General Information of Drug (ID: DMDLER8)

Drug Name
DEBROMOHYMENIALDISINE Drug Info
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
135451156
CAS Number
CAS 125118-55-0
TTD Drug ID
DMDLER8

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Clinical Trial Drug(s)
Patented Agent(s)
Discontinued Drug(s)
Investigative Drug(s)
Preclinical Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
E7850 DM8K5IF Solid tumour/cancer 2A00-2F9Z Phase 2 [3]
PMID27410995-Compound-Figure3j DMJRZLB N. A. N. A. Patented [4]
XL844 DMHTG38 Solid tumour/cancer 2A00-2F9Z Discontinued in Phase 1 [5]
PMID22564207C25b DMBMYKQ Discovery agent N.A. Investigative [6]
2-(4-Phenoxy-phenyl)-1H-benzoimidazol-5-ylamine DMSPOAT Discovery agent N.A. Investigative [7]
PV-1019 DMRI1LF Solid tumour/cancer 2A00-2F9Z Investigative [8]
5-Nitro-2-(4-phenoxy-phenyl)-1H-benzoimidazole DM26MIC Discovery agent N.A. Investigative [7]
CCT-241533 DMZXFT9 Solid tumour/cancer 2A00-2F9Z Investigative [9]
Chk2 inhibitor II DMNSPFG Discovery agent N.A. Investigative [10]
⏷ Show the Full List of 9 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Selumetinib DMC7W6R Neurofibromatosis type 1 LD2D.10 Phase 3 [11]
Diamidothiazole derivative 1 DM02V5Q N. A. N. A. Patented [12]
Pyridic ketone derivative 1 DM3GU7K N. A. N. A. Patented [13]
RDEA-436 DM0ILRU Solid tumour/cancer 2A00-2F9Z Discontinued in Phase 1 [14]
4,5,6,7-tetrabromo-1H-benzo[d][1,2,3]triazole DMN9YOB Discovery agent N.A. Investigative [15]
REVERSINE DMWDNOK Discovery agent N.A. Investigative [16]
OROIDIN DMA2DQT Discovery agent N.A. Investigative [2]
PD98059 DMZC90M Cardiac arrest MC82 Investigative [17]
4,5-Dibromo-1H-pyrrole-2-carboxylic acid amide DMDM9UV Discovery agent N.A. Investigative [2]
5-phenylamino-4-cyano-3-hydroxy-isothiazole DMX6R0H Discovery agent N.A. Investigative [18]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
MLN2480 DMBR8NF Solid tumour/cancer 2A00-2F9Z Phase 2 [19]
RG7304 DMGFAVQ Solid tumour/cancer 2A00-2F9Z Phase 1 [20]
SPN-803 DM8O2AQ Parkinson disease 8A00.0 Phase 1 [19]
LXH254 DMQE9PS Non-small-cell lung cancer 2C25.Y Phase 1 [11]
ICo-007 DM79W8K Diabetic macular edema 9B71.02 Phase 1 [21]
LErafAON DMNHPOT Solid tumour/cancer 2A00-2F9Z Phase 1 [22]
ZM-336372 DMD5JYQ Discovery agent N.A. Investigative [23]
6-[(E)-2-(4-Fluoro-phenyl)-vinyl]-9H-purine DMDNG8F Discovery agent N.A. Investigative [24]
PLX-ORI3 DMZG1L5 Solid tumour/cancer 2A00-2F9Z Investigative [19]
6-Benzylsulfanyl-9H-purine DMI7FNZ Discovery agent N.A. Investigative [24]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
BVD-523 DMNB4XK Melanoma 2C30 Phase 2 [25]
HH2710 DM0C5MV Solid tumour/cancer 2A00-2F9Z Phase 1/2 [26]
ASTX029 DMVZXIA Solid tumour/cancer 2A00-2F9Z Phase 1/2 [27]
VAN-10-4-eluting stent DM3ZW6A Artery stenosis BD52 Phase 1 [28]
GDC-0994 DMFC2OY Solid tumour/cancer 2A00-2F9Z Phase 1 [29]
JSI-1187 DMVJWBS Solid tumour/cancer 2A00-2F9Z Phase 1 [30]
LY3214996 DMFDAY7 Solid tumour/cancer 2A00-2F9Z Phase 1 [11]
CHIR-99021 DMB8MNU Allergic inflammation 4A80-4A85 Patented [31]
COR-D DMLXMCB T-cell leukaemia 2A90 Preclinical [32]
SB220025 DMSBUET Arthritis FA20 Terminated [33]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting Checkpoint kinase-1 (CHK1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
LY2603618 DMCXRZF Pancreatic cancer 2C10 Phase 2 [34]
UCN-01 DMUNJZB Non-small-cell lung cancer 2C25.Y Phase 2 [35]
SCH-900776 DM67EMK Solid tumour/cancer 2A00-2F9Z Phase 2 [36]
LY2606368 DM4XMF7 Ovarian cancer 2C73 Phase 2 [11]
LY2880070 DMADEHZ Solid tumour/cancer 2A00-2F9Z Phase 1/2 [37]
RG7741 DMK6P9J Lymphoma 2A80-2A86 Phase 1 [38]
GDC-0425 DMDZ26X Lymphoma 2A80-2A86 Phase 1 [39]
AZD7762 DM1FW0C Solid tumour/cancer 2A00-2F9Z Phase 1 [40]
MK-8776 DMAS1RB Hodgkin lymphoma 2B30 Phase 1 [41]
Diamidothiazole derivative 1 DM02V5Q N. A. N. A. Patented [12]
⏷ 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
Checkpoint kinase-1 (CHK1) TTTU902 CHK1_HUMAN Inhibitor [1]
ERK activator kinase 1 (MEK1) TTIDAPM MP2K1_HUMAN Inhibitor [2]
Extracellular signal-regulated kinase 2 (ERK2) TT4TQBX MK01_HUMAN Inhibitor [1]
Raf messenger RNA (Raf mRNA) TTAN5W2 RAF1_HUMAN Inhibitor [2]
Serine/threonine-protein kinase Chk2 (RAD53) TT9ABMF CHK2_HUMAN Inhibitor [1]

References

1 Potent inhibition of checkpoint kinase activity by a hymenialdisine-derived indoloazepine. Bioorg Med Chem Lett. 2004 Aug 16;14(16):4319-21.
2 Aldisine alkaloids from the Philippine sponge Stylissa massa are potent inhibitors of mitogen-activated protein kinase kinase-1 (MEK-1). J Med Chem. 2002 Jan 17;45(2):529-32.
3 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: 1988).
4 Ribosomal S6 kinase (RSK) modulators: a patent review.Expert Opin Ther Pat. 2016 Sep;26(9):1061-78.
5 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
6 Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase. J Med Chem. 2012 May 24;55(10):4580-93.
7 Checkpoint kinase inhibitors: SAR and radioprotective properties of a series of 2-arylbenzimidazoles. J Med Chem. 2005 Mar 24;48(6):1873-85.
8 Cellular inhibition of checkpoint kinase 2 (Chk2) and potentiation of camptothecins and radiation by the novel Chk2 inhibitor PV1019 [7-nitro-1H-indole-2-carboxylic acid {4-[1-(guanidinohydrazone)-ethyl]-phenyl}-amide]. J Pharmacol Exp Ther. 2009 Dec;331(3):816-26.
9 CCT241533 Is a Potent and Selective Inhibitor of CHK2 that Potentiates the Cytotoxicity of PARP Inhibitors. Cancer Res. 2011 Jan 15;71(2):463-72.
10 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.
11 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
12 Cyclin-dependent kinase inhibitors for cancer therapy: a patent review (2009 - 2014).Expert Opin Ther Pat. 2015;25(9):953-70.
13 MEK inhibitors in oncology: a patent review (2015-Present).Expert Opin Ther Pat. 2017 Aug;27(8):887-906.
14 Clinical pipeline report, company report or official report of MedKoo Biosciences.
15 Optimization of protein kinase CK2 inhibitors derived from 4,5,6,7-tetrabromobenzimidazole. J Med Chem. 2004 Dec 2;47(25):6239-47.
16 Reversine increases the plasticity of lineage-committed mammalian cells. Proc Natl Acad Sci U S A. 2007 Jun 19;104(25):10482-7.
17 The MEK1 inhibitor PD98059 sensitizes C8161 melanoma cells to cisplatin-induced apoptosis. Melanoma Res. 2001 Feb;11(1):11-9.
18 Discovery of 3-hydroxy-4-carboxyalkylamidino-5-arylamino-isothiazoles as potent MEK1 inhibitors. Bioorg Med Chem Lett. 2006 Aug 1;16(15):3975-80.
19 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: 2184).
20 Clinical pipeline report, company report or official report of Roche.
21 Clinical pipeline report, company report or official report of ISIS Pharmaceuticals (2009).
22 Combination with liposome-entrapped, ends-modified raf antisense oligonucleotide (LErafAON) improves the anti-tumor efficacies of cisplatin, epirubicin, mitoxantrone, docetaxel and gemcitabine. Anticancer Drugs. 2004 Mar;15(3):243-53.
23 The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315.
24 Synthesis and biological testing of purine derivatives as potential ATP-competitive kinase inhibitors. J Med Chem. 2005 Feb 10;48(3):710-22.
25 DOI: 10.1158/1538-7445.AM2015-4693
26 Clinical pipeline report, company report or official report of HaiHe Biopharma.
27 Clinical pipeline report, company report or official report of Astex Pharmaceuticals.
28 WO patent application no. 2013,1850,32, Nanotherapeutics for drug targeting.
29 ERK Mutations Confer Resistance to Mitogen-Activated Protein Kinase Pathway Inhibitors
30 National Cancer Institute Drug Dictionary (drug name JSI1187).
31 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.
32 Corchorusin-D directed apoptosis of K562 cells occurs through activation of mitochondrial and death receptor pathways and suppression of AKT/PKB pathway. Cell Physiol Biochem. 2012;30(4):915-26.
33 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
34 Characterization and preclinical development of LY2603618: a selective and potent Chk1 inhibitor. Invest New Drugs. 2014 Apr;32(2):213-26.
35 Characterization of an inhibitory dynamic pharmacophore for the ERCC1-XPA interaction using a combined molecular dynamics and virtual screening app... J Mol Graph Model. 2009 Sep;28(2):113-30.
36 Targeting the replication checkpoint using SCH 900776, a potent and functionally selective CHK1 inhibitor identified via high content screening. Mol Cancer Ther. 2011 Apr;10(4):591-602.
37 A phase Ib study of oral Chk1 inhibitor LY2880070 in combination with gemcitabine in patients with advanced or metastatic cancer. Journal of Clinical Oncology 38, no. 15_suppl (May 20, 2020) 3581-3581.
38 National Cancer Institute Drug Dictionary (drug id 730054).
39 Quantitative assessment of BCL-2:BIM complexes as a pharmacodynamic marker for venetoclax (ABT-199).
40 Clinical pipeline report, company report or official report of AstraZeneca (2009).
41 Chk1 Inhibitor MK-8776 Restores the Sensitivity of Chemotherapeutics in P-glycoprotein Overexpressing Cancer Cells. Int J Mol Sci. 2019 Aug 22;20(17):4095.