Target Information
Target General Infomation | |||||
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Target ID |
T47101
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Former ID |
TTDC00024
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Target Name |
Basic fibroblast growth factor receptor 1
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Gene Name |
FGFR1
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Synonyms |
CD331 antigen; FGFR-1; Fms-like tyrosine kinase 2; bFGF-R; c-fgr; FGFR1
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Target Type |
Clinical Trial
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Disease | Advanced solid tumor [ICD9: 140-199; ICD10: C00-C75, C7A, C7B] | ||||
Alzheimer disease [ICD9: 331; ICD10: G30] | |||||
Acute myeloid leukemia [ICD9: 205; ICD10: C92.0] | |||||
Cancer [ICD9: 140-229; ICD10: C00-C96] | |||||
Dermatological disease [ICD10: L00-L99] | |||||
Endometrial cancer [ICD9: 182; ICD10: C54.1] | |||||
Idiopathic pulmonary fibrosis; Non-small cell lung cancer [ICD9:516.3; ICD10: J84.1, C33-C34] | |||||
Lymphoma [ICD9: 202.8, 208.9; ICD10: C81-C86] | |||||
Ovarian cancer [ICD9: 183; ICD10: C56] | |||||
Peripheral arterial occlusive disease [ICD10: I73.9] | |||||
Retinoblastoma [ICD10: C69.2] | |||||
Severe coronary heart disease [ICD9: 414; ICD10: I25.1] | |||||
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48] | |||||
Unspecified [ICD code not available] | |||||
BioChemical Class |
Kinase
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Target Validation |
T47101
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UniProt ID | |||||
EC Number |
EC 2.7.10.1
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Sequence |
MWSWKCLLFWAVLVTATLCTARPSPTLPEQAQPWGAPVEVESFLVHPGDLLQLRCRLRDD
VQSINWLRDGVQLAESNRTRITGEEVEVQDSVPADSGLYACVTSSPSGSDTTYFSVNVSD ALPSSEDDDDDDDSSSEEKETDNTKPNRMPVAPYWTSPEKMEKKLHAVPAAKTVKFKCPS SGTPNPTLRWLKNGKEFKPDHRIGGYKVRYATWSIIMDSVVPSDKGNYTCIVENEYGSIN HTYQLDVVERSPHRPILQAGLPANKTVALGSNVEFMCKVYSDPQPHIQWLKHIEVNGSKI GPDNLPYVQILKTAGVNTTDKEMEVLHLRNVSFEDAGEYTCLAGNSIGLSHHSAWLTVLE ALEERPAVMTSPLYLEIIIYCTGAFLISCMVGSVIVYKMKSGTKKSDFHSQMAVHKLAKS IPLRRQVTVSADSSASMNSGVLLVRPSRLSSSGTPMLAGVSEYELPEDPRWELPRDRLVL GKPLGEGCFGQVVLAEAIGLDKDKPNRVTKVAVKMLKSDATEKDLSDLISEMEMMKMIGK HKNIINLLGACTQDGPLYVIVEYASKGNLREYLQARRPPGLEYCYNPSHNPEEQLSSKDL VSCAYQVARGMEYLASKKCIHRDLAARNVLVTEDNVMKIADFGLARDIHHIDYYKKTTNG RLPVKWMAPEALFDRIYTHQSDVWSFGVLLWEIFTLGGSPYPGVPVEELFKLLKEGHRMD KPSNCTNELYMMMRDCWHAVPSQRPTFKQLVEDLDRIVALTSNQEYLDLSMPLDQYSPSF PDTRSSTCSSGEDSVFSHEPLPEEPCLPRHPAQLANGGLKRR |
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Drugs and Mode of Action | |||||
Drug(s) | Nintedanib | Drug Info | Approved | Idiopathic pulmonary fibrosis | [556264] |
E-3810 | Drug Info | Phase 3 | Solid tumours | [524749], [542632] | |
Nintedanib | Drug Info | Phase 3 | Non-small cell lung cancer | [524516], [524899], [541221] | |
AZD4547 | Drug Info | Phase 2/3 | Solid tumours | [524785], [542682] | |
AM-001 | Drug Info | Phase 2 | Dermatological disease | [524425] | |
BGJ398 | Drug Info | Phase 2 | Cancer | [524793], [542803] | |
FGF-1 | Drug Info | Phase 2 | Severe coronary heart disease | [468100] | |
FP-1039 | Drug Info | Phase 2 | Endometrial cancer | [523259] | |
Nintedanib | Drug Info | Phase 2 | Ovarian cancer | [523930], [541221] | |
JNJ-42756493 | Drug Info | Phase 1/2 | Lymphoma | [549426] | |
MK-2461 | Drug Info | Phase 1/2 | Alzheimer disease | [530708] | |
ARQ-087 | Drug Info | Phase 1 | Cancer | [524164] | |
KW-2449 | Drug Info | Phase 1 | Acute myeloid leukemia | [530222], [541033] | |
SU-6668 | Drug Info | Phase 1 | Advanced solid tumor | [527156], [542760] | |
Sulfatinib | Drug Info | Phase 1 | Cancer | [524745] | |
BMS-695735 | Drug Info | Preclinical | Solid tumours | [548135] | |
PD-0183812 | Drug Info | Terminated | Retinoblastoma | [547217] | |
Inhibitor | 2-(1H-indazol-3-yl)-1H-benzo[d]imidazole | Drug Info | [528122] | ||
3-(3-methoxybenzyl)-1H-pyrrolo[2,3-b]pyridine | Drug Info | [551374] | |||
3-Benzimidazol-2-ylhydroquinolin-2-one | Drug Info | [529891] | |||
AAL-993 | Drug Info | [526484] | |||
ACTB-1003 | Drug Info | [543495] | |||
ARQ-087 | Drug Info | [543495] | |||
BMS-695735 | Drug Info | [529668] | |||
compound 2c | Drug Info | [532818] | |||
compound 7r | Drug Info | [533268] | |||
compound 8h | Drug Info | [531959] | |||
E-3810 | Drug Info | [525382] | |||
MK-2461 | Drug Info | [530708] | |||
NP-506 | Drug Info | [529888] | |||
PD-0166326 | Drug Info | [525862] | |||
PD-0173952 | Drug Info | [525862] | |||
PD-0173955 | Drug Info | [525862] | |||
PD-0173956 | Drug Info | [525862] | |||
PD-0173958 | Drug Info | [525862] | |||
PD-0179483 | Drug Info | [525862] | |||
PD-0180970 | Drug Info | [525862] | |||
PD-0183812 | Drug Info | [525924] | |||
Ro-4396686 | Drug Info | [528018] | |||
SEMAXINIB | Drug Info | [526484] | |||
SU-6668 | Drug Info | [536137], [536474] | |||
Sulfatinib | Drug Info | [550989] | |||
Modulator | 3052230 | Drug Info | |||
AZD4547 | Drug Info | [531819] | |||
BGJ398 | Drug Info | [532105] | |||
JNJ-42756493 | Drug Info | [543495] | |||
Nintedanib | Drug Info | [533123] | |||
Antagonist | AM-001 | Drug Info | [548887] | ||
FP-1039 | Drug Info | [544282] | |||
Binder | FGF-1 | Drug Info | [551435] | ||
Agonist | SAR-106881 | Drug Info | [543495] | ||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
Pathways | |||||
KEGG Pathway | MAPK signaling pathway | ||||
Ras signaling pathway | |||||
Rap1 signaling pathway | |||||
PI3K-Akt signaling pathway | |||||
Adherens junction | |||||
Signaling pathways regulating pluripotency of stem cells | |||||
Regulation of actin cytoskeleton | |||||
Pathways in cancer | |||||
Proteoglycans in cancer | |||||
Prostate cancer | |||||
Melanoma | |||||
Central carbon metabolism in cancer | |||||
NetPath Pathway | TCR Signaling Pathway | ||||
PANTHER Pathway | Angiogenesis | ||||
FGF signaling pathway | |||||
Pathway Interaction Database | Glypican 1 network | ||||
Syndecan-4-mediated signaling events | |||||
N-cadherin signaling events | |||||
FGF signaling pathway | |||||
WikiPathways | Regulation of Actin Cytoskeleton | ||||
Endochondral Ossification | |||||
MAPK Signaling Pathway | |||||
Mesodermal Commitment Pathway | |||||
Induction (Part 1 of 3) | |||||
Integrated Pancreatic Cancer Pathway | |||||
Signaling Pathways in Glioblastoma | |||||
Neural Crest Differentiation | |||||
Signaling by FGFR | |||||
References | |||||
Ref 468100 | (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: 4923). | ||||
Ref 523259 | ClinicalTrials.gov (NCT01244438) Study of FP-1039 in Subjects With Endometrial Cancers. U.S. National Institutes of Health. | ||||
Ref 523930 | ClinicalTrials.gov (NCT01610869) Low Dose Cyclophosphamide +/-- Nintedanib in Advanced Ovarian Cancer. U.S. National Institutes of Health. | ||||
Ref 524164 | ClinicalTrials.gov (NCT01752920) Phase 1 Dose Escalation Study of ARQ 087 in Adult Subjects With Advanced Solid Tumors. U.S. National Institutes of Health. | ||||
Ref 524425 | ClinicalTrials.gov (NCT01938599) Study Comparing AM001 Cream to Vehicle in the Treatment of Plaque Psoriasis. U.S. National Institutes of Health. | ||||
Ref 524516 | ClinicalTrials.gov (NCT01979952) Nintedanib Twice Daily vs Placebo in Patients Diagnosed With Idiopathic Pulmonary Fibrosis (IPF). U.S. National Institutes of Health. | ||||
Ref 524745 | ClinicalTrials.gov (NCT02133157) Phase I Study of Sulfatinib(HMPL-012) in Patients With Advanced Solid Tumors. U.S. National Institutes of Health. | ||||
Ref 524749 | ClinicalTrials.gov (NCT02135107) A Double-blind Comparative Study of the Efficacy and Safety of E3810 10mg Once and Twice Daily in Maintenance Therapy for PPI Resistant Gastroesophageal Reflux Disease Patients. U.S. National Institutes of Health. | ||||
Ref 524785 | ClinicalTrials.gov (NCT02154490) Lung-MAP: S1400 Biomarker-Targeted Second-Line Therapy in Treating Patients With Recurrent Stage IIIB-IV Squamous Cell Lung Cancer. U.S. National Institutes of Health. | ||||
Ref 524793 | ClinicalTrials.gov (NCT02160041) BGJ398 for Patients With Tumors With FGFR Genetic Alterations. U.S. National Institutes of Health. | ||||
Ref 524899 | ClinicalTrials.gov (NCT02231164) LUME-Columbus: Nintedanib Plus Docetaxel in Advanced Non-small Cell Lung Cancer With Translational Research. U.S. National Institutes of Health. | ||||
Ref 527156 | A phase I surrogate endpoint study of SU6668 in patients with solid tumors. Invest New Drugs. 2004 Nov;22(4):459-66. | ||||
Ref 530222 | 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. | ||||
Ref 530708 | MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33. | ||||
Ref 541033 | (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: 5691). | ||||
Ref 541221 | (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: 5936). | ||||
Ref 542632 | (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: 7649). | ||||
Ref 542682 | (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: 7707). | ||||
Ref 542760 | (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: 7816). | ||||
Ref 542803 | (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: 7877). | ||||
Ref 547217 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014130) | ||||
Ref 548135 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800022289) | ||||
Ref 525382 | 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. doi: 10.1158/0008-5472.CAN-10-2700. Epub 2011 Jan 6. | ||||
Ref 525862 | Biochem 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. | ||||
Ref 525924 | J Med Chem. 2000 Nov 30;43(24):4606-16.Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases. | ||||
Ref 526484 | J Med Chem. 2002 Dec 19;45(26):5687-93.Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. | ||||
Ref 528018 | Bioorg 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. | ||||
Ref 528122 | Bioorg 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. | ||||
Ref 529668 | J 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. | ||||
Ref 529888 | Bioorg 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. | ||||
Ref 529891 | J 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. | ||||
Ref 530222 | 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. | ||||
Ref 530708 | MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33. | ||||
Ref 531819 | AZD4547: an orally bioavailable, potent, and selective inhibitor of the fibroblast growth factor receptor tyrosine kinase family. Cancer Res. 2012 Apr 15;72(8):2045-56. | ||||
Ref 531959 | The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors. Bioorg Med Chem Lett. 2012 Aug 1;22(15):4979-85. | ||||
Ref 532105 | Pharmacological inhibition of fibroblast growth factor (FGF) receptor signaling ameliorates FGF23-mediated hypophosphatemic rickets. J Bone Miner Res. 2013 Apr;28(4):899-911. | ||||
Ref 532818 | Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors. ACS Med Chem Lett. 2012 Jul 26;3(9):705-9. | ||||
Ref 533268 | Design, synthesis and biological evaluation of novel FGFR inhibitors bearing an indazole scaffold. Org Biomol Chem. 2015 Jul 28;13(28):7643-54. | ||||
Ref 536137 | Dose-finding study of the multitargeted tyrosine kinase inhibitor SU6668 in patients with advanced malignancies. Clin Cancer Res. 2005 Sep 1;11(17):6240-6. | ||||
Ref 536474 | 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. | ||||
Ref 543495 | (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: 1808). | ||||
Ref 544282 | FGF1-gold nanoparticle conjugates targeting FGFR efficiently decrease cell viability upon NIR irradiation. Int J Nanomedicine. 2012; 7: 5915-5927. | ||||
Ref 548887 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029917) |
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