General Information of Drug (ID: DMEYMTX)

Drug Name
CP-461 Drug Info
Synonyms
CP-461; OSI 461; UNII-68OJX9I7DT; CP 461; 68OJX9I7DT; 1H-Indene-3-acetamide, 5-fluoro-2-methyl-N-(phenylmethyl)-1-(4-pyridinylmethylene)-, monohydrochloride, (1Z)-; 227619-96-7; N-benzyl-2-[(3Z)-6-fluoro-2-methyl-3-(pyridin-4-ylmethylidene)inden-1-yl]acetamide hydrochloride; AC1O6379; 279238-68-5
Indication
Disease Entry ICD 11 Status REF
Inflammatory bowel disease DD72 Phase 2 [1]
Cross-matching ID
PubChem CID
6445781
CAS Number
CAS 227619-96-7
TTD Drug ID
DMEYMTX

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Clinical Trial Drug(s)
Patented Agent(s)
Approved Drug(s)
Discontinued Drug(s)
Investigative Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tofisopam DMTGNWU Hyperuricaemia 5C55.Y Phase 2 [7]
ND7001 DMUBTC6 Mood disorder 6A60-6E23 Phase 1 [8]
Pyrido[3,2-e][1,2,4]triazolo[4,3-a]pyrazine derivative 1 DMC8935 N. A. N. A. Patented [9]
Pyrido[3,2-e][1,2,4]triazolo[4,3-a]pyrazine derivative 2 DM4CSBD N. A. N. A. Patented [9]
Imidazo[5,1-c]pyrido[2,3-e][1,2,4]triazine derivative 2 DMS3ROL N. A. N. A. Patented [9]
Triazolo-pyridine derivative 5 DM1R205 N. A. N. A. Patented [9]
PMID27321640-Compound-58 DM0NYK3 N. A. N. A. Patented [9]
Triazolo-pyridine derivative 4 DM5ZQKS N. A. N. A. Patented [9]
Imidazo[5,1-c]pyrido[2,3-e][1,2,4]triazine derivative 3 DMZ61T8 N. A. N. A. Patented [9]
Imidazo[5,1-c]pyrido[2,3-e][1,2,4]triazine derivative 4 DMKR5ZO N. A. N. A. Patented [9]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [10]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [11]
Gefitinib DM15F0X Colon adenocarcinoma Approved [12]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [13]
Colchicine DM2POTE Acute gout flare FA25.0 Approved [14]
Quercetin DM3NC4M Obesity 5B81 Approved [15]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [16]
Glucosamine DM4ZLFD Osteoarthritis FA00-FA05 Approved [17]
Vinblastine DM5TVS3 Advanced cancer 2A00-2F9Z Approved [14]
Ethacrynic acid DM60QMR Edema MG29 Approved [18]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Testosterone enanthate DMB6871 N. A. N. A. Approved [19]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [20]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [21]
Vorinostat DMWMPD4 Adult acute monocytic leukemia Approved [22]
Triclosan DMZUR4N Malaria 1F40-1F45 Approved [23]
Methamphetamine DMPM4SK Anxiety Approved [24]
EXISULIND DMBY56U Colorectal cancer 2B91.Z Phase 3 [4]
Benzo(a)pyrene DMN7J43 N. A. N. A. Phase 1 [25]
Geldanamycin DMS7TC5 Kidney cancer 2C90.0 Discontinued in Phase 2 [26]
(5-(1-benzyl-1H-indazol-3-yl)furan-2-yl)methanol DM15P2G Discovery agent N.A. Investigative [4]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Catenin beta-1 (CTNNB1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [11]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [27]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [28]
Quercetin DM3NC4M Obesity 5B81 Approved [29]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [30]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [31]
Aspirin DM672AH Acute coronary syndrome BA41 Approved [32]
Hydroquinone DM6AVR4 Melasma ED60.1 Approved [33]
Testosterone DM7HUNW Hot flushes GA30 Approved [34]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [35]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [36]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [37]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [38]
Gefitinib DM15F0X Colon adenocarcinoma Approved [39]
Talazoparib DM1KS78 Breast cancer 2C60-2C65 Approved [40]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [41]
Etretinate DM2CZFA Keratosis ED56 Approved [42]
Prednisone DM2HG4X Acute asthma CA23 Approved [43]
Ciprofloxacin XR DM2NLS9 Acute gonococcal cervicitis Approved [44]
Colchicine DM2POTE Acute gout flare FA25.0 Approved [45]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Phosphodiesterase 2A (PDE2A) TTJGW1Z PDE2A_HUMAN Inhibitor [2]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Catenin beta-1 (CTNNB1) OTZ932A3 CTNB1_HUMAN Gene/Protein Processing [3]
cGMP-dependent protein kinase 1 (PRKG1) OTPAS4LF KGP1_HUMAN Gene/Protein Processing [4]
Cyclin-dependent kinase inhibitor 1 (CDKN1A) OTQWHCZE CDN1A_HUMAN Gene/Protein Processing [5]
Mitogen-activated protein kinase 8 (MAPK8) OTEREYS5 MK08_HUMAN Gene/Protein Processing [6]
Vasodilator-stimulated phosphoprotein OTFC3010 VASP_HUMAN Post-Translational Modifications [5]

References

1 ClinicalTrials.gov (NCT00060710) CP-461 in the Treatment of Patients With Advanced Melanoma. U.S. National Institutes of Health.
2 Sulindac and its derivatives: a novel class of anticancer agents. Curr Opin Investig Drugs. 2001 May;2(5):677-83.
3 Pro-apoptotic actions of exisulind and CP461 in SW480 colon tumor cells involve beta-catenin and cyclin D1 down-regulation. Biochem Pharmacol. 2002 Nov 1;64(9):1325-36. doi: 10.1016/s0006-2952(02)01345-x.
4 Cyclic GMP-dependent protein kinase activation and induction by exisulind and CP461 in colon tumor cells. J Pharmacol Exp Ther. 2001 Nov;299(2):583-92.
5 Synergistic effects of acyclic retinoid and OSI-461 on growth inhibition and gene expression in human hepatoma cells. Clin Cancer Res. 2004 Oct 1;10(19):6710-21. doi: 10.1158/1078-0432.CCR-04-0659.
6 Cyclic GMP mediates apoptosis induced by sulindac derivatives via activation of c-Jun NH2-terminal kinase 1. Clin Cancer Res. 2000 Oct;6(10):4136-41.
7 The atypical anxiolytic drug, tofisopam, selectively blocks phosphodiesterase isoenzymes and is active in the mouse model of negative symptoms of psychosis. J Neural Transm (Vienna). 2010 Nov;117(11):1319-25.
8 Phosphodiesterase 2 inhibitors promote axonal outgrowth in organotypic slice co-cultures. Neurosignals. 2013;21(3-4):197-212.
9 Towards selective phosphodiesterase 2A (PDE2A) inhibitors: a patent review (2010 - present).Expert Opin Ther Pat. 2016 Aug;26(8):933-46.
10 Cisplatin induces autophagy to enhance hepatitis B virus replication via activation of ROS/JNK and inhibition of the Akt/mTOR pathway. Free Radic Biol Med. 2019 Feb 1;131:225-236. doi: 10.1016/j.freeradbiomed.2018.12.008. Epub 2018 Dec 11.
11 Inhibition of autophagic flux differently modulates cannabidiol-induced death in 2D and 3D glioblastoma cell cultures. Sci Rep. 2020 Feb 14;10(1):2687. doi: 10.1038/s41598-020-59468-4.
12 Frankincense myrrh attenuates hepatocellular carcinoma by regulating tumor blood vessel development through multiple epidermal growth factor receptor-mediated signaling pathways. World J Gastrointest Oncol. 2022 Feb 15;14(2):450-477. doi: 10.4251/wjgo.v14.i2.450.
13 Neuroprotective effects of glucomoringin-isothiocyanate against H(2)O(2)-Induced cytotoxicity in neuroblastoma (SH-SY5Y) cells. Neurotoxicology. 2019 Dec;75:89-104. doi: 10.1016/j.neuro.2019.09.008. Epub 2019 Sep 12.
14 Nocodazole-induced p53-dependent c-Jun N-terminal kinase activation reduces apoptosis in human colon carcinoma HCT116 cells. J Biol Chem. 2002 Nov 15;277(46):43648-58. doi: 10.1074/jbc.M203214200. Epub 2002 Sep 6.
15 Quercetin potentiates apoptosis by inhibiting nuclear factor-kappaB signaling in H460 lung cancer cells. Biol Pharm Bull. 2013;36(6):944-51. doi: 10.1248/bpb.b12-01004.
16 Lon protease and eiF2 are involved in acute, but not prolonged, antiretroviral induced stress response in HepG2 cells. Chem Biol Interact. 2016 May 25;252:82-6. doi: 10.1016/j.cbi.2016.03.021. Epub 2016 Apr 1.
17 Disease-modifying effects of glucosamine HCl involving regulation of metalloproteinases and chemokines activated by interleukin-1beta in human primary synovial fibroblasts. J Cell Biochem. 2008 May 1;104(1):38-50. doi: 10.1002/jcb.21597.
18 Characterization of cell death induced by ethacrynic acid in a human colon cancer cell line DLD-1 and suppression by N-acetyl-L-cysteine. Cancer Sci. 2003 Oct;94(10):886-93.
19 Transcriptional profiling of testosterone-regulated genes in the skeletal muscle of human immunodeficiency virus-infected men experiencing weight loss. J Clin Endocrinol Metab. 2007 Jul;92(7):2793-802. doi: 10.1210/jc.2006-2722. Epub 2007 Apr 17.
20 Human embryonic stem cell-derived test systems for developmental neurotoxicity: a transcriptomics approach. Arch Toxicol. 2013 Jan;87(1):123-43.
21 Bringing in vitro analysis closer to in vivo: studying doxorubicin toxicity and associated mechanisms in 3D human microtissues with PBPK-based dose modelling. Toxicol Lett. 2018 Sep 15;294:184-192.
22 Definition of transcriptome-based indices for quantitative characterization of chemically disturbed stem cell development: introduction of the STOP-Toxukn and STOP-Toxukk tests. Arch Toxicol. 2017 Feb;91(2):839-864.
23 Transcriptome and DNA methylome dynamics during triclosan-induced cardiomyocyte differentiation toxicity. Stem Cells Int. 2018 Oct 29;2018:8608327.
24 Genome-wide association for methamphetamine dependence: convergent results from 2 samples. Arch Gen Psychiatry. 2008 Mar;65(3):345-55. doi: 10.1001/archpsyc.65.3.345.
25 Air pollution and DNA methylation alterations in lung cancer: A systematic and comparative study. Oncotarget. 2017 Jan 3;8(1):1369-1391. doi: 10.18632/oncotarget.13622.
26 Identification of transcriptome signatures and biomarkers specific for potential developmental toxicants inhibiting human neural crest cell migration. Arch Toxicol. 2016 Jan;90(1):159-80.
27 Microarray analysis of H2O2-, HNE-, or tBH-treated ARPE-19 cells. Free Radic Biol Med. 2002 Nov 15;33(10):1419-32.
28 Sulindac suppresses beta-catenin expression in human cancer cells. Eur J Pharmacol. 2008 Mar 31;583(1):26-31. doi: 10.1016/j.ejphar.2007.12.034. Epub 2008 Feb 5.
29 Multifaceted preventive effects of single agent quercetin on a human prostate adenocarcinoma cell line (PC-3): implications for nutritional transcriptomics and multi-target therapy. Med Oncol. 2011 Dec;28(4):1395-404. doi: 10.1007/s12032-010-9603-3. Epub 2010 Jul 2.
30 Multifaceted suppression of aggressive behavior of thyroid carcinoma by all-trans retinoic acid induced re-differentiation. Mol Cell Endocrinol. 2012 Jan 2;348(1):260-9. doi: 10.1016/j.mce.2011.09.002. Epub 2011 Sep 6.
31 Arsenic trioxide and 2-methoxyestradiol reduce beta-catenin accumulation after proteasome inhibition and enhance the sensitivity of myeloma cells to Bortezomib. Leuk Res. 2008 Nov;32(11):1674-83. doi: 10.1016/j.leukres.2008.03.039. Epub 2008 May 15.
32 Effect of aspirin on the Wnt/beta-catenin pathway is mediated via protein phosphatase 2A. Oncogene. 2006 Oct 19;25(49):6447-56. doi: 10.1038/sj.onc.1209658. Epub 2006 Jul 31.
33 Benzene metabolite hydroquinone induces apoptosis of bone marrow mononuclear cells through inhibition of -catenin signaling. Toxicol In Vitro. 2018 Feb;46:361-369. doi: 10.1016/j.tiv.2017.08.018. Epub 2017 Sep 5.
34 Anti-androgen 2-hydroxyflutamide modulates cadherin, catenin and androgen receptor phosphorylation in androgen-sensitive LNCaP and androgen-independent PC3 prostate cancer cell lines acting via PI3K/Akt and MAPK/ERK1/2 pathways. Toxicol In Vitro. 2017 Apr;40:324-335. doi: 10.1016/j.tiv.2017.01.019. Epub 2017 Feb 2.
35 Anthelmintic Niclosamide Disrupts the Interplay of p65 and FOXM1/-catenin and Eradicates Leukemia Stem Cells in Chronic Myelogenous Leukemia. Clin Cancer Res. 2017 Feb 1;23(3):789-803. doi: 10.1158/1078-0432.CCR-16-0226. Epub 2016 Aug 4.
36 Zidovudine induces S-phase arrest and cell cycle gene expression changes in human cells. Mutagenesis. 2005 Mar;20(2):139-46. doi: 10.1093/mutage/gei019. Epub 2005 Mar 22.
37 Cannabidiol Activates Neuronal Precursor Genes in Human Gingival Mesenchymal Stromal Cells. J Cell Biochem. 2017 Jun;118(6):1531-1546. doi: 10.1002/jcb.25815. Epub 2016 Dec 29.
38 Gene expression profiles with activation of the estrogen receptor alpha-selective estrogen receptor modulator complex in breast cancer cells expressing wild-type estrogen receptor. Cancer Res. 2002 Aug 1;62(15):4419-26.
39 Leptomycin B reduces primary and acquired resistance of gefitinib in lung cancer cells. Toxicol Appl Pharmacol. 2017 Nov 15;335:16-27. doi: 10.1016/j.taap.2017.09.017. Epub 2017 Sep 21.
40 BMN 673 (talazoparib): A potent PARP inhibitor for triple negative breast cancer with different genetic profile. J Biochem Mol Toxicol. 2019 May;33(5):e22286. doi: 10.1002/jbt.22286. Epub 2019 Jan 23.
41 Gene expression after treatment with hydrogen peroxide, menadione, or t-butyl hydroperoxide in breast cancer cells. Cancer Res. 2002 Nov 1;62(21):6246-54.
42 Bexarotene activates the p53/p73 pathway in human cutaneous T-cell lymphoma. Br J Dermatol. 2009 Mar;160(3):519-26. doi: 10.1111/j.1365-2133.2008.08931.x. Epub 2008 Nov 25.
43 Glucocorticoids induce G1 arrest of lymphoblastic cells through retinoblastoma protein Rb1 dephosphorylation in childhood acute lymphoblastic leukemia in vivo. Cancer Biol Ther. 2004 May;3(5):470-6. doi: 10.4161/cbt.3.5.838. Epub 2004 May 9.
44 Ciprofloxacin mediated cell growth inhibition, S/G2-M cell cycle arrest, and apoptosis in a human transitional cell carcinoma of the bladder cell line. Clin Cancer Res. 2000 Mar;6(3):891-900.
45 Utilization of CDKN1A/p21 gene for class discrimination of DNA damage-induced clastogenicity. Toxicology. 2014 Jan 6;315:8-16. doi: 10.1016/j.tox.2013.10.009. Epub 2013 Nov 6.