpyrazole deriv., 8; CHEMBL244917; ZINC37156; BDBM23706; MolPort-001-906-669; 3,4-dichlorophenyl pyrazolyl ketone; STK044137; AKOS000577014; MCULE-6190861509; ST033189; (3,4-dichlorophenyl)-pyrazol-1-ylmethanone; (3,4-Dichloro-phenyl)-pyrazol-1-yl-methanone; 1-[(3,4-dichlorophenyl)carbonyl]-1H-pyrazole; SR-01000521426; SR-01000521426-1
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 2600 nM
External Link
 Compound Name 2-(2-Hydroxy-phenyl)-1H-indole-5-carboxamidine Investigative [30]
Synonyms
amino[2-(2-hydroxyphenyl)-1H-indol-5-yl]methaniminium; AC1L1BMI; BDBM13942; CTK8A0256; APC-8328; DB02463; [amino-[2-(2-hydroxyphenyl)-1H-indol-5-yl]methylidene]azanium
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Fucose Investigative [24]
Synonyms
L-galactomethylose; 6-Desoxygalactose; SCHEMBL13092958; AKOS030212707
    Click to Show/Hide
MOA Inhibitor
External Link
2B91: Colorectal cancer 25 Compound(s) Regulating the Disease Click to Show/Hide the Full List
 Compound Name Retifanlimab Approved [31]
Synonyms
INCMGA0012; Retifanlimab
    Click to Show/Hide
External Link
 Compound Name Aflibercept Approved [32]
Synonyms
Ziv-Aflibercept; Zaltrap (TN); VEGF Trap; VEGF Trap-Eye
    Click to Show/Hide
External Link
 Compound Name Regorafenib Approved [33]
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]
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 Compound Name Bevacizumab Approved [34]
Synonyms
Bevacizumab (ophthalmic slow-release tissue tablet)
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 Compound Name SYM-004 Phase 3 [34]
Synonyms
Chimeric IgG1 antibody 1024 (cancer), Symphogen; Chimeric IgG1 antibody 992 (cancer), Symphogen; Chimeric IgG1 antibodies992 + 1024 (cancer), Symphogen
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 Compound Name Bevacizumab + Erlotinib Phase 3 [35]
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 Compound Name CPI-613 Phase 3 [34]
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
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 Compound Name Bevacizumab Approved [32]
External Link
 Compound Name AlloStim Phase 2/3 [36]
Synonyms
AlloStim (TN)
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 Compound Name Sibrotuzumab Phase 2 [37]
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 Compound Name CV301 Phase 2 [38]
External Link
 Compound Name Efatutazone Phase 2 [39]
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
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 Compound Name LOR-2040 Phase 2 [40]
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 Compound Name RG7221 Phase 2 [41]
External Link
 Compound Name PEG-SN38 Phase 2 [42]
Synonyms
EZN-2208
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 Compound Name MEGF0444A Phase 2 [43]
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 Compound Name Encapsulated cell therapy Phase 1/2 [44]
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 Compound Name AB928 Phase 1/2 [45]
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 Compound Name MGD007 Phase 1 [41]
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 Compound Name BNC-101 Phase 1 [46]
External Link
 Compound Name Navicixizumab Phase 1 [34]
External Link
 Compound Name RG7160 Discontinued in Phase 2 [47]
External Link
 Compound Name Nimesulide Terminated [48]
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
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 Compound Name Saracatinib Phase 2 [49]
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 Compound Name G3139 + Irinotecan Investigative [50]
External Link
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