Target General Infomation
Target ID
T80975
Former ID
TTDS00008
Target Name
Vascular endothelial growth factor receptor 2
Gene Name
KDR
Synonyms
VEGFR-2; VEGFR2; Fetal liver kinase 1; FLK-1; Kinase insert domain receptor; Protein-tyrosine kinase receptor flk-1; CD309; FLK1; VEGF-2 receptor; KDR
Target Type
Successful
Disease Cutaneous Melanoma [ICD10: C43-C44]
Advanced solid tumor [ICD9: 140-199; ICD10: C00-C75, C7A, C7B]
Advanced malignancies [ICD9: 140-229; ICD10: C00-C96]
Angiogenesis disorder [ICD10: I00-I99]
Alzheimer disease [ICD9: 331; ICD10: G30]
Advanced renal cell carcinoma [ICD9: 189; ICD10: C64]
Breast cancer; Liver cancer [ICD9:174, 175, 140-229, 155, 203.0; ICD10: C50, C22]
Biliary cancer [ICD10: C22, C24]
Breast cancer [ICD9: 174, 175; ICD10: C50]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Colorectal cancer [ICD9: 153, 154; ICD10: C18-C21]
Cardiovascular disorder [ICD10: I00-I99]
Chronic pain [ICD9: 338.2,780; ICD10: R52.1-R52.2, G89]
Fallopian tube cancer; Ovarian cancer; Peritoneal cavity cancer [ICD9: 140-229, 158, 183, 183.2, 221.0; ICD10: C48.1, C48.2, C56, C57, D28]
Gastric cancer; Renal cell carcinoma; Squamous cell cancer of head and neck [ICD9: 140-229, 151, 189; ICD10: C16, C64]
Gastrointestinal cancers; Advanced renal cell carcinoma [ICD9:150-159, 189; ICD10: C15-C26, C64]
Glioma; Solid tumours [ICD9: 140-199, 191; ICD10: C00-C75, C71, C7A, C7B]
Gastric cancer [ICD9: 151; ICD10: C16]
Hepatocellular carcinoma; NSCLC; Melanoma [ICD9: 155, 162, 172; ICD10: C22.0, C33, C34, C43]
Head and neck cancer [ICD9: 140-149, 140-229; ICD10: C07-C14, C32-C33]
Myelodysplastic syndrome; AML; Head and neck cancer; Breast cancer; Pancreatic cancer [ICD9: 140-149, 140-229, 157, 183, 205.0; ICD10: C07-C14, C25, C32, C33, C56, C92.0]
Metastatic colorectal cancer [ICD9: 153, 154; ICD10: C18-C21]
Medullary thyroid cancer [ICD9: 193; ICD10: C73]
Metastatic castration-resistant prostate cancer; Ovarian cancer [ICD9: 140-229, 183, 185; ICD10: C56, C61]
Metastatic breast cancer [ICD10: C50]
Melanoma [ICD9: 172; ICD10: C43]
Non-small-cell lung cancer; Ovarian cancer; Solid tumours [ICD9: 140-199, 140-229, 162, 183, 210-229; ICD10: C33-C34, C56, D10-D36, D3A]
Non-small cell lung cancer [ICD10: C33-C34]
Ovarian cancer [ICD9: 183; ICD10: C56]
Renal cancer [ICD9: 140-229, 189; ICD10: C64]
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48]
Thyroid cancer; Renal cell carcinoma [ICD9: 140-229, 189, 193; ICD10: C64, C73]
Function
Tyrosine-protein kinase that acts as a cell-surface receptor for VEGFA, VEGFC and VEGFD. Plays an essential role in the regulation of angiogenesis, vascular development, vascular permeability, and embryonic hematopoiesis. Promotes proliferation, survival, migration and differentiation of endothelial cells. Promotes reorganization of the actin cytoskeleton. Isoforms lacking a transmembrane domain, such as isoform 2 and isoform 3, may function as decoy receptors for VEGFA, VEGFC and/or VEGFD. Isoform 2 plays an important role as negative regulator of VEGFA- and VEGFC-mediated lymphangiogenesis by limiting the amount of free VEGFA and/or VEGFC and preventing their binding to FLT4. Modulates FLT1 and FLT4 signaling by forming heterodimers. Binding of vascular growth factors to isoform 1 leads to the activation of several signaling cascades. Activation of PLCG1 leads to the production of the cellular signaling molecules diacylglycerol and inositol 1,4,5-trisphosphate and the activation of protein kinase C. Mediates activation of MAPK1/ERK2, MAPK3/ERK1 and the MAP kinase signaling pathway, as well as of the AKT1 signaling pathway. Mediates phosphorylation of PIK3R1, the regulatory subunit of phosphatidylinositol 3-kinase, reorganization of the actin cytoskeleton and activation of PTK2/FAK1. Required for VEGFA-mediated induction of NOS2 and NOS3, leading to the production of the signaling molecule nitric oxide (NO) by endothelial cells. Phosphorylates PLCG1. Promotes phosphorylation of FYN, NCK1, NOS3, PIK3R1, PTK2/FAK1 and SRC.
BioChemical Class
Kinase
Target Validation
T80975
UniProt ID
EC Number
EC 2.7.10.1
Sequence
MQSKVLLAVALWLCVETRAASVGLPSVSLDLPRLSIQKDILTIKANTTLQITCRGQRDLD
WLWPNNQSGSEQRVEVTECSDGLFCKTLTIPKVIGNDTGAYKCFYRETDLASVIYVYVQD
YRSPFIASVSDQHGVVYITENKNKTVVIPCLGSISNLNVSLCARYPEKRFVPDGNRISWD
SKKGFTIPSYMISYAGMVFCEAKINDESYQSIMYIVVVVGYRIYDVVLSPSHGIELSVGE
KLVLNCTARTELNVGIDFNWEYPSSKHQHKKLVNRDLKTQSGSEMKKFLSTLTIDGVTRS
DQGLYTCAASSGLMTKKNSTFVRVHEKPFVAFGSGMESLVEATVGERVRIPAKYLGYPPP
EIKWYKNGIPLESNHTIKAGHVLTIMEVSERDTGNYTVILTNPISKEKQSHVVSLVVYVP
PQIGEKSLISPVDSYQYGTTQTLTCTVYAIPPPHHIHWYWQLEEECANEPSQAVSVTNPY
PCEEWRSVEDFQGGNKIEVNKNQFALIEGKNKTVSTLVIQAANVSALYKCEAVNKVGRGE
RVISFHVTRGPEITLQPDMQPTEQESVSLWCTADRSTFENLTWYKLGPQPLPIHVGELPT
PVCKNLDTLWKLNATMFSNSTNDILIMELKNASLQDQGDYVCLAQDRKTKKRHCVVRQLT
VLERVAPTITGNLENQTTSIGESIEVSCTASGNPPPQIMWFKDNETLVEDSGIVLKDGNR
NLTIRRVRKEDEGLYTCQACSVLGCAKVEAFFIIEGAQEKTNLEIIILVGTAVIAMFFWL
LLVIILRTVKRANGGELKTGYLSIVMDPDELPLDEHCERLPYDASKWEFPRDRLKLGKPL
GRGAFGQVIEADAFGIDKTATCRTVAVKMLKEGATHSEHRALMSELKILIHIGHHLNVVN
LLGACTKPGGPLMVIVEFCKFGNLSTYLRSKRNEFVPYKTKGARFRQGKDYVGAIPVDLK
RRLDSITSSQSSASSGFVEEKSLSDVEEEEAPEDLYKDFLTLEHLICYSFQVAKGMEFLA
SRKCIHRDLAARNILLSEKNVVKICDFGLARDIYKDPDYVRKGDARLPLKWMAPETIFDR
VYTIQSDVWSFGVLLWEIFSLGASPYPGVKIDEEFCRRLKEGTRMRAPDYTTPEMYQTML
DCWHGEPSQRPTFSELVEHLGNLLQANAQQDGKDYIVLPISETLSMEEDSGLSLPTSPVS
CMEEEEVCDPKFHYDNTAGISQYLQNSKRKSRPVSVKTFEDIPLEEPEVKVIPDDNQTDS
GMVLASEELKTLEDRTKLSPSFGGMVPSKSRESVASEGSNQTSGYQSGYHSDDTDTTVYS
SEEAELLKLIEIGVQTGSTAQILQPDSGTTLSSPPV
Structure
1VR2; 1Y6A; 1Y6B; 1YWN; 2M59; 2MET; 2MEU; 2OH4; 2P2H; 2P2I; 2QU5; 2QU6; 2RL5; 2X1W; 2X1X; 2XIR; 3B8Q; 3B8R; 3BE2; 3C7Q; 3CJF; 3CJG; 3CP9; 3CPB; 3CPC; 3DTW; 3EFL; 3EWH; 3KVQ; 3S35; 3S36; 3S37; 3U6J; 3V2A; 3V6B; 3VHE; 3VHK; 3VID; 3VNT; 3VO3; 4AG8; 4AGC; 4AGD; 4ASD; 4ASE; 1VR2; 1Y6A; 1Y6B; 1YWN; 2M59; 2MET; 2MEU; 2OH4; 2P2H; 2P2I; 2QU5; 2QU6; 2RL5; 2X1W; 2X1X; 2XIR; 3B8Q; 3B8R; 3BE2; 3C7Q; 3CJF; 3CJG; 3CP9; 3CPB; 3CPC; 3DTW; 3EFL; 3EWH; 3KVQ; 3S35; 3S36;3S37; 3U6J; 3V2A; 3V6B; 3VHE; 3VHK; 3VID; 3VNT; 3VO3; 4AG8; 4AGC; 4AGD; 4ASD; 4ASE
Drugs and Mode of Action
Drug(s) Axitinib Drug Info Approved Advanced renal cell carcinoma [532210], [532919], [541003]
Cabozantinib Drug Info Approved Medullary thyroid cancer [541185], [550636]
Pazopanib HCl Drug Info Approved Renal cancer [530677]
Ramucirumab Drug Info Approved Gastric cancer [533123], [542411]
Regorafenib Drug Info Approved Metastatic colorectal cancer [532210], [541189]
Sorafenib Drug Info Approved Advanced renal cell carcinoma [528230], [541050]
Sunitinib Drug Info Approved Gastrointestinal cancers; Advanced renal cell carcinoma [528715], [537114], [541052]
Vandetanib Drug Info Approved Solid tumours [531783], [541055]
YN-968D1 Drug Info Approved Breast cancer [525168], [542631], [549965]
Brivanib Drug Info Phase 3 Breast cancer; Liver cancer [523016], [541015]
Cediranib Drug Info Phase 3 Fallopian tube cancer; Ovarian cancer; Peritoneal cavity cancer [525194], [541007]
E-3810 Drug Info Phase 3 Solid tumours [524749], [542632]
Fruquintinib Drug Info Phase 3 Cancer [525024]
HKI-272 Drug Info Phase 3 Breast cancer [548009]
Sorafenib Drug Info Phase 3 Hepatocellular carcinoma; NSCLC; Melanoma [537114], [541050]
Tivozanib Drug Info Phase 3 Renal cancer [522960], [541307]
Alacizumab pegol Drug Info Phase 2 Non-small cell lung cancer [521677]
BAY-57-9352 Drug Info Phase 2 Solid tumours [548058]
BMS-690514 Drug Info Phase 2 Chronic pain [528940]
Cabozantinib Drug Info Phase 2 Metastatic castration-resistant prostate cancer; Ovarian cancer [541185], [550636]
CP-547632 Drug Info Phase 2 Non-small-cell lung cancer; Ovarian cancer; Solid tumours [521618], [542806]
Delphinidin Drug Info Phase 2 Cardiovascular disorder [527896]
Famitinib Drug Info Phase 2 Cancer [532104], [542811]
RAF265 Drug Info Phase 2 Melanoma [521813], [541017]
Sorafenib Drug Info Phase 2 Myelodysplastic syndrome; AML; Head and neck cancer; Breast cancer; Pancreatic cancer [537114], [541050]
VATALANIB Drug Info Phase 2 Solid tumours [521851], [541046]
XL880 Drug Info Phase 2 Gastric cancer; Renal cell carcinoma; Squamous cell cancer of head and neck [541022], [550637]
Anti-VEGFR2 CD8 cell therapy Drug Info Phase 1/2 Cancer [523207]
Elpamotide Drug Info Phase 1/2 Biliary cancer [522286]
MK-2461 Drug Info Phase 1/2 Alzheimer disease [530708]
OTSGC-A24 Drug Info Phase 1/2 Colorectal cancer [523227]
Cabozantinib Drug Info Phase 1b Thyroid cancer; Renal cell carcinoma [541185], [550636]
Altiratinib Drug Info Phase 1 Solid tumours [549538]
CEP-11981 Drug Info Phase 1 Solid tumours [522626], [542989]
CYC116 Drug Info Phase 1 Solid tumours [522163]
E 7080 Drug Info Phase 1 Ovarian cancer [536839]
E-7050 Drug Info Phase 1 Head and neck cancer [525301], [542872]
KRN633 Drug Info Phase 1 Glioma; Solid tumours [541306], [547568]
OSI-930 Drug Info Phase 1 Solid tumours [531624], [531955]
Pegdinetanib Drug Info Phase 1 Non-small cell lung cancer [523078]
PF-00337210 Drug Info Phase 1 Solid tumours [523008]
SU-6668 Drug Info Phase 1 Advanced solid tumor [527156], [542760]
Sulfatinib Drug Info Phase 1 Cancer [524745]
TAK-593 Drug Info Phase 1 Cancer [532187]
XL880 Drug Info Phase 1 Solid tumours [541022], [550637]
XL999 Drug Info Phase 1 Advanced malignancies [537114]
Motesanib Drug Info Discontinued in Phase 3 Non-small cell lung cancer [541005], [546905]
SU-14813 Drug Info Discontinued in Phase 2 Metastatic breast cancer [541051], [548093]
IMC-1C11 Drug Info Discontinued in Phase 1 Cancer [547109]
AG1295 Drug Info Terminated Discovery agent [541205], [546396]
CEP-5214 Drug Info Terminated Solid tumours [547462]
Inhibitor (2-Methoxy-phenyl)-(5-phenyl-oxazol-2-yl)-amine Drug Info [527458]
(3-Phenoxy-phenyl)-(5-phenyl-oxazol-2-yl)-amine Drug Info [527458]
(4-Phenoxy-phenyl)-quinazolin-4-yl-amine Drug Info [525876]
(5-Phenyl-oxazol-2-yl)-m-tolyl-amine Drug Info [527458]
2-(1H-indazol-3-yl)-1H-benzo[d]imidazole Drug Info [528122]
2-(5-Phenyl-oxazol-2-ylamino)-benzonitrile Drug Info [527458]
2-(p-toluidino)-4-phenylpyrimidine-5-carbonitrile Drug Info [528821]
2-(pyrimidin-4-ylamino)thiazole-5-carbonitrile Drug Info [527935]
3,4-di-(4-methoxyphenyl)-1H-pyrrole-2,5-dione Drug Info [528032]
3,4-diphenyl-1H-pyrrole-2,5-dione Drug Info [528032]
3,6-Di-pyridin-4-yl-pyrazolo[1,5-a]pyrimidine Drug Info [526462]
3-((3-bromothiophen-2-yl)methylene)indolin-2-one Drug Info [528681]
3-(1H-Indol-2-yl)-1H-quinolin-2-one Drug Info [526914]
3-(4-aminophenyl)thieno[3,2-c]pyridin-4-amine Drug Info [528593]
3-(4-methoxyphenyl)-4-phenyl-1H-pyrrole-2,5-dione Drug Info [528032]
3-(5-Phenyl-oxazol-2-ylamino)-benzonitrile Drug Info [527458]
3-(5-Thiophen-3-yl-pyridin-3-yl)-1H-indole Drug Info [526703]
3-Benzimidazol-2-ylhydroquinolin-2-one Drug Info [529891]
3-methyl-1H-thieno[2,3-c]pyrazole-5-carboxamide Drug Info [527793]
3-phenyl-1,4-dihydroindeno[1,2-c]pyrazole Drug Info [528227]
4-(4-aminophenyl)-1H-indazol-3yl-amine Drug Info [528716]
4-(4-m-Tolylamino-phthalazin-1-yl)-benzamide Drug Info [527725]
4-(4-p-Tolylamino-phthalazin-1-yl)-benzamide Drug Info [527725]
4-(5-Phenyl-oxazol-2-ylamino)-benzenesulfonamide Drug Info [527458]
4-(isoquinolin-5-yl)-N-m-tolylphthalazin-1-amine Drug Info [527948]
4-(isoquinolin-5-yl)-N-o-tolylphthalazin-1-amine Drug Info [527948]
4-Chloro-N-(2-chloro-benzoyl)-benzenesulfonamide Drug Info [527245]
4-Chloro-N-(2-methyl-benzoyl)-benzenesulfonamide Drug Info [527245]
4-Chloro-N-(3-chloro-benzoyl)-benzenesulfonamide Drug Info [527245]
4-Chloro-N-(4-chloro-benzoyl)-benzenesulfonamide Drug Info [527245]
4-Chloro-N-(4-nitro-benzoyl)-benzenesulfonamide Drug Info [527245]
4-phenyl-2-(phenylamino)pyrimidine-5-carbonitrile Drug Info [528821]
5-(4-Methoxy-phenyl)-1-phenyl-1H-benzoimidazole Drug Info [526669]
6-(1H-Benzoimidazol-2-yl)-benzocyclohepten-7-one Drug Info [526914]
6-o-tolylquinazolin-2-amine Drug Info [528429]
8-methyl-4H,7H-indolo[6,5,4-cd]indol-5-one Drug Info [528681]
AAL-993 Drug Info [526484]
AG-E-85378 Drug Info [529047]
AG1295 Drug Info [530377]
AMG-429 Drug Info [543499]
AST-487 Drug Info [528954]
BAY-57-9352 Drug Info [536474]
BIBF-1202 Drug Info [531679]
BMS-536924 Drug Info [527711]
BMS-645737 Drug Info [529409]
BMS-690514 Drug Info [530732]
BX-795 Drug Info [527484]
BX-912 Drug Info [527484]
Cabozantinib Drug Info [550636]
CB-676475 Drug Info [527794]
Cediranib Drug Info [536474], [550288]
CEP-11981 Drug Info [536474]
CEP-5104 Drug Info [529647]
compound 13a Drug Info [532338]
compound 8h Drug Info [531959]
CP-547632 Drug Info [536201], [536474]
CYC116 Drug Info [550374]
E 7080 Drug Info [536839]
E-3810 Drug Info [525382]
Famitinib Drug Info [532104]
Fruquintinib Drug Info [533061]
HKI-272 Drug Info [528774]
IM-023911 Drug Info [527725]
IM-094261 Drug Info [527725]
IM-094882 Drug Info [527948]
Indolin-2-one deriv. 4b Drug Info [525828]
Isoindolinone Urea derivative Drug Info [527209]
JNJ-38158471 Drug Info [543499]
K-252a analogue Drug Info [527569]
Ki-20227 Drug Info [528535]
KRN633 Drug Info [536474]
L000021649 Drug Info [526462]
MG-516 Drug Info [543499]
MK-2461 Drug Info [530708]
Motesanib Drug Info [537551], [550250], [551087]
N-(2,4-Dichloro-benzoyl)-benzenesulfonamide Drug Info [527245]
N-(3-Bromo-benzoyl)-4-chloro-benzenesulfonamide Drug Info [527245]
Pazopanib HCl Drug Info [530677]
Phenyl-(5-phenyl-oxazol-2-yl)-amine Drug Info [527458]
PLX-4720 Drug Info [526516]
PP121 Drug Info [529744]
Pyrazolo[1,5-a]pyrimidine 3G Drug Info [526462]
Ro-4396686 Drug Info [528018]
SEMAXINIB Drug Info [526484]
SU-11652 Drug Info [526575]
SU-14813 Drug Info [536260], [536474], [549974]
SU-6668 Drug Info [536137], [536474]
Sulfatinib Drug Info [550989]
TG-100435 Drug Info [528527]
Vandetanib Drug Info [536474], [550288]
VATALANIB Drug Info [528774]
VEGF receptor 2 kinase inhibitor I Drug Info [534662]
WHI-P180 Drug Info [528681]
XL999 Drug Info [536402]
YN-968D1 Drug Info [531412]
[3-(5-Phenyl-oxazol-2-ylamino)-phenyl]-methanol Drug Info [527458]
Antagonist Altiratinib Drug Info [550598]
CEP-5214 Drug Info [528142]
Modulator Anti-VEGFR2 CD8 cell therapy Drug Info [523207], [532072]
Axitinib Drug Info [532210], [532919]
Brivanib Drug Info [1572591]
Delphinidin Drug Info [527896]
E-7050 Drug Info [530452]
EPI-0030 Drug Info [543499]
OSI-930 Drug Info [531624], [531955]
Pegdinetanib Drug Info [543499]
PF-00337210 Drug Info [544325]
RAF265 Drug Info [531962]
Ramucirumab Drug Info [533123]
Regorafenib Drug Info [551871]
Sorafenib Drug Info [528230]
Sunitinib Drug Info [526516], [528715]
TAK-593 Drug Info [532187], [553086]
Tivozanib Drug Info [550325]
XL880 Drug Info [1572591]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Ras signaling pathway
Rap1 signaling pathway
Cytokine-cytokine receptor interaction
Endocytosis
PI3K-Akt signaling pathway
VEGF signaling pathway
Focal adhesion
Proteoglycans in cancer
NetPath Pathway IL2 Signaling Pathway
PANTHER Pathway Angiogenesis
VEGF signaling pathway
Pathway Interaction Database HIF-2-alpha transcription factor network
Beta3 integrin cell surface interactions
Signaling events mediated by TCPTP
SHP2 signaling
S1P1 pathway
VEGF and VEGFR signaling network
Integrins in angiogenesis
Signaling events mediated by VEGFR1 and VEGFR2
Notch-mediated HES/HEY network
Reactome Neurophilin interactions with VEGF and VEGFR
VEGF binds to VEGFR leading to receptor dimerization
Integrin cell surface interactions
EPHA-mediated growth cone collapse
VEGFA-VEGFR2 Pathway
VEGFR2 mediated cell proliferation
WikiPathways Focal Adhesion
Nifedipine Activity
Cardiac Progenitor Differentiation
Signaling by VEGF
Angiogenesis
References
Ref 521618ClinicalTrials.gov (NCT00096239) CP-547,632 in Treating Patients With Recurrent or Persistent Ovarian Cancer, Primary Peritoneal Cancer, or Fallopian Tube Cancer. U.S. National Institutes of Health.
Ref 521677ClinicalTrials.gov (NCT00152477) A Study of Paclitaxel/Carboplatin With or Without CDP791 in Patients With Lung Cancer. U.S. National Institutes of Health.
Ref 521813ClinicalTrials.gov (NCT00304525) A Study to Evaluate RAF265, an Oral Drug Administered to Subjects With Locally Advanced or Metastatic Melanoma. U.S. National Institutes of Health.
Ref 521851ClinicalTrials.gov (NCT00348790) Vatalanib in Treating Patients With Recurrent or Progressive Meningioma. U.S. National Institutes of Health.
Ref 522163ClinicalTrials.gov (NCT00560716) A Phase I Pharmacologic Study of CYC116, an Oral Aurora Kinase Inhibitor, in Patients With Advanced Solid Tumors. U.S. National Institutes of Health.
Ref 522286ClinicalTrials.gov (NCT00655785) Antiangiogenic Peptide Vaccine Therapy With Gemcitabine in Treating Patient With Pancreatic Cancer (Phase1/2). U.S. National Institutes of Health.
Ref 522626ClinicalTrials.gov (NCT00875264) Open-Label Study to Determine the Maximum Tolerated Oral Dose of the Kinase Inhibitor CEP-11981 in Patients With Advanced Cancer. U.S. National Institutes of Health.
Ref 522960ClinicalTrials.gov (NCT01076010) An Extension Treatment Protocol for Subjects Who Have Participated in a Phase 3 Study of Tivozanib Versus Sorafenib in Renal Cell Carcinoma (Protocol AV-951-09-301). U.S. National Institutes of Health.
Ref 523008ClinicalTrials.gov (NCT01105533) A Dose Finding Study Of A New Medication, PF-00337210 That Will Possibly Decrease Blood Supply To Tumors. U.S. National Institutes of Health.
Ref 523016ClinicalTrials.gov (NCT01108705) Comparison of Brivanib and Best Supportive Care (BSC) With Placebo and BSC for Treatment of Liver Cancer in Asian Patients Who Have Failed Sorafenib Treatment. U.S. National Institutes of Health.
Ref 523078ClinicalTrials.gov (NCT01146171) Japanese Phase 1 Study of BMS-844203 (CT322). U.S. National Institutes of Health.
Ref 523207ClinicalTrials.gov (NCT01218867) CAR T Cell Receptor Immunotherapy Targeting VEGFR2 for Patients With Metastatic Cancer. U.S. National Institutes of Health.
Ref 523227ClinicalTrials.gov (NCT01227772) Study of OTSGC-A24 Vaccine in Advanced Gastric Cancer. U.S. National Institutes of Health.
Ref 524745ClinicalTrials.gov (NCT02133157) Phase I Study of Sulfatinib(HMPL-012) in Patients With Advanced Solid Tumors. U.S. National Institutes of Health.
Ref 524749ClinicalTrials.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 525024ClinicalTrials.gov (NCT02314819) A Phase III Trial Evaluating Fruquintinib Efficacy and Safety in 3+ Line Colorectal Cancer Patients ???RESCO). U.S. National Institutes of Health.
Ref 525168ClinicalTrials.gov (NCT02426034) Study of Apatinib Tablets in the Treatment of Advanced or Metastatic Gastric Cancer. U.S. National Institutes of Health.
Ref 525194ClinicalTrials.gov (NCT02446600) Olaparib or Cediranib Maleate and Olaparib Compared With Standard Platinum-Based Chemotherapy in Treating Patients With Recurrent Platinum-Sensitive Ovarian, Fallopian Tube, or Primary Peritoneal Cancer. U.S. National Institutes of Health.
Ref 525301ClinicalTrials.gov (NCT02533102) Pharmacokinetics and Food Effect of Single Oral Dose of E7050 in Healthy Volunteers.
Ref 527156A phase I surrogate endpoint study of SU6668 in patients with solid tumors. Invest New Drugs. 2004 Nov;22(4):459-66.
Ref 527896Delphinidin, a dietary anthocyanidin, inhibits vascular endothelial growth factor receptor-2 phosphorylation. Carcinogenesis. 2006 May;27(5):989-96. Epub 2005 Nov 23.
Ref 528230Sorafenib (BAY 43-9006, Nexavar), a dual-action inhibitor that targets RAF/MEK/ERK pathway in tumor cells and tyrosine kinases VEGFR/PDGFR in tumor vasculature. Methods Enzymol. 2006;407:597-612.
Ref 5287152006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
Ref 528940A novel epidermal growth factor receptor inhibitor promotes apoptosis in non-small cell lung cancer cells resistant to erlotinib. Cancer Res. 2007 Jul 1;67(13):6253-62.
Ref 530677Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
Ref 530708MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33.
Ref 531624Inhibition of c-Kit, VEGFR-2 (KDR), and ABCG2 by analogues of OSI-930. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6495-9.
Ref 5317832011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
Ref 531955OSI-930 analogues as novel reversal agents for ABCG2-mediated multidrug resistance. Biochem Pharmacol. 2012 Sep 15;84(6):766-74.
Ref 532104Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706.
Ref 532187Anti-angiogenic and anti-tumor effects of TAK-593, a potent and selective inhibitor of vascular endothelial growth factor and platelet-derived growth factor receptor tyrosine kinase. Cancer Sci. 2013Apr;104(4):486-94.
Ref 532210Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
Ref 532919Axitinib: VEGF inhibition in advanced thyroid cancer. Lancet Oncol. 2014 Jul;15(8):e310.
Ref 5331232014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
Ref 536839Emerging drugs for ovarian cancer. Expert Opin Emerg Drugs. 2008 Sep;13(3):523-36.
Ref 537114Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127.
Ref 541003(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: 5659).
Ref 541005(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: 5660).
Ref 541007(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: 5664).
Ref 541015(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: 5671).
Ref 541017(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: 5674).
Ref 541022(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: 5679).
Ref 541046(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: 5705).
Ref 541050(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: 5711).
Ref 541051(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: 5712).
Ref 541052(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: 5713).
Ref 541055(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: 5717).
Ref 541185(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: 5887).
Ref 541189(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: 5891).
Ref 541205(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: 5914).
Ref 541306(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: 6057).
Ref 541307(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: 6058).
Ref 542411(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: 7390).
Ref 542631(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: 7648).
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 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 542806(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: 7881).
Ref 542811(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: 7886).
Ref 542872(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: 7956).
Ref 542989(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: 8189).
Ref 546396Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007894)
Ref 546905Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011016)
Ref 547109Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013121)
Ref 547462Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016567)
Ref 547568Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017407)
Ref 548009Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021154)
Ref 548058Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021605)
Ref 548093Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021861)
Ref 549538Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800040094)
Ref 549965Clinical pipeline report, company report or official report of LSK BioPharma.
Ref 550636Clinical pipeline report, company report or official report of Exelixis (2011).
Ref 550637Clinical pipeline report, company report or official report of Exelixis (2011).
Ref
Ref 523207ClinicalTrials.gov (NCT01218867) CAR T Cell Receptor Immunotherapy Targeting VEGFR2 for Patients With Metastatic Cancer. U.S. National Institutes of Health.
Ref 525382E-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 525828Identification of substituted 3-[(4,5,6, 7-tetrahydro-1H-indol-2-yl)methylene]-1,3-dihydroindol-2-ones as growth factor receptor inhibitors for VEGF-R2 (Flk-1/KDR), FGF-R1, and PDGF-Rbeta tyrosine kinases. J Med Chem. 2000 Jul 13;43(14):2655-63.
Ref 525876Bioorg Med Chem Lett. 2000 Oct 2;10(19):2167-70.Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I.
Ref 526462Bioorg Med Chem Lett. 2002 Dec 16;12(24):3537-41.Optimization of a pyrazolo[1,5-a]pyrimidine class of KDR kinase inhibitors: improvements in physical properties enhance cellular activity and pharmacokinetics.
Ref 526484J Med Chem. 2002 Dec 19;45(26):5687-93.Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors.
Ref 526516In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship. Clin Cancer Res. 2003 Jan;9(1):327-37.
Ref 526575J Med Chem. 2003 Mar 27;46(7):1116-9.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 tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase.
Ref 526669Bioorg Med Chem Lett. 2003 Aug 4;13(15):2485-8.Design and synthesis of 1,5-diarylbenzimidazoles as inhibitors of the VEGF-receptor KDR.
Ref 526703Bioorg Med Chem Lett. 2003 Sep 15;13(18):2973-6.Discovery and evaluation of 3-(5-thien-3-ylpyridin-3-yl)-1H-indoles as a novel class of KDR kinase inhibitors.
Ref 526914Bioorg Med Chem Lett. 2004 Jan 19;14(2):351-5.Optimization of the indolyl quinolinone class of KDR (VEGFR-2) kinase inhibitors: effects of 5-amido- and 5-sulphonamido-indolyl groups on pharmacokinetics and hERG binding.
Ref 527209Bioorg Med Chem Lett. 2004 Sep 6;14(17):4505-9.Isoindolinone ureas: a novel class of KDR kinase inhibitors.
Ref 527245J Med Chem. 2004 Oct 21;47(22):5367-80.Acyl sulfonamide anti-proliferatives: benzene substituent structure-activity relationships for a novel class of antitumor agents.
Ref 527458J Med Chem. 2005 Mar 10;48(5):1610-9.Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors.
Ref 527484Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. J Biol Chem. 2005 May 20;280(20):19867-74. Epub 2005 Mar 16.
Ref 527569J Med Chem. 2005 Jun 2;48(11):3776-83.Synthesis, modeling, and in vitro activity of (3'S)-epi-K-252a analogues. Elucidating the stereochemical requirements of the 3'-sugar alcohol on trkA tyrosine kinase activity.
Ref 527711J Med Chem. 2005 Sep 8;48(18):5639-43.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 antitumor activity.
Ref 527725Bioorg Med Chem Lett. 2005 Nov 1;15(21):4696-8.Arylphthalazines: identification of a new phthalazine chemotype as inhibitors of VEGFR kinase.
Ref 527793Bioorg Med Chem Lett. 2006 Jan 1;16(1):96-9. Epub 2005 Oct 10.Scaffold oriented synthesis. Part 1: Design, preparation, and biological evaluation of thienopyrazoles as kinase inhibitors.
Ref 527794Bioorg Med Chem Lett. 2006 Jan 1;16(1):129-33. Epub 2005 Oct 10.Synthesis of a novel biotin-tagged photoaffinity probe for VEGF receptor tyrosine kinases.
Ref 527896Delphinidin, a dietary anthocyanidin, inhibits vascular endothelial growth factor receptor-2 phosphorylation. Carcinogenesis. 2006 May;27(5):989-96. Epub 2005 Nov 23.
Ref 527935Bioorg Med Chem Lett. 2006 Mar 1;16(5):1146-50. Epub 2005 Dec 20.Potent 2-[(pyrimidin-4-yl)amine}-1,3-thiazole-5-carbonitrile-based inhibitors of VEGFR-2 (KDR) kinase.
Ref 527948Bioorg Med Chem Lett. 2006 Mar 15;16(6):1579-81. Epub 2005 Dec 28.Arylphthalazines. Part 2: 1-(Isoquinolin-5-yl)-4-arylamino phthalazines as potent inhibitors of VEGF receptors I and II.
Ref 528018Bioorg 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 528032J Med Chem. 2006 Feb 23;49(4):1271-81.Design, synthesis, and biological evaluation of 3,4-diarylmaleimides as angiogenesis inhibitors.
Ref 528122Bioorg 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 528142Neuropilin-2 interacts with VEGFR-2 and VEGFR-3 and promotes human endothelial cell survival and migration. Blood. 2006 Aug 15;108(4):1243-50. Epub 2006 Apr 18.
Ref 528227Bioorg Med Chem Lett. 2006 Aug 15;16(16):4371-5. Epub 2006 Jun 5.Hit-to-lead optimization of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of KDR kinase inhibitors.
Ref 528230Sorafenib (BAY 43-9006, Nexavar), a dual-action inhibitor that targets RAF/MEK/ERK pathway in tumor cells and tyrosine kinases VEGFR/PDGFR in tumor vasculature. Methods Enzymol. 2006;407:597-612.
Ref 528429J Med Chem. 2006 Sep 21;49(19):5671-86.Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity.
Ref 528527Bioorg Med Chem Lett. 2007 Feb 1;17(3):602-8. Epub 2006 Nov 7.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 kinase inhibitor with anti-tumor activity in preclinical assays.
Ref 528535A 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.
Ref 528593Bioorg Med Chem Lett. 2007 Mar 1;17(5):1246-9. Epub 2006 Dec 9.Thienopyridine urea inhibitors of KDR kinase.
Ref 528681Bioorg Med Chem Lett. 2007 Apr 15;17(8):2126-33. Epub 2007 Feb 2.Pharmacophore modeling and in silico screening for new KDR kinase inhibitors.
Ref 5287152006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
Ref 528716J Med Chem. 2007 Apr 5;50(7):1584-97. Epub 2007 Mar 8.Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor.
Ref 528774Bioorg Med Chem. 2007 Jun 1;15(11):3635-48. Epub 2007 Mar 23.Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cysteine residues in the kinase domains of EGFR and VEGFR-2.
Ref 528821Bioorg Med Chem Lett. 2007 Jun 15;17(12):3266-70. Epub 2007 Apr 10.4-Aryl-5-cyano-2-aminopyrimidines as VEGF-R2 inhibitors: synthesis and biological evaluation.
Ref 528954The RET kinase inhibitor NVP-AST487 blocks growth and calcitonin gene expression through distinct mechanisms in medullary thyroid cancer cells. Cancer Res. 2007 Jul 15;67(14):6956-64.
Ref 529047Discovery of N-phenyl nicotinamides as potent inhibitors of Kdr. Bioorg Med Chem Lett. 2007 Nov 1;17(21):6003-8. Epub 2007 Aug 22.
Ref 529196Phase I evaluation of CDP791, a PEGylated di-Fab' conjugate that binds vascular endothelial growth factor receptor 2. Clin Cancer Res. 2007 Dec 1;13(23):7113-8.
Ref 529409Bioorg Med Chem Lett. 2008 May 1;18(9):2985-9. Epub 2008 Mar 22.Discovery and preclinical studies of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737), an in vivo active potent VEGFR-2 inhibitor.
Ref 529647J Med Chem. 2008 Sep 25;51(18):5680-9. Epub 2008 Aug 21.Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models.
Ref 529744Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol. 2008 Nov;4(11):691-9.
Ref 529891J 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 530377Bioorg Med Chem. 2009 Oct 15;17(20):7324-36. Epub 2009 Aug 22.Design, synthesis, and X-ray crystal structures of 2,4-diaminofuro[2,3-d]pyrimidines as multireceptor tyrosine kinase and dihydrofolate reductase inhibitors.
Ref 530452E7050: a dual c-Met and VEGFR-2 tyrosine kinase inhibitor promotes tumor regression and prolongs survival in mouse xenograft models. Cancer Sci. 2010 Jan;101(1):210-5.
Ref 530677Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
Ref 530708MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33.
Ref 530732Preclinical pharmacokinetics and in vitro metabolism of BMS-690514, a potent inhibitor of EGFR and VEGFR2. J Pharm Sci. 2010 Aug;99(8):3579-93.
Ref 531412YN968D1 is a novel and selective inhibitor of vascular endothelial growth factor receptor-2 tyrosine kinase with potent activity in vitro and in vivo. Cancer Sci. 2011 Jul;102(7):1374-80.
Ref 531624Inhibition of c-Kit, VEGFR-2 (KDR), and ABCG2 by analogues of OSI-930. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6495-9.
Ref 531679Comprehensive analysis of kinase inhibitor selectivity. Nat Biotechnol. 2011 Oct 30;29(11):1046-51.
Ref 531955OSI-930 analogues as novel reversal agents for ABCG2-mediated multidrug resistance. Biochem Pharmacol. 2012 Sep 15;84(6):766-74.
Ref 531959The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors. Bioorg Med Chem Lett. 2012 Aug 1;22(15):4979-85.
Ref 531962RAF265, a dual BRAF and VEGFR2 inhibitor, prevents osteoclast formation and resorption. Therapeutic implications. Invest New Drugs. 2013 Feb;31(1):200-5.
Ref 532029Clinical phase I study of elpamotide, a peptide vaccine for vascular endothelial growth factor receptor 2, in patients with advanced solid tumors. Cancer Sci. 2012 Dec;103(12):2135-8.
Ref 532072Vascular normalizing doses of antiangiogenic treatment reprogram the immunosuppressive tumor microenvironment and enhance immunotherapy. Proc Natl Acad Sci U S A. 2012 Oct 23;109(43):17561-6.
Ref 532104Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706.
Ref 532187Anti-angiogenic and anti-tumor effects of TAK-593, a potent and selective inhibitor of vascular endothelial growth factor and platelet-derived growth factor receptor tyrosine kinase. Cancer Sci. 2013Apr;104(4):486-94.
Ref 532210Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
Ref 532338Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe. Bioorg Med Chem Lett. 2013 Jun 1;23(11):3248-52.
Ref 532919Axitinib: VEGF inhibition in advanced thyroid cancer. Lancet Oncol. 2014 Jul;15(8):e310.
Ref 533061Discovery of fruquintinib, a potent and highly selective small molecule inhibitor of VEGFR 1, 2, 3 tyrosine kinases for cancer therapy. Cancer Biol Ther. 2014;15(12):1635-45.
Ref 5331232014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
Ref 534662Synthesis and biological evaluations of 3-substituted indolin-2-ones: a novel class of tyrosine kinase inhibitors that exhibit selectivity toward particular receptor tyrosine kinases. J Med Chem. 1998 Jul 2;41(14):2588-603.
Ref 535250Technology evaluation: IMC-1C11, ImClone Systems. Curr Opin Mol Ther. 2001 Aug;3(4):418-24.
Ref 536137Dose-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 536201YM-359445, an orally bioavailable vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor, has highly potent antitumor activity against established tumors. Clin Cancer Res. 2006 Mar 1;12(5):1630-8.
Ref 536260SU14813: a novel multiple receptor tyrosine kinase inhibitor with potent antiangiogenic and antitumor activity. Mol Cancer Ther. 2006 Jul;5(7):1774-82.
Ref 536402Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2007 Mar;29(2):153-73.
Ref 536474A 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 536839Emerging drugs for ovarian cancer. Expert Opin Emerg Drugs. 2008 Sep;13(3):523-36.
Ref 537551Phase II study of safety and efficacy of motesanib in patients with progressive or symptomatic, advanced or metastatic medullary thyroid cancer. J Clin Oncol. 2009 Aug 10;27(23):3794-801. Epub 2009 Jun 29.
Ref 543499(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: 1813).
Ref 544325Inhibition of VEGFR-2 Reverses Type 1 Diabetes in NOD Mice by Abrogating Insulitis and Restoring Islet Function. Diabetes. 2013 August; 62(8): 2870-2878.
Ref 549698J Clin Oncol 33, 2015 (suppl 3; abstr 65).
Ref 549974Pfizer. Product Development Pipeline. March 31 2009.
Ref 550250Clinical pipeline report, company report or official report of Amgen (2009).
Ref 550288Clinical pipeline report, company report or official report of AstraZeneca (2009).
Ref 550325Clinical pipeline report, company report or official report of AVEO Pharmaceuticals.
Ref 550374Clinical pipeline report, company report or official report of Cyclacel.
Ref 550598Clinical pipeline report, company report or official report of Deciphera Pharmaceuticals.
Ref 550636Clinical pipeline report, company report or official report of Exelixis (2011).
Ref 550989Clinical pipeline report, company report or official report of Hutchison Medi Pharma.
Ref 551087Axitinib for renal cell carcinoma. Expert Opin Investig Drugs. 2008 May;17(5):741-8.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 553086Biochemical characterization of TAK-593, a novel VEGFR/PDGFR inhibitor with a two-step slow binding mechanism. Biochemistry. 2011 Feb 8;50(5):738-51. doi: 10.1021/bi101777f. Epub 2011 Jan 10.
Ref 1572591Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
Ref 1587926URL: https://www.ebi.ac.uk/chembl/ The ChEMBL database in 2017

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