General Information of Drug (ID: DM051PI)

Drug Name
FR-180204 Drug Info
Synonyms
865362-74-9; FR 180204; FR180204; FR-180204; ERK Inhibitor II, FR180204; 5-(2-Phenyl-pyrazolo[1,5-a]pyridin-3-yl)-1H-pyrazolo[3,4-c]pyridazin-3-ylamine; CHEMBL259551; 5-(2-PHENYLPYRAZOLO[1,5-A]PYRIDIN-3-YL)-1H-PYRAZOLO[3,4-C]PYRIDAZIN-3-AMINE; C18H13N7; 5-{2-phenylpyrazolo[1,5-a]pyridin-3-yl}-1H-pyrazolo[3,4-c]pyridazin-3-amine; 5-{2-phenylpyrazolo[1,5-a]pyridin-3-yl}-2H-pyrazolo[3,4-c]pyridazin-3-amine; 5-(2-phenylpyrazolo[1,5-a]pyridin-3-yl)-2H-pyrazolo[3,4-c]pyridazin-3-amine; ERK inhibitor II; MLS002607685
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
11493598
ChEBI ID
CHEBI:91383
CAS Number
CAS 865362-74-9
TTD Drug ID
DM051PI

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Clinical Trial Drug(s)
Patented Agent(s)
Preclinical Drug(s)
Discontinued Drug(s)
Approved Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
BVD-523 DMNB4XK Melanoma 2C30 Phase 2 [4]
HH2710 DM0C5MV Solid tumour/cancer 2A00-2F9Z Phase 1/2 [5]
ASTX029 DMVZXIA Solid tumour/cancer 2A00-2F9Z Phase 1/2 [6]
VAN-10-4-eluting stent DM3ZW6A Artery stenosis BD52 Phase 1 [7]
GDC-0994 DMFC2OY Solid tumour/cancer 2A00-2F9Z Phase 1 [8]
JSI-1187 DMVJWBS Solid tumour/cancer 2A00-2F9Z Phase 1 [9]
LY3214996 DMFDAY7 Solid tumour/cancer 2A00-2F9Z Phase 1 [10]
CHIR-99021 DMB8MNU Allergic inflammation 4A80-4A85 Patented [11]
COR-D DMLXMCB T-cell leukaemia 2A90 Preclinical [12]
SB220025 DMSBUET Arthritis FA20 Terminated [13]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ethanol DMDRQZU Chronic pain MG30 Approved [14]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [15]
Carvedilol DMHTEAO Chronic heart failure BD1Z Approved [16]
Paclitaxel DMLB81S Breast carcinoma Approved [17]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [18]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [19]
Urokinase DM0GOUD Myocardial infarction BA41-BA43 Approved [20]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [21]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [22]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [23]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fructose DM43AN2 Vomiting MD90 Approved [20]
Aprepitant DM053KT Depression 6A70-6A7Z Approved [24]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [21]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [25]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [26]
Colchicine DM2POTE Acute gout flare FA25.0 Approved [27]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [28]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [29]
Deoxycholic acid DM3GYAL Subcutaneous fat disorder EF02 Approved [30]
Quercetin DM3NC4M Obesity 5B81 Approved [31]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [19]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [15]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [32]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [22]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [23]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [33]
Secobarbital DM14RF5 Epilepsy 8A60-8A68 Approved [34]
Gefitinib DM15F0X Colon adenocarcinoma Approved [35]
Fexofenadine DM17ONX Allergic rhinitis CA08.0 Approved [36]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [37]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dexamethasone DMMWZET Acute adrenal insufficiency Approved [20]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [21]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [38]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [39]
Trametinib DM2JGQ3 Melanoma 2C30 Approved [40]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [41]
Methotrexate DM2TEOL Anterior urethra cancer Approved [42]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [43]
Cladribine DM3JDRP Hairy cell leukaemia 2A82.2 Approved [44]
Quercetin DM3NC4M Obesity 5B81 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
Extracellular signal-regulated kinase 2 (ERK2) TT4TQBX MK01_HUMAN Inhibitor [2]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Mitogen-activated protein kinase 1 (MAPK1) OTH85PI5 MK01_HUMAN Post-Translational Modifications [3]
Mitogen-activated protein kinase 3 (MAPK3) OTCYKGKO MK03_HUMAN Post-Translational Modifications [3]
NF-kappa-B inhibitor alpha (NFKBIA) OTFT924M IKBA_HUMAN Gene/Protein Processing [3]
Signal transducer and activator of transcription 3 (STAT3) OTAAGKYZ STAT3_HUMAN Post-Translational Modifications [3]

References

1 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. (Ligand id: 5966).
2 Crystal structure of human ERK2 complexed with a pyrazolo[3,4-c]pyridazine derivative. Bioorg Med Chem Lett. 2006 Jan 1;16(1):55-8.
3 Molecular mechanisms of quinalizarin induces apoptosis and G0/G1 cell cycle of human esophageal cancer HCE-4 cells depends on MAPK, STAT3, and NF-B signaling pathways. Environ Toxicol. 2021 Feb;36(2):276-286. doi: 10.1002/tox.23033. Epub 2020 Oct 8.
4 DOI: 10.1158/1538-7445.AM2015-4693
5 Clinical pipeline report, company report or official report of HaiHe Biopharma.
6 Clinical pipeline report, company report or official report of Astex Pharmaceuticals.
7 WO patent application no. 2013,1850,32, Nanotherapeutics for drug targeting.
8 ERK Mutations Confer Resistance to Mitogen-Activated Protein Kinase Pathway Inhibitors
9 National Cancer Institute Drug Dictionary (drug name JSI1187).
10 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
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.
12 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.
13 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
14 Downregulation of mitogen-activated protein kinases (MAPKs) in chronic ethanol-induced fatty liver. Toxicol Mech Methods. 2020 Jul;30(6):407-416. doi: 10.1080/15376516.2020.1747126. Epub 2020 Apr 1.
15 Progesterone increases csk homologous kinase in HMC-1560 human mast cells and reduces cell proliferation. J Cell Biochem. 2007 Dec 1;102(5):1271-80. doi: 10.1002/jcb.21357.
16 A unique mechanism of beta-blocker action: carvedilol stimulates beta-arrestin signaling. Proc Natl Acad Sci U S A. 2007 Oct 16;104(42):16657-62. doi: 10.1073/pnas.0707936104. Epub 2007 Oct 9.
17 The stent-eluting drugs sirolimus and paclitaxel suppress healing of the endothelium by induction of autophagy. Am J Pathol. 2009 Nov;175(5):2226-34.
18 Modulation of apoptosis in HaCaT keratinocytes via differential regulation of ERK signaling pathway by flavonoids. J Biol Chem. 2005 Sep 9;280(36):31498-507. doi: 10.1074/jbc.M505537200. Epub 2005 Jul 13.
19 Treatment with anticancer agents induces dysregulation of specific Wnt signaling pathways in human ovarian luteinized granulosa cells in vitro. Toxicol Sci. 2013 Nov;136(1):183-92. doi: 10.1093/toxsci/kft175. Epub 2013 Aug 16.
20 ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
21 Cannabidiol Modulates the Immunophenotype and Inhibits the Activation of the Inflammasome in Human Gingival Mesenchymal Stem Cells. Front Physiol. 2016 Nov 24;7:559. doi: 10.3389/fphys.2016.00559. eCollection 2016.
22 Sertraline, an antidepressant, induces apoptosis in hepatic cells through the mitogen-activated protein kinase pathway. Toxicol Sci. 2014 Feb;137(2):404-15. doi: 10.1093/toxsci/kft254. Epub 2013 Nov 5.
23 Growth stimulation of human pulmonary adenocarcinoma cells and small airway epithelial cells by beta-carotene via activation of cAMP, PKA, CREB and ERK1/2. Int J Cancer. 2006 Mar 15;118(6):1370-80. doi: 10.1002/ijc.21537.
24 Neurokinin-1 receptor (NK1R) inhibition sensitizes APL cells to anti-tumor effect of arsenic trioxide via restriction of NF-B axis: Shedding new light on resistance to Aprepitant. Int J Biochem Cell Biol. 2018 Oct;103:105-114. doi: 10.1016/j.biocel.2018.08.010. Epub 2018 Aug 23.
25 ERE-independent ERalpha target genes differentially expressed in human breast tumors. Mol Cell Endocrinol. 2005 Dec 21;245(1-2):53-9. doi: 10.1016/j.mce.2005.10.003. Epub 2005 Nov 17.
26 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.
27 Microtubules are required for NF-kappaB nuclear translocation in neuroblastoma IMR-32 cells: modulation by zinc. J Neurochem. 2006 Oct;99(2):402-15. doi: 10.1111/j.1471-4159.2006.04005.x.
28 Protein phosphatase 2A interacts with and directly dephosphorylates RelA. J Biol Chem. 2001 Dec 21;276(51):47828-33. doi: 10.1074/jbc.M106103200. Epub 2001 Oct 8.
29 Activation of nuclear factor-kappa B pathway by simvastatin and RhoA silencing increases doxorubicin cytotoxicity in human colon cancer HT29 cells. Mol Pharmacol. 2008 Aug;74(2):476-84.
30 Prevention of deoxycholate-induced gastric apoptosis by aspirin: roles of NF-kappaB and PKC signaling. J Surg Res. 2008 Mar;145(1):66-73. doi: 10.1016/j.jss.2007.04.039. Epub 2007 Jul 20.
31 Comparison of phenotypic and transcriptomic effects of false-positive genotoxins, true genotoxins and non-genotoxins using HepG2 cells. Mutagenesis. 2011 Sep;26(5):593-604.
32 Cannabidiol upregulates melanogenesis through CB1 dependent pathway by activating p38 MAPK and p42/44 MAPK. Chem Biol Interact. 2017 Aug 1;273:107-114. doi: 10.1016/j.cbi.2017.06.005. Epub 2017 Jun 7.
33 Estrogen and pure antiestrogen fulvestrant (ICI 182 780) augment cell-matrigel adhesion of MCF-7 breast cancer cells through a novel G protein coupled estrogen receptor (GPR30)-to-calpain signaling axis. Toxicol Appl Pharmacol. 2014 Mar 1;275(2):176-81. doi: 10.1016/j.taap.2014.01.005. Epub 2014 Jan 17.
34 Inhibition of activator protein 1 by barbiturates is mediated by differential effects on mitogen-activated protein kinases and the small G proteins ras and rac-1. J Pharmacol Exp Ther. 2004 Dec;311(3):1232-40. doi: 10.1124/jpet.104.071332. Epub 2004 Jul 19.
35 Growth of hormone-dependent MCF-7 breast cancer cells is promoted by constitutive caveolin-1 whose expression is lost in an EGF-R-mediated manner during development of tamoxifen resistance. Breast Cancer Res Treat. 2010 Feb;119(3):575-91. doi: 10.1007/s10549-009-0355-8. Epub 2009 Mar 15.
36 Effect of histamine H1 receptor antagonists on TARC/CCL17 and MDC/CCL22 production from CD14+ cells induced by antigenic stimulation in vitro. Int Arch Allergy Immunol. 2011;155(1):38-51. doi: 10.1159/000318720. Epub 2010 Nov 25.
37 SIRT3 Mediates the Antioxidant Effect of Hydrogen Sulfide in Endothelial Cells. Antioxid Redox Signal. 2016 Feb 20;24(6):329-43. doi: 10.1089/ars.2015.6331. Epub 2015 Nov 10.
38 Immunomodulatory effect of selective serotonin reuptake inhibitors (SSRIs) on human T lymphocyte function and gene expression. Eur Neuropsychopharmacol. 2007 Dec;17(12):774-80.
39 Diesel exhaust particulate-induced activation of Stat3 requires activities of EGFR and Src in airway epithelial cells. Am J Physiol Lung Cell Mol Physiol. 2007 Feb;292(2):L422-9. doi: 10.1152/ajplung.00204.2006. Epub 2006 Oct 6.
40 Physapubescin B enhances the sensitivity of gastric cancer cells to trametinib by inhibiting the STAT3 signaling pathway. Toxicol Appl Pharmacol. 2020 Dec 1;408:115273. doi: 10.1016/j.taap.2020.115273. Epub 2020 Oct 6.
41 Sulindac induces apoptosis and inhibits tumor growth in vivo in head and neck squamous cell carcinoma. Neoplasia. 2007 Mar;9(3):192-9. doi: 10.1593/neo.06781.
42 Global molecular effects of tocilizumab therapy in rheumatoid arthritis synovium. Arthritis Rheumatol. 2014 Jan;66(1):15-23.
43 Simvastatin acts as an inhibitor of interferon gamma-induced cycloxygenase-2 expression in human THP-1 cells, but not in murine RAW264.7 cells. Biocell. 2009 Aug;33(2):107-14.
44 Therapeutic potential of cladribine in combination with STAT3 inhibitor against multiple myeloma. BMC Cancer. 2011 Jun 16;11:255. doi: 10.1186/1471-2407-11-255.
45 Quercetin exerts anti-melanoma activities and inhibits STAT3 signaling. Biochem Pharmacol. 2014 Feb 1;87(3):424-34. doi: 10.1016/j.bcp.2013.11.008. Epub 2013 Nov 23.