Therapeutic Targets Database
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TTD Target ID: TTDC00024

Target Information
NameBasic fibroblast growth factor receptor 1    
Type of targetClinical trial target    
SynonymsCD331 antigen    
FGFR-1    
Fms-like tyrosine kinase 2    
bFGF-R    
c-fgr    
DiseasePeripheral Vascular Disease
[ICD9: 443.9   ICD10: I73.9]
[1]
Severe Coronary Heart Disease
[ICD9: 414.0   ICD10: I25.1]
[1]
Solid tumors
[ICD9: 140-199, 210-229   ICD10: C00-C75, C7A, C7B, D10-D36, D3A]
[2]
Ulcers
[ICD9: 556   ICD10: K51]
[1]
Drug(s)BrivanibPhase IIIFirst-line liver cancer, liver cancer (TACE) (see also colorectal, sarcoma)
NintedanibPhase IIINon-small cell lung cancer (NSCLC)
NintedanibPhase IIIOvarian cancer
AZD4547Phase IISolid Tumors
AZD4547Phase IISolid tumours
BrivanibPhase IIMetastatic colorectal cancer
BrivanibPhase IISarcoma
FGF-1Phase IISevere Coronary Heart Disease[3]
BGJ398Phase ISolid Tumors
FGF-1Phase IPeripheral Vascular Disease, Ulcers[3]
JNJ-42756493Phase ILymphoma
SU-6668DiscontinuedAdvanced solid tumours[4][5]
EC NumberEC 2.7.10.1
PathwayAdherens junction
MAPK signaling pathway
Melanoma
Pathways in cancer
Prostate cancer
Regulation of actin cytoskeleton
UniProt IDP11362
PDB Structure1AGW; 1CVS; 1EVT; 1FGI; 1FGK; 1FQ9; 1XR0; 2CR3; 2FGI; 3C4F; 3GQI; 3GQL; 3JS2; 3KRJ; 3KRL; 3KXX; 3KY2; 3OJV; 3RHX; 3TT0; 4F63; 4F64; 4F65.    
SequenceMWSWKCLLFWAVLVTATLCTARPSPTLPEQAQPWGAPVEVESFLVHPGDLLQLRCRLRDD VQSINWLRDGVQLAESNRTRITGEEVEVQDSVPADSGLYACVTSSPSGSDTTYFSVNVSD ALPSSEDDDDDDDSSSEEKETDNTKPNRMPVAPYWTSPEKMEKKLHAVPAAKTVKFKCPS SGTPNPTLRWLKNGKEFKPDHRIGGYKVRYATWSIIMDSVVPSDKGNYTCIVENEYGSIN HTYQLDVVERSPHRPILQAGLPANKTVALGSNVEFMCKVYSDPQPHIQWLKHIEVNGSKI GPDNLPYVQILKTAGVNTTDKEMEVLHLRNVSFEDAGEYTCLAGNSIGLSHHSAWLTVLE ALEERPAVMTSPLYLEIIIYCTGAFLISCMVGSVIVYKMKSGTKKSDFHSQMAVHKLAKS IPLRRQVTVSADSSASMNSGVLLVRPSRLSSSGTPMLAGVSEYELPEDPRWELPRDRLVL GKPLGEGCFGQVVLAEAIGLDKDKPNRVTKVAVKMLKSDATEKDLSDLISEMEMMKMIGK HKNIINLLGACTQDGPLYVIVEYASKGNLREYLQARRPPGLEYCYNPSHNPEEQLSSKDL VSCAYQVARGMEYLASKKCIHRDLAARNVLVTEDNVMKIADFGLARDIHHIDYYKKTTNG RLPVKWMAPEALFDRIYTHQSDVWSFGVLLWEIFTLGGSPYPGVPVEELFKLLKEGHRMD KPSNCTNELYMMMRDCWHAVPSQRPTFKQLVEDLDRIVALTSNQEYLDLSMPLDQYSPSF PDTRSSTCSSGEDSVFSHEPLPEEPCLPRHPAQLANGGLKRR
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
Inhibitor2- (1H-indazol-3-yl)-1H-benzo[d]imidazole[6]
3- (3-methoxybenzyl)-1H-pyrrolo[2,3-b]pyridine[7]
3-Benzimidazol-2-ylhydroquinolin-2-one[8]
AAL-993[9]
BMS-540215[10]
BMS-695735[11]
NP-506[12]
PD-0166326,   PD-166326[13]
PD-0173952[13]
PD-0173955,   PD-17395[13]
PD-0173956[13]
PD-0173958[13]
PD-0179483[13]
PD-0180970[13]
PD-0183812[14]
PD-173074[15]
Ro-4396686[16]
SEMAXINIB[9]
SU-5402[17]
SU-6668[4][5]
SU4984[18]
BinderFGF-1[3]
MultitargetSU-6668[4][5]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1CenterWatch. Drugs in Clinical Trials Database. CenterWatch. 2008. To Reference
Ref 2Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2007 Mar;29(2):153-73. To Reference
Ref 3Fibroblast Growth Factor-1 (FGF-1) for the Treatment of Coronary Heart Disease. Food and Drug Administration. 2009 To Reference
Ref 4A 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. To Reference
Ref 5Dose-finding study of the multitargeted tyrosine kinase inhibitor SU6668 in patients with advanced malignancies. Clin Cancer Res. 2005 Sep 1;11(17):6240-6. To Reference
Ref 6Bioorg Med Chem Lett. 2006 Jul 1;16(13):3595-9. Epub 2006 Apr 5.Design and structure-activity relationship of 3-benzimidazol-2-yl-1H-indazoles as inhibitors of receptor tyrosine kinases. To Reference
Ref 7Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. To Reference
Ref 8J Med Chem. 2009 Jan 22;52(2):278-92.Design, structure-activity relationships and in vivo characterization of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones: a novel class of receptor tyrosine kinase inhibitors. To Reference
Ref 9J Med Chem. 2002 Dec 19;45(26):5687-93.Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. To Reference
Ref 10J Med Chem. 2006 Apr 6;49(7):2143-6.Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor. To Reference
Ref 11J Med Chem. 2008 Oct 9;51(19):5897-900. Epub 2008 Sep 3.Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinase with broad spectrum in vivo antitumor activity. To Reference
Ref 12Bioorg Med Chem Lett. 2009 Feb 1;19(3):745-50. Epub 2008 Dec 10.5-Substituted pyrido[2,3-d]pyrimidine, an inhibitor against three receptor tyrosine kinases. To Reference
Ref 13Biochem Pharmacol. 2000 Oct 1;60(7):885-98.Biochemical and cellular effects of c-Src kinase-selective pyrido[2, 3-d]pyrimidine tyrosine kinase inhibitors. To Reference
Ref 14J Med Chem. 2000 Nov 30;43(24):4606-16.Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases. To Reference
Ref 15J Med Chem. 2005 Jul 14;48(14):4628-53.Synthesis and structure-activity relationships of soluble 7-substituted 3-(3,5-dimethoxyphenyl)-1,6-naphthyridin-2-amines and related ureas as dual inhibitors of the fibroblast growth factor receptor-1 and vascular endothelial growth factor receptor-2 tyrosine kinases. To Reference
Ref 16Bioorg Med Chem Lett. 2006 Apr 1;16(7):1950-3. Epub 2006 Feb 3.Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis. To Reference
Ref 17Science. 1997 May 9;276(5314):955-60.Structures of the tyrosine kinase domain of fibroblast growth factor receptor in complex with inhibitors. To Reference
Ref 18Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. To Reference



 

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