General Information of DTT (ID: TTI7421)

DTT Name Platelet-derived growth factor receptor beta (PDGFRB) DTT Info
Gene Name PDGFRB

Molecule-Related Drug & Molecule List

Molecule-Related Drug List
Molecule Type:
DTT
DTP
DME
Drug Status:
Discontinued Drug(s)
Approved Drug(s)
Clinical Trial Drug(s)
Patented Agent(s)
Investigative Drug(s)
3 Approved Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Becaplermin DM1R5X4 Diabetic complication 5A2Y Approved [1]
Romiplostim DM3U7SZ Thrombocytopenia 3B64 Approved [2]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [3]
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6 Clinical Trial Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
E-3810 DM42PFT Solid tumour/cancer 2A00-2F9Z Phase 3 [4]
Famitinib DMSFWT7 Solid tumour/cancer 2A00-2F9Z Phase 2 [5]
XL-820 DMMHX9K Solid tumour/cancer 2A00-2F9Z Phase 2 [6]
MK-2461 DM21WBH Alzheimer disease 8A20 Phase 1/2 [7]
SNN-0031 DM2X3BR Brain injury NA07.Z Phase 1/2 [8]
TAK-593 DMNFZOT Solid tumour/cancer 2A00-2F9Z Phase 1 [9]
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⏷ Show the Full List of 6 Clinical Trial Drug(s)
4 Patented Agent(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
PMID25656651-Compound-21a DMCKAON N. A. N. A. Patented [10]
PMID25656651-Compound-21b DMVABXI N. A. N. A. Patented [10]
PMID28460551-Compound-2 DM4DOUB N. A. N. A. Patented [11]
Pyridine derivative 18 DMBZMYT N. A. N. A. Patented [12]
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5 Discontinued Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
CDP-860 DMEI0LJ Solid tumour/cancer 2A00-2F9Z Discontinued in Phase 2 [13]
SRI-62-834 DMRKE9G Solid tumour/cancer 2A00-2F9Z Discontinued in Phase 2 [14]
CEP-2563 DMH1PQ0 Solid tumour/cancer 2A00-2F9Z Discontinued in Phase 1 [14]
AG1295 DMT10C2 N. A. N. A. Terminated [15]
RG-13022 DMRFYOS N. A. N. A. Terminated [16]
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106 Investigative Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
(1H-indol-2-yl)(5-methoxy-1H-indol-2-yl)methanone DM21CXZ Discovery agent N.A. Investigative [17]
(1H-indol-2-yl)(5-phenoxy-1H-indol-2-yl)methanone DM94XJ2 Discovery agent N.A. Investigative [17]
(1H-indol-2-yl)(6-methoxy-1H-indol-2-yl)methanone DM7KDNM Discovery agent N.A. Investigative [17]
(2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamine DMNGEFS Discovery agent N.A. Investigative [18]
(5-fluoro-1H-indol-2-yl)-(1H-indol-2-yl)methanone DMIV4BU Discovery agent N.A. Investigative [17]
(5-hydroxy-1H-indol-2-yl)(1H-indol-2-yl)methanone DMPBNYM Discovery agent N.A. Investigative [17]
(benzo[b]furan-2-yl)-(1H-indol-2-yl)methanone DME80RK Discovery agent N.A. Investigative [15]
1-Phenyl-1H-benzoimidazol-5-ol DMGV6BI Discovery agent N.A. Investigative [19]
1-Phenyl-1H-benzoimidazole DM8YPH0 Discovery agent N.A. Investigative [19]
2-(1H-indazol-3-yl)-1H-benzo[d]imidazole DM0CSH8 Discovery agent N.A. Investigative [20]
3-((E)-Styryl)-quinoline DMAO64J Discovery agent N.A. Investigative [16]
3-(1H-Indol-3-yl)-6,7-dimethoxy-quinoline DMSGCKU Discovery agent N.A. Investigative [16]
3-(1H-Indol-3-yl)-quinoline DMW7XN5 Discovery agent N.A. Investigative [16]
3-(2-Cyclohexyl-ethyl)-6,7-dimethoxy-quinoline DMVUK96 Discovery agent N.A. Investigative [16]
3-(3,4-Dichloro-phenyl)-6,7-dimethoxy-quinoline DMEJH13 Discovery agent N.A. Investigative [16]
3-(3,4-Difluoro-phenyl)-6,7-dimethoxy-quinoline DMX3AMB Discovery agent N.A. Investigative [16]
3-(3,4-Dimethoxy-phenyl)-6,7-dimethoxy-quinoline DMDU10A Discovery agent N.A. Investigative [16]
3-(3-Fluoro-phenyl)-6,7-dimethoxy-quinoline DM0ZHJQ Discovery agent N.A. Investigative [16]
3-(4-dimethylamino-benzylidenyl)-2-indolinone DM6XC0M Discovery agent N.A. Investigative [21]
3-(4-Fluoro-phenyl)-6,7-dimethoxy-quinoline DM0POH2 Discovery agent N.A. Investigative [16]
3-(6,7-Dimethoxy-quinolin-4-yloxy)-phenol DM4DFUS Discovery agent N.A. Investigative [22]
3-(6,7-Dimethoxy-quinolin-4-yloxy)-phenylamine DMAWXV6 Discovery agent N.A. Investigative [22]
3-Benzimidazol-2-ylhydroquinolin-2-one DMQXJA1 Discovery agent N.A. Investigative [23]
3-Benzyloxy-6,7-dimethoxy-quinoline DMPG315 Discovery agent N.A. Investigative [16]
3-Cyclohexylethynyl-6,7-dimethoxy-quinoline DMCQ6J8 Discovery agent N.A. Investigative [16]
3-Cyclopent-1-enyl-6,7-dimethoxy-quinoline DM1FSZM Discovery agent N.A. Investigative [16]
3-Cyclopentyl-6,7-dimethoxy-quinoline DMS7B6T Discovery agent N.A. Investigative [16]
3-Pyridin-3-yl-quinoline-6,7-diol DM60Q1B Discovery agent N.A. Investigative [16]
3-Pyridin-4-yl-quinolin-7-ol DM0SEL5 Discovery agent N.A. Investigative [24]
3-Pyridin-4-yl-quinoline DM6U074 Discovery agent N.A. Investigative [24]
3-Pyridin-4-yl-quinoline-5,7-diol DMPCT0A Discovery agent N.A. Investigative [24]
3-Thiophen-3-yl-quinoline DM9MFZ1 Discovery agent N.A. Investigative [16]
4-(2,3-Dimethoxy-phenoxy)-6,7-dimethoxy-quinoline DM6PMFJ Discovery agent N.A. Investigative [22]
4-(3,4-Dimethoxy-phenoxy)-6,7-dimethoxy-quinoline DMW1H6C Discovery agent N.A. Investigative [22]
4-(3,5-Dimethoxy-phenoxy)-6,7-dimethoxy-quinoline DM5279R Discovery agent N.A. Investigative [22]
4-(3-Bromo-phenoxy)-6,7-dimethoxy-quinazoline DMNBLQ8 Discovery agent N.A. Investigative [22]
4-(3-Bromo-phenoxy)-6,7-dimethoxy-quinoline DMK6JV7 Discovery agent N.A. Investigative [22]
4-(3-Ethoxy-phenoxy)-6,7-dimethoxy-quinoline DMOQE5W Discovery agent N.A. Investigative [22]
4-(3-Ethyl-phenoxy)-6,7-dimethoxy-quinoline DMFM9SH Discovery agent N.A. Investigative [22]
4-(3-Fluoro-phenoxy)-6,7-dimethoxy-quinoline DMER3D9 Discovery agent N.A. Investigative [22]
4-(5-Methoxy-benzoimidazol-1-yl)-phenylamine DMIWT60 Discovery agent N.A. Investigative [25]
4-(6,7-Dimethoxy-quinolin-3-yl)-benzoic acid DM8A6UH Discovery agent N.A. Investigative [16]
4-(6,7-Dimethoxy-quinolin-3-yl)-phenol DM9RNUX Discovery agent N.A. Investigative [16]
4-Benzoimidazol-1-yl-phenylamine DM7AOGD Discovery agent N.A. Investigative [19]
5,6,7-Trimethoxy-3-pyridin-4-yl-quinoline DM53CLY Discovery agent N.A. Investigative [24]
5,7-Dimethoxy-3-pyridin-4-yl-quinoline DM724JF Discovery agent N.A. Investigative [24]
5,7-Dimethoxy-3-thiophen-3-yl-quinoline DMJAQ41 Discovery agent N.A. Investigative [16]
5,7-Dimethyl-3-thiophen-3-yl-quinoline DM3P79O Discovery agent N.A. Investigative [16]
5-(6,7-Dimethoxy-quinolin-3-yl)-1H-pyridin-2-one DMVMBG0 Discovery agent N.A. Investigative [16]
5-Methoxy-1-phenyl-1H-benzoimidazole DMPEKWD Discovery agent N.A. Investigative [19]
6,7-Dichloro-3-thiophen-3-yl-quinoline DMJNHSL Discovery agent N.A. Investigative [16]
6,7-Difluoro-3-thiophen-3-yl-quinoline DMUZYXQ Discovery agent N.A. Investigative [16]
6,7-Dimethoxy-3-((E)-styryl)-quinoline DMSM0QV Discovery agent N.A. Investigative [16]
6,7-Dimethoxy-3-(3-methoxy-phenyl)-quinoline DMDENVF Discovery agent N.A. Investigative [16]
6,7-Dimethoxy-3-(4-methoxy-phenyl)-quinoline DM12DVT Discovery agent N.A. Investigative [16]
6,7-Dimethoxy-3-(4-nitro-phenyl)-quinoline DMM7NHI Discovery agent N.A. Investigative [16]
6,7-Dimethoxy-3-p-tolyl-quinoline DMM7IAK Discovery agent N.A. Investigative [16]
6,7-Dimethoxy-3-phenyl-quinoline DM516B4 Discovery agent N.A. Investigative [16]
6,7-Dimethoxy-3-phenylethynyl-quinoline DMFRXDT Discovery agent N.A. Investigative [16]
6,7-Dimethoxy-3-pyridin-3-yl-quinoline DMSG1AY Discovery agent N.A. Investigative [16]
6,7-Dimethoxy-3-pyridin-4-yl-quinoline DMW7K5P Discovery agent N.A. Investigative [24]
6,7-Dimethoxy-3-thiophen-2-yl-quinoline DM6WD8T Discovery agent N.A. Investigative [16]
6,7-Dimethoxy-4-(2-methoxy-phenoxy)-quinoline DMU15YV Discovery agent N.A. Investigative [22]
6,7-Dimethoxy-4-(3-methoxy-phenoxy)-quinoline DMPS2GX Discovery agent N.A. Investigative [22]
6,7-Dimethoxy-4-(3-nitro-phenoxy)-quinoline DM3YSNX Discovery agent N.A. Investigative [22]
6,7-Dimethoxy-4-(4-methoxy-phenoxy)-quinoline DMX2VFP Discovery agent N.A. Investigative [22]
6,7-Dimethoxy-4-m-tolyloxy-quinoline DMEMGPU Discovery agent N.A. Investigative [22]
6,7-Dimethoxy-4-phenoxy-quinoline DMBZP3I Discovery agent N.A. Investigative [22]
6-Methoxy-3-pyridin-4-yl-quinoline DM52SDO Discovery agent N.A. Investigative [24]
6-Methoxy-3-thiophen-3-yl-quinoline DMOYL71 Discovery agent N.A. Investigative [16]
7-Chloro-3-pyridin-4-yl-quinoline DM53A1R Discovery agent N.A. Investigative [24]
7-Fluoro-3-thiophen-3-yl-quinoline DM0QI8V Discovery agent N.A. Investigative [16]
7-Methoxy-3-pyridin-4-yl-quinoline DMUZIDT Discovery agent N.A. Investigative [24]
7-Methoxy-3-thiophen-3-yl-quinoline DM9QKLC Discovery agent N.A. Investigative [16]
7-Thiophen-3-yl-[1,3]dioxolo[4,5-g]quinoline DMMU5SO Discovery agent N.A. Investigative [16]
AGL 2043 DMM9A5N Discovery agent N.A. Investigative [26]
Benzyl-(6,7-dimethoxy-quinolin-3-yl)-amine DMFTIMS Discovery agent N.A. Investigative [16]
Bis(5-acetoxybenzo[b]furan-2-yl)methanone DM36VKH Discovery agent N.A. Investigative [15]
Bis(5-aminobenzo[b]furan-2-yl)methanone DMHRGTY Discovery agent N.A. Investigative [15]
Bis(5-hydroxybenzo[b]furan-2-yl)methanone DMGRKDP Discovery agent N.A. Investigative [15]
Bis(5-methoxybenzo[b]furan-2-yl)methanone DM9XC6A Discovery agent N.A. Investigative [15]
Bis(6-hydroxybenzo[b]furan-2-yl)methanone DMRGNSQ Discovery agent N.A. Investigative [15]
Bis(benzo[b]furan-2-yl)methanone DMK2ZG4 Discovery agent N.A. Investigative [15]
Bis-(5-hydroxy-1H-indol-2-yl)-methanone DMTSEXB Discovery agent N.A. Investigative [17]
BMS-536924 DMXJB4N Discovery agent N.A. Investigative [27]
CP-673451 DMVBPRO Discovery agent N.A. Investigative [28]
Di(1H-indol-2-yl)methanone DM3DR6J Discovery agent N.A. Investigative [17]
GTP-14564 DMW23Y9 Discovery agent N.A. Investigative [29]
HKI-9924129 DM5LR2B Gram-positive bacterial infection 1B74-1G40 Investigative [30]
JNJ-10198409 DM9GDP5 Discovery agent N.A. Investigative [18]
Ki-11502 DMLG2EA Discovery agent N.A. Investigative [31]
Ki-20227 DM9M3VC Discovery agent N.A. Investigative [32]
PD-0166326 DMD2CG9 Discovery agent N.A. Investigative [30]
PD-0173952 DMSCQ9U Discovery agent N.A. Investigative [30]
PD-0173955 DMOZEW9 Discovery agent N.A. Investigative [30]
PD-0173956 DM8RW92 Discovery agent N.A. Investigative [30]
PD-0173958 DMZQ8YV Discovery agent N.A. Investigative [30]
PD-0179483 DMKO8LE Discovery agent N.A. Investigative [30]
PDGF receptor tyrosine kinase inhibitor III DMORLTH Discovery agent N.A. Investigative [33]
PMID22765894C8h DMH5RFU Discovery agent N.A. Investigative [34]
Ro-4396686 DM5DMCH Discovery agent N.A. Investigative [35]
RPR-101511 DM0HD3O Discovery agent N.A. Investigative [16]
RPR-108514A DM37I92 Discovery agent N.A. Investigative [36]
SU-11652 DMGQXN7 Discovery agent N.A. Investigative [2]
TG-100435 DMIR3X2 Discovery agent N.A. Investigative [37]
XB-387 DMBN7UX Non-small-cell lung cancer 2C25.Y Investigative [38]
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⏷ Show the Full List of 106 Investigative Drug(s)
Molecule Interaction Atlas

References

1 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
2 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.
3 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.
4 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.
5 Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706.
6 National Cancer Institute Drug Dictionary (drug id 452042).
7 MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33.
8 Company report (Neuronova)
9 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.
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13 Blockade of platelet-derived growth factor receptor-beta by CDP860, a humanized, PEGylated di-Fab', leads to fluid accumulation and is associated w... J Clin Oncol. 2005 Feb 10;23(5):973-81.
14 Therapeutic target database update 2012: a resource for facilitating target-oriented drug discovery. Nucleic Acids Res. 2012 Jan;40(Database issue):D1128-36.
15 Inhibition of FLT3 and PDGFR tyrosine kinase activity by bis(benzo[b]furan-2-yl)methanones. Bioorg Med Chem. 2007 Mar 1;15(5):2187-97.
16 A new series of PDGF receptor tyrosine kinase inhibitors: 3-substituted quinoline derivatives. J Med Chem. 1994 Jul 8;37(14):2129-37.
17 Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase. J Med Chem. 2006 Jun 1;49(11):3101-15.
18 (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.
19 Structure-activity relationships for 1-phenylbenzimidazoles as selective ATP site inhibitors of the platelet-derived growth factor receptor. J Med Chem. 1998 Dec 31;41(27):5457-65.
20 Design and structure-activity relationship of 3-benzimidazol-2-yl-1H-indazoles as inhibitors of receptor tyrosine kinases. Bioorg Med Chem Lett. 2006 Jul 1;16(13):3595-9.
21 Synthesis and biological activity of N(4)-phenylsubstituted-6-(2,4-dichloro phenylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as vascular endo... Bioorg Med Chem. 2010 May 15;18(10):3575-87.
22 A novel series of 4-phenoxyquinolines: potent and highly selective inhibitors of PDGF receptor autophosphorylation, Bioorg. Med. Chem. Lett. 7(23):2935-2940 (1997).
23 Design, structure-activity relationships and in vivo characterization of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones: a novel class of receptor... J Med Chem. 2009 Jan 22;52(2):278-92.
24 5,7-Dimethoxy-3-(4-pyridinyl)quinoline is a potent and selective inhibitor of human vascular beta-type platelet-derived growth factor receptor tyro... J Med Chem. 1994 Aug 19;37(17):2627-9.
25 Structure-activity relationships for 5-substituted 1-phenylbenzimidazoles as selective inhibitors of the platelet-derived growth factor receptor. J Med Chem. 1999 Jul 1;42(13):2373-82.
26 Tricyclic quinoxalines as potent kinase inhibitors of PDGFR kinase, Flt3 and Kit. Bioorg Med Chem. 2003 May 1;11(9):2007-18.
27 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.
28 Antiangiogenic and antitumor activity of a selective PDGFR tyrosine kinase inhibitor, CP-673,451. Cancer Res. 2005 Feb 1;65(3):957-66.
29 Selective cytotoxic mechanism of GTP-14564, a novel tyrosine kinase inhibitor in leukemia cells expressing a constitutively active Fms-like tyrosin... J Biol Chem. 2003 Aug 29;278(35):32892-8.
30 Biochemical and cellular effects of c-Src kinase-selective pyrido[2, 3-d]pyrimidine tyrosine kinase inhibitors. Biochem Pharmacol. 2000 Oct 1;60(7):885-98.
31 Identification of potent and selective inhibitors of PDGF receptor autophosphorylation. J Med Chem. 2006 Apr 6;49(7):2186-92.
32 A c-fms tyrosine kinase inhibitor, Ki20227, suppresses osteoclast differentiation and osteolytic bone destruction in a bone metastasis model. Mol Cancer Ther. 2006 Nov;5(11):2634-43.
33 Potent and selective inhibitors of platelet-derived growth factor receptor phosphorylation. 3. Replacement of quinazoline moiety and improvement of metabolic polymorphism of 4-[4-(N-substituted (thio)carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline derivatives. J Med Chem. 2003 Nov 6;46(23):4910-25.
34 The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors. Bioorg Med Chem Lett. 2012 Aug 1;22(15):4979-85.
35 Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1950-3.
36 The synthesis and SAR of new 4-(N-alkyl-N-phenyl)amino-6,7-dimethoxyquinazolines and 4-(N-alkyl-N-phenyl)aminopyrazolo[3,4-d]pyrimidines, inhibitors of CSF-1R tyrosine kinase activity, Bioorg. Med. Chem. Lett. 7(4):421-424 (1997).
37 Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinas... Bioorg Med Chem Lett. 2007 Feb 1;17(3):602-8.
38 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: 1804).