General Information of Drug (ID: DM9GDP5)

Drug Name
JNJ-10198409 Drug Info
Synonyms
JNJ-10198409; 627518-40-5; PDGFR Tyrosine Kinase Inhibitor IV; PDGF Receptor Tyrosine Kinase Inhibitor IV; CHEMBL120077; N-(3-fluorophenyl)-6,7-dimethoxy-1,4-dihydroindeno[1,2-c]pyrazol-3-amine; 3-Fluoro-N-(6,7-dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamine; ZDNURMVOKAERHZ-UHFFFAOYSA-N; SCHEMBL3088170; GTPL6020; CTK8E8807; jnj10198409; DTXSID70430890; MolPort-009-019-131; HMS3650O03; HMS3229I11; ZINC13677843; BDBM50179207; AKOS030525202; RWJ 540973; CCG-206773; NCGC00343986-02; RT-014973; KB-274227; SR-01000946814
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
9797370
CAS Number
CAS 627518-40-5
TTD Drug ID
DM9GDP5

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Investigative Drug(s)
Patented Agent(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dasatinib DMJV2EK Blast phase chronic myelogenous leukemia, BCR-ABL1 positive Approved [3]
VX-680 DM93YKJ Solid tumour/cancer 2A00-2F9Z Phase 2 [3]
JNJ-26483327 DMSQ3AZ Solid tumour/cancer 2A00-2F9Z Phase 1 [4]
ISIS-CRP DMQDUG4 Cardiovascular disease BA00-BE2Z Phase 1 [5]
RO-316233 DMAGLPW Discovery agent N.A. Investigative [6]
Bisindolylmaleimide-I DMOQJZC Discovery agent N.A. Investigative [6]
4,5,6,7-tetrabromo-1H-benzo[d][1,2,3]triazole DMN9YOB Discovery agent N.A. Investigative [7]
CI-1040 DMF3DZX Discovery agent N.A. Investigative [6]
AMP-PNP DMTOK1D Discovery agent N.A. Investigative [8]
BMS-536924 DMXJB4N Discovery agent N.A. Investigative [9]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dasatinib DMJV2EK Blast phase chronic myelogenous leukemia, BCR-ABL1 positive Approved [3]
JNJ-26483327 DMSQ3AZ Solid tumour/cancer 2A00-2F9Z Phase 1 [10]
Ro-4396686 DM5DMCH Discovery agent N.A. Investigative [11]
PMID15546730C2 DMOPUIH Discovery agent N.A. Investigative [12]
CEP-5104 DMV43GY Discovery agent N.A. Investigative [13]
CEP-6331 DMNXBTD Discovery agent N.A. Investigative [13]
1-Methoxy-2-[2-(2-Methoxy-Ethoxy]-Ethane DMD7WNV Discovery agent N.A. Investigative [14]
⏷ Show the Full List of 7 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Romiplostim DM3U7SZ Thrombocytopenia 3B64 Approved [15]
Ripretinib DM958QB Gastrointestinal stromal tumour 2B5B Approved [16]
Olaratumab DMNYOIX Soft tissue sarcoma 2B57 Approved [17]
Avapritinib DMK2GZX Gastrointestinal stromal tumour 2B5B Approved [18]
E-3810 DM42PFT Solid tumour/cancer 2A00-2F9Z Phase 3 [19]
CP-868596 DMZIM37 Gastrointestinal cancer 2C11 Phase 3 [20]
Famitinib DMSFWT7 Solid tumour/cancer 2A00-2F9Z Phase 2 [21]
XL-820 DMMHX9K Solid tumour/cancer 2A00-2F9Z Phase 2 [22]
MP470 DMELUAK Solid tumour/cancer 2A00-2F9Z Phase 2 [23]
MEDI-575 DMI9WVM Glioblastoma multiforme 2A00.0 Phase 2 [24]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [25]
Romiplostim DM3U7SZ Thrombocytopenia 3B64 Approved [15]
Becaplermin DM1R5X4 Diabetic complication 5A2Y Approved [26]
E-3810 DM42PFT Solid tumour/cancer 2A00-2F9Z Phase 3 [19]
Famitinib DMSFWT7 Solid tumour/cancer 2A00-2F9Z Phase 2 [21]
XL-820 DMMHX9K Solid tumour/cancer 2A00-2F9Z Phase 2 [22]
MK-2461 DM21WBH Alzheimer disease 8A20 Phase 1/2 [27]
SNN-0031 DM2X3BR Brain injury NA07.Z Phase 1/2 [28]
TAK-593 DMNFZOT Solid tumour/cancer 2A00-2F9Z Phase 1 [29]
Pyridine derivative 18 DMBZMYT N. A. N. A. Patented [30]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ponatinib DMYGJQO Acute lymphoblastic leukaemia 2A85 Approved [31]
Bosutinib DMTI8YE Blast phase chronic myelogenous leukemia, BCR-ABL1 positive Approved [3]
SKI-758 DMQ8E9R Ischemia 8B10-8B11 Approved [32]
Adenosine triphosphate DM79F6G Malnutrition 5B50-5B71 Approved [33]
Saracatinib DMBLHGP Hematologic tumour 2B33.Y Phase 2 [34]
Flumatinib DM0G5O6 Chronic myelogenous leukaemia 2A20.0 Phase 2 [35]
DCC-2036 DMJKFNU Chronic myeloid leukaemia 2A20 Phase 1/2 [36]
ISIS-CRP DMQDUG4 Cardiovascular disease BA00-BE2Z Phase 1 [37]
KW-2449 DMFO7RP Acute myeloid leukaemia 2A60 Phase 1 [38]
IkT-148009 DMMJ9HY Parkinson disease 8A00.0 Phase 1 [39]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting Proto-oncogene c-Src (SRC)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dasatinib DMJV2EK Blast phase chronic myelogenous leukemia, BCR-ABL1 positive Approved [3]
Bosutinib DMTI8YE Blast phase chronic myelogenous leukemia, BCR-ABL1 positive Approved [3]
SKI-758 DMQ8E9R Ischemia 8B10-8B11 Approved [32]
Herbimycin A DM6YWBF Solid tumour/cancer 2A00-2F9Z Approved [40]
AL3818 DM3WP0N Alveolar soft part sarcoma 2A60-2C35 Phase 3 [41]
CP-868596 DMZIM37 Gastrointestinal cancer 2C11 Phase 3 [41]
Masitinib DMRSNEU Amyotrophic lateral sclerosis 8B60.0 Phase 3 [42]
KX-01 DMF0NA9 Actinic keratosis EK90.0 Phase 3 [43]
Saracatinib DMBLHGP Hematologic tumour 2B33.Y Phase 2 [34]
TPX-0046 DMIVE67 Solid tumour/cancer 2A00-2F9Z Phase 1/2 [44]
⏷ 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
Fyn tyrosine protein kinase (FYN) TT2B9KF FYN_HUMAN Inhibitor [2]
LCK tyrosine protein kinase (LCK) TT860QF LCK_HUMAN Inhibitor [2]
Platelet-derived growth factor receptor alpha (PDGFRA) TT8FYO9 PGFRA_HUMAN Inhibitor [2]
Platelet-derived growth factor receptor beta (PDGFRB) TTI7421 PGFRB_HUMAN Inhibitor [2]
Proto-oncogene c-Src (SRC) TT6PKBN SRC_HUMAN Inhibitor [2]
Tyrosine-protein kinase ABL1 (ABL) TT3PJMV ABL1_HUMAN Inhibitor [2]

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: 6020).
2 (6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad ant... J Med Chem. 2005 Dec 29;48(26):8163-73.
3 A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.
4 National Cancer Institute Drug Dictionary (drug id 596693).
5 The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315.
6 Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105.
7 Optimization of protein kinase CK2 inhibitors derived from 4,5,6,7-tetrabromobenzimidazole. J Med Chem. 2004 Dec 2;47(25):6239-47.
8 The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
9 Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitum... J Med Chem. 2005 Sep 8;48(18):5639-43.
10 National Cancer Institute Drug Dictionary (drug id 596693).
11 Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1950-3.
12 Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitors. Bioorg Med Chem Lett. 2004 Dec 20;14(24):6061-6.
13 Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-linea... J Med Chem. 2008 Sep 25;51(18):5680-9.
14 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
15 Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel... J Med Chem. 2003 Mar 27;46(7):1116-9.
16 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
17 A phase I study of olaratumab, an anti-platelet-derived growth factor receptor alpha (PDGFRalpha) monoclonal antibody, in patients with advanced solid tumors. Cancer Chemother Pharmacol. 2014 Mar;73(3):595-604.
18 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
19 E-3810 is a potent dual inhibitor of VEGFR and FGFR that exerts antitumor activity in multiple preclinical models. Cancer Res. 2011 Feb 15;71(4):1396-405.
20 The FLT3 and PDGFR inhibitor crenolanib is a substrate of the multidrug resistance protein ABCB1 but does not inhibit transport function at pharmacologically relevant concentrations.Invest New Drugs.2015 Apr;33(2):300-9.
21 Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706.
22 National Cancer Institute Drug Dictionary (drug id 452042).
23 Phase 1B study of amuvatinib in combination with five standard cancer therapies in adults with advanced solid tumors. Cancer Chemother Pharmacol. 2014 Jul;74(1):195-204.
24 Clinical pipeline report, company report or official report of MedImmune (2011).
25 Preclinical overview of sorafenib, a multikinase inhibitor that targets both Raf and VEGF and PDGF receptor tyrosine kinase signaling.Mol Cancer Ther.2008 Oct;7(10):3129-40.
26 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
27 MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33.
28 Company report (Neuronova)
29 Biochemical characterization of TAK-593, a novel VEGFR/PDGFR inhibitor with a two-step slow binding mechanism. Biochemistry. 2011 Feb 8;50(5):738-51.
30 RET kinase inhibitors: a review of recent patents (2012-2015).Expert Opin Ther Pat. 2017 Jan;27(1):91-99.
31 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
32 Synthesis and Src kinase inhibitory activity of a series of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-7-furyl-3-quinolinecarbonitriles. J Med Chem. 2006 Dec 28;49(26):7868-76.
33 Targeted chronic myeloid leukemia therapy: Seeking a cure. Am J Health Syst Pharm. 2007 Dec 15;64(24 Suppl 15):S9-15.
34 Novel dual Src/Abl inhibitors for hematologic and solid malignancies.Expert Opin Investig Drugs.2010 Aug;19(8):931-45.
35 Flumatinib, a selective inhibitor of BCR-ABL/PDGFR/KIT, effectively overcomes drug resistance of certain KIT mutants. Cancer Sci. 2014 Jan;105(1):117-25.
36 Company report (Deciphera Pharmaceuticals: Tumor-Targeted Programs and Indications)
37 Structure-based optimization of pyrazolo[3,4-d]pyrimidines as Abl inhibitors and antiproliferative agents toward human leukemia cell lines. J Med Chem. 2008 Mar 13;51(5):1252-9.
38 KW-2449, a novel multikinase inhibitor, suppresses the growth of leukemia cells with FLT3 mutations or T315I-mutated BCR/ABL translocation. Blood. 2009 Aug 20;114(8):1607-17.
39 The c-Abl inhibitor IkT-148009 suppresses neurodegeneration in mouse models of heritable and sporadic Parkinson's disease. Sci Transl Med. 2023 Jan 18;15(679):eabp9352.
40 In vivo antitumor activity of herbimycin A, a tyrosine kinase inhibitor, targeted against BCR/ABL oncoprotein in mice bearing BCR/ABL-transfected cells. Leuk Res. 1994 Nov;18(11):867-73.
41 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
42 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
43 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
44 Clinical pipeline report, company report or official report of Turning Point Therapeutics.