Target Information
Target General Infomation | |||||
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Target ID |
T40474
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Former ID |
TTDC00110
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Target Name |
Hepatocyte growth factor receptor
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Gene Name |
MET
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Synonyms |
C-Met receptor tyrosine kinase; C-met; HGF receptor; HGF-SF receptor; Met proto-oncogene tyrosine kinase; MET
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Target Type |
Successful
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Disease | ALK-positive advanced or metastatic NSCLC [ICD9: 162; ICD10: C33, C34] | ||||
Alzheimer disease [ICD9: 331; ICD10: G30] | |||||
Advanced solid tumor [ICD9: 140-199; ICD10: C00-C75, C7A, C7B] | |||||
Advanced cancers [ICD9: 140-229; ICD10: C00-C96] | |||||
Chemotherapy-induced mucositis [ICD9: 528; ICD10: K12.3] | |||||
Cancer [ICD9: 140-229; ICD10: C00-C96] | |||||
Fibrosis [ICD9: 709.2; ICD10: L90.5] | |||||
Gastric cancer; Renal cell carcinoma; Squamous cell cancer of head and neck [ICD9: 140-229, 151, 189; ICD10: C16, C64] | |||||
Hepatocellular carcinoma [ICD9: 155; ICD10: C22.0] | |||||
Heart disease [ICD9: 390-429; ICD10: I00-I52] | |||||
Head and neck cancer [ICD9: 140-149, 140-229; ICD10: C07-C14, C32-C33] | |||||
Liver disease [ICD9: 570-574; ICD10: K70-K77] | |||||
Metastatic HER2-negative gastric cancer; Non-small cell lung cancer [ICD9:140-229, 151; ICD10: C16, C33-C34] | |||||
Medullary thyroid cancer [ICD9: 193; ICD10: C73] | |||||
Metastatic castration-resistant prostate cancer; Ovarian cancer [ICD9: 140-229, 183, 185; ICD10: C56, C61] | |||||
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48] | |||||
Thyroid cancer; Renal cell carcinoma [ICD9: 140-229, 189, 193; ICD10: C64, C73] | |||||
Function |
Acts as a receptor for Listeria internalin inlB, mediating entry of the pathogen into cells.
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BioChemical Class |
Kinase
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Target Validation |
T40474
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UniProt ID | |||||
EC Number |
EC 2.7.10.1
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Sequence |
MKAPAVLAPGILVLLFTLVQRSNGECKEALAKSEMNVNMKYQLPNFTAETPIQNVILHEH
HIFLGATNYIYVLNEEDLQKVAEYKTGPVLEHPDCFPCQDCSSKANLSGGVWKDNINMAL VVDTYYDDQLISCGSVNRGTCQRHVFPHNHTADIQSEVHCIFSPQIEEPSQCPDCVVSAL GAKVLSSVKDRFINFFVGNTINSSYFPDHPLHSISVRRLKETKDGFMFLTDQSYIDVLPE FRDSYPIKYVHAFESNNFIYFLTVQRETLDAQTFHTRIIRFCSINSGLHSYMEMPLECIL TEKRKKRSTKKEVFNILQAAYVSKPGAQLARQIGASLNDDILFGVFAQSKPDSAEPMDRS AMCAFPIKYVNDFFNKIVNKNNVRCLQHFYGPNHEHCFNRTLLRNSSGCEARRDEYRTEF TTALQRVDLFMGQFSEVLLTSISTFIKGDLTIANLGTSEGRFMQVVVSRSGPSTPHVNFL LDSHPVSPEVIVEHTLNQNGYTLVITGKKITKIPLNGLGCRHFQSCSQCLSAPPFVQCGW CHDKCVRSEECLSGTWTQQICLPAIYKVFPNSAPLEGGTRLTICGWDFGFRRNNKFDLKK TRVLLGNESCTLTLSESTMNTLKCTVGPAMNKHFNMSIIISNGHGTTQYSTFSYVDPVIT SISPKYGPMAGGTLLTLTGNYLNSGNSRHISIGGKTCTLKSVSNSILECYTPAQTISTEF AVKLKIDLANRETSIFSYREDPIVYEIHPTKSFISGGSTITGVGKNLNSVSVPRMVINVH EAGRNFTVACQHRSNSEIICCTTPSLQQLNLQLPLKTKAFFMLDGILSKYFDLIYVHNPV FKPFEKPVMISMGNENVLEIKGNDIDPEAVKGEVLKVGNKSCENIHLHSEAVLCTVPNDL LKLNSELNIEWKQAISSTVLGKVIVQPDQNFTGLIAGVVSISTALLLLLGFFLWLKKRKQ IKDLGSELVRYDARVHTPHLDRLVSARSVSPTTEMVSNESVDYRATFPEDQFPNSSQNGS CRQVQYPLTDMSPILTSGDSDISSPLLQNTVHIDLSALNPELVQAVQHVVIGPSSLIVHF NEVIGRGHFGCVYHGTLLDNDGKKIHCAVKSLNRITDIGEVSQFLTEGIIMKDFSHPNVL SLLGICLRSEGSPLVVLPYMKHGDLRNFIRNETHNPTVKDLIGFGLQVAKGMKYLASKKF VHRDLAARNCMLDEKFTVKVADFGLARDMYDKEYYSVHNKTGAKLPVKWMALESLQTQKF TTKSDVWSFGVLLWELMTRGAPPYPDVNTFDITVYLLQGRRLLQPEYCPDPLYEVMLKCW HPKAEMRPSFSELVSRISAIFSTFIGEHYVHVNATYVNVKCVAPYPSLLSSEDNADDEVD TRPASFWETS |
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Structure |
1FYR; 1R0P; 1R1W; 1SHY; 1SSL; 1UX3; 2G15; 2RFN; 2RFS; 2UZX; 2UZY; 2WD1; 2WGJ; 2WKM; 3A4P; 3BUX; 3C1X; 3CCN; 3CD8; 3CE3; 3CTH; 3CTJ; 3DKC; 3DKF; 3DKG; 3EFJ; 3EFK; 3F66; 3F82; 3I5N; 3L8V; 3LQ8; 3Q6U; 3Q6W; 3QTI; 3R7O; 3RHK; 3U6H; 3U6I; 3VW8; 3ZBX; 3ZC5; 3ZCL; 3ZXZ; 3ZZE; 4AOI; 4AP7; 4DEG; 4DEH; 4DEI; 4EEV; 4GG5; 4GG7; 4IWD; 4K3J; 4KNB; 4MXC; 4O3T; 4O3U
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Drugs and Mode of Action | |||||
Drug(s) | Cabozantinib | Drug Info | Approved | Medullary thyroid cancer | [1], [2] |
Crizotinib | Drug Info | Approved | ALK-positive advanced or metastatic NSCLC | [3], [4] | |
Beperminogene perplasmid | Drug Info | Phase 3 | Heart disease | [5] | |
RG3638 | Drug Info | Phase 3 | Metastatic HER2-negative gastric cancer; Non-small cell lung cancer | [6] | |
Tivantinib | Drug Info | Phase 3 | Solid tumours | [7], [8] | |
AMG 208 | Drug Info | Phase 2 | Solid tumours | [9] | |
AMG 337 | Drug Info | Phase 2 | Cancer | [10] | |
Cabozantinib | Drug Info | Phase 2 | Metastatic castration-resistant prostate cancer; Ovarian cancer | [1], [2] | |
HM-5016504 | Drug Info | Phase 2 | Cancer | [11] | |
INCB28060 | Drug Info | Phase 2 | Hepatocellular carcinoma | [12] | |
LY-2875358 | Drug Info | Phase 2 | Cancer | [13] | |
LY2801653 | Drug Info | Phase 2 | Cancer | [14] | |
SAR-125844 | Drug Info | Phase 2 | Solid tumours | [15] | |
Volitinib | Drug Info | Phase 2 | Solid tumours | [11] | |
XL880 | Drug Info | Phase 2 | Gastric cancer; Renal cell carcinoma; Squamous cell cancer of head and neck | [16], [17] | |
BMS-777607 | Drug Info | Phase 1/2 | Discovery agent | [18], [19] | |
ChronSeal | Drug Info | Phase 1/2 | Fibrosis | [20] | |
MK-2461 | Drug Info | Phase 1/2 | Alzheimer disease | [21] | |
MSC2156119 | Drug Info | Phase 1/2 | Cancer | [22] | |
Cabozantinib | Drug Info | Phase 1b | Thyroid cancer; Renal cell carcinoma | [1], [2] | |
ABT-700 | Drug Info | Phase 1 | Advanced solid tumor | [23] | |
Altiratinib | Drug Info | Phase 1 | Solid tumours | [24] | |
E-7050 | Drug Info | Phase 1 | Head and neck cancer | [25], [26] | |
EMD-1204831 | Drug Info | Phase 1 | Solid tumours | [27] | |
EMD-1214063 | Drug Info | Phase 1 | Solid tumours | [28], [29] | |
Hepapoietin | Drug Info | Phase 1 | Liver disease | [30] | |
JNJ-38877605 | Drug Info | Phase 1 | Solid tumours | [31] | |
LY3164530 | Drug Info | Phase 1 | Advanced cancers | [32] | |
Merestinib, LY2801653 | Drug Info | Phase 1 | Cancer | [33] | |
MGCD516 | Drug Info | Phase 1 | Solid tumours | [34] | |
MK-8033 | Drug Info | Phase 1 | Solid tumours | [35] | |
PF-4217903 | Drug Info | Phase 1 | Cancer | [36] | |
SGX523 | Drug Info | Phase 1 | Solid tumours | [37], [38] | |
XL880 | Drug Info | Phase 1 | Solid tumours | [16], [17] | |
Mteron-F1 | Drug Info | Preclinical | Chemotherapy-induced mucositis | [39] | |
Inhibitor | 1-(2-nitrophenethyl)-1H-pyrrolo[3,2-b]pyridine | Drug Info | [40] | ||
1-(phenylsulfonyl)-1H-pyrrolo[3,2-b]pyridine | Drug Info | [40] | |||
1-benzyl-1H-pyrrolo[3,2-b]pyridine | Drug Info | [40] | |||
3-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridine | Drug Info | [40] | |||
Altiratinib | Drug Info | [41] | |||
AM7 | Drug Info | [42] | |||
Anti-cMET mab | Drug Info | [43] | |||
APS-3010 | Drug Info | [43] | |||
BAY-85-3474 | Drug Info | [43] | |||
BMS-536924 | Drug Info | [44] | |||
BMS-777607 | Drug Info | [45] | |||
C-Met kinase inhibitors | Drug Info | [43] | |||
Cabozantinib | Drug Info | [2] | |||
ChronSeal | Drug Info | [46] | |||
CMET Avimer polypeptides | Drug Info | [43] | |||
compound 16 | Drug Info | [47] | |||
compound 1o | Drug Info | [48] | |||
compound 27 | Drug Info | [49] | |||
compound R-16 | Drug Info | [50] | |||
DP-3590 | Drug Info | [43] | |||
EMD-1204831 | Drug Info | [51] | |||
Hepapoietin | Drug Info | [52] | |||
HM-5016504 | Drug Info | [43] | |||
JNJ-38877605 | Drug Info | [53] | |||
MG-516 | Drug Info | [43] | |||
MGCD516 | Drug Info | [54] | |||
MK-2461 | Drug Info | [21] | |||
MK-8033 | Drug Info | [55] | |||
MSC2156119 | Drug Info | [56] | |||
PF-00614435 | Drug Info | [43] | |||
PF-4217903 | Drug Info | [57] | |||
PHA-665752 | Drug Info | [43] | |||
PRS-110 | Drug Info | [43] | |||
RP-1040 | Drug Info | [43] | |||
SAR-125844 | Drug Info | [58] | |||
SGX523 | Drug Info | [59] | |||
SU11274 | Drug Info | [60] | |||
Tivantinib | Drug Info | [8] | |||
TP-801 | Drug Info | [43] | |||
Modulator | ABT-700 | Drug Info | [61] | ||
AMG 208 | Drug Info | [62] | |||
AMG 337 | Drug Info | [63] | |||
Beperminogene perplasmid | Drug Info | [64] | |||
Crizotinib | Drug Info | [65] | |||
E-7050 | Drug Info | [66] | |||
EMD-1214063 | Drug Info | [67] | |||
GE-137 | Drug Info | [68] | |||
INCB28060 | Drug Info | [69] | |||
LY2801653 | Drug Info | [70], [71] | |||
LY3164530 | Drug Info | [72] | |||
Merestinib, LY2801653 | Drug Info | [73] | |||
RG3638 | Drug Info | [43] | |||
Volitinib | Drug Info | [74] | |||
XL880 | Drug Info | [75] | |||
Stimulator | Mteron-F1 | Drug Info | [39] | ||
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 | |||||
Axon guidance | |||||
Focal adhesion | |||||
Adherens junction | |||||
Bacterial invasion of epithelial cells | |||||
Epithelial cell signaling in Helicobacter pylori infection | |||||
Malaria | |||||
Pathways in cancer | |||||
Transcriptional misregulation in cancer | |||||
Proteoglycans in cancer | |||||
MicroRNAs in cancer | |||||
Renal cell carcinoma | |||||
Melanoma | |||||
Central carbon metabolism in cancer | |||||
Pathway Interaction Database | Signaling events mediated by Hepatocyte Growth Factor Receptor (c-Met) | ||||
Arf6 signaling events | |||||
Signaling events mediated by TCPTP | |||||
Posttranslational regulation of adherens junction stability and dissassembly | |||||
Direct p53 effectors | |||||
Syndecan-1-mediated signaling events | |||||
Stabilization and expansion of the E-cadherin adherens junction | |||||
a6b1 and a6b4 Integrin signaling | |||||
FGF signaling pathway | |||||
Regulation of retinoblastoma protein | |||||
Reactome | Sema4D mediated inhibition of cell attachment and migration | ||||
WikiPathways | TGF beta Signaling Pathway | ||||
Signaling of Hepatocyte Growth Factor Receptor | |||||
Focal Adhesion | |||||
Extracellular vesicle-mediated signaling in recipient cells | |||||
Signaling Pathways in Glioblastoma | |||||
miR-targeted genes in squamous cell - TarBase | |||||
miR-targeted genes in muscle cell - TarBase | |||||
miR-targeted genes in lymphocytes - TarBase | |||||
miR-targeted genes in epithelium - TarBase | |||||
Semaphorin interactions | |||||
References | |||||
REF 1 | (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 2 | Clinical pipeline report, company report or official report of Exelixis (2011). | ||||
REF 3 | (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: 4903). | ||||
REF 4 | 2011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4. | ||||
REF 5 | ClinicalTrials.gov (NCT02144610) Safety and Efficacy of Subjects With Critical Limb Ischemia. U.S. National Institutes of Health. | ||||
REF 6 | ClinicalTrials.gov (NCT02488330) An Extension Study of Onartuzumab in Patients With Solid Tumors on Study Treatment Previously Enrolled in a Company Sponsored Study. | ||||
REF 7 | A phase II trial of a selective c-Met inhibitor tivantinib (ARQ 197) monotherapy as a second- or third-line therapy in the patients with metastatic gastric cancer. Invest New Drugs. 2014 Apr;32(2):355-61. | ||||
REF 8 | (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: 7948). | ||||
REF 9 | ClinicalTrials.gov (NCT02420587) AMG 208 Tumor Microenvironment in Metastatic Castration Resistant Prostate Cancer (mCRPC). U.S. National Institutes of Health. | ||||
REF 10 | ClinicalTrials.gov (NCT02016534) Phase 2 Study of AMG 337 in MET Amplified Gastric/Esophageal Adenocarcinoma or Other Solid Tumors. U.S. National Institutes of Health. | ||||
REF 11 | ClinicalTrials.gov (NCT02127710) A Phase II Trial to Evaluate the Efficacy of AZD6094 (HMPL-504) in Patients With Papillary Renal Cell Carcinoma (PRCC). U.S. National Institutes of Health. | ||||
REF 12 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031741) | ||||
REF 13 | ClinicalTrials.gov (NCT01900652) A Study of LY2875358 in Non Small Cell Lung Cancer (NSCLC) Participants. U.S. National Institutes of Health. | ||||
REF 14 | ClinicalTrials.gov (NCT01285037) A Study of LY2801653 in Advanced Cancer. U.S. National Institutes of Health. | ||||
REF 15 | ClinicalTrials.gov (NCT02435121) A Study Assessing Efficacy and Safety of SAR125844 in NSCLC Patients With MET Amplification. U.S. National Institutes of Health. | ||||
REF 16 | (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 17 | Clinical pipeline report, company report or official report of Exelixis (2011). | ||||
REF 18 | ClinicalTrials.gov (NCT00605618) Multiple Ascending Dose Study of BMS-777607 in Subjects With Advanced or Metastatic Solid Tumors. U.S. National Institutes of Health. | ||||
REF 19 | (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: 7953). | ||||
REF 20 | ClinicalTrials.gov (NCT00797706) Phase I/II Dose Ranging CHRONSEAL Study in Venous Leg Ulcers. U.S. National Institutes of Health. | ||||
REF 21 | MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33. | ||||
REF 22 | ClinicalTrials.gov (NCT01982955) MSC2156119J With Gefitinib in Subjects With Advanced Non-small Cell Lung Cancer. U.S. National Institutes of Health. | ||||
REF 23 | ClinicalTrials.gov (NCT01472016) Study of ABT-700 in Subjects With Advanced Solid Tumors. U.S. National Institutes of Health. | ||||
REF 24 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800040094) | ||||
REF 25 | ClinicalTrials.gov (NCT02533102) Pharmacokinetics and Food Effect of Single Oral Dose of E7050 in Healthy Volunteers. | ||||
REF 26 | (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 27 | ClinicalTrials.gov (NCT01110083) First-in-Man, Dose-escalation Trial of c-Met Kinase Inhibitor EMD 1204831 in Subjects With Advanced Solid Tumors. U.S. National Institutes of Health. | ||||
REF 28 | ClinicalTrials.gov (NCT01014936) First-in-Man, Dose-escalation Trial of C-met Kinase Inhibitor MSC2156119J in Subjects With Advanced Solid Tumors. U.S. National Institutes of Health. | ||||
REF 29 | (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: 8293). | ||||
REF 30 | Pharmacokinetics and biochemical effects of hepapoietin in patients with chronic liver disease. Aliment Pharmacol Ther. 2002 Feb;16(2):235-42. | ||||
REF 31 | ClinicalTrials.gov (NCT00651365) A Safety and Dose-finding Study of JNJ-38877605 in Patients With Advanced or Refractory Solid Tumors.. U.S. National Institutes of Health. | ||||
REF 32 | ClinicalTrials.gov (NCT02221882) A Study of LY3164530 in Participants With Cancer | ||||
REF 33 | Clinical pipeline report, company report or official report of Eli Lilly. | ||||
REF 34 | ClinicalTrials.gov (NCT02219711) Phase 1/1b Study of MGCD516 in Patients With Advanced Cancer. U.S. National Institutes of Health. | ||||
REF 35 | ClinicalTrials.gov (NCT00559182) A Study of MK-8033 in Patients With Advanced Solid Tumors (MK-8033-001). U.S. National Institutes of Health. | ||||
REF 36 | ClinicalTrials.gov (NCT00706355) A Study of PF-04217903 in Patients With Advanced Cancer. U.S. National Institutes of Health. | ||||
REF 37 | ClinicalTrials.gov (NCT00607399) Safety Study of SGX523, a Small Molecule Met Inhibitor, to Treat Solid Tumors. U.S. National Institutes of Health. | ||||
REF 38 | (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: 5709). | ||||
REF 39 | Emerging drugs for chemotherapy-induced mucositis. Expert Opin Emerg Drugs. 2008 Sep;13(3):511-22. | ||||
REF 40 | Bioorg Med Chem Lett. 2009 May 15;19(10):2780-4. Epub 2009 Mar 27.Discovery of 4-azaindoles as novel inhibitors of c-Met kinase. | ||||
REF 41 | Clinical pipeline report, company report or official report of Deciphera Pharmaceuticals. | ||||
REF 42 | c-Met inhibitors with novel binding mode show activity against several hereditary papillary renal cell carcinoma-related mutations. J Biol Chem. 2008 Feb 1;283(5):2675-83. Epub 2007 Nov 30. | ||||
REF 43 | (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: 1815). | ||||
REF 44 | J 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 45 | J Med Chem. 2009 Mar 12;52(5):1251-4.Discovery of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a selective and orally efficacious inhibitor of the Met kinase superfamily. | ||||
REF 46 | Clinical pipeline report, company report or official report of Kringle Pharma. | ||||
REF 47 | Pyrrolo-pyrimidones: a novel class of MK2 inhibitors with potent cellular activity. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6142-6. | ||||
REF 48 | Design and synthesis of novel 3-(benzo[d]oxazol-2-yl)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine derivatives as selective G-protein-coupled receptor kinase-2 and -5 inhibitors. Bioorg Med Chem Lett. 2013 Dec 15;23(24):6711-6. | ||||
REF 49 | Fused bicyclic derivatives of 2,4-diaminopyrimidine as c-Met inhibitors. Bioorg Med Chem Lett. 2011 Jan 1;21(1):164-7. | ||||
REF 50 | Improvement in oral bioavailability of 2,4-diaminopyrimidine c-Met inhibitors by incorporation of a 3-amidobenzazepin-2-one group. Bioorg Med Chem. 2011 Nov 1;19(21):6274-84. | ||||
REF 51 | 2012 ASCO Annual Meeting. | ||||
REF 52 | Pharmacokinetics and biochemical effects of hepapoietin in patients with chronic liver disease. Alimentary Pharmacology & Therapeutics Volume 16, Issue 2, pages 235-242, February 2002. | ||||
REF 53 | The c-Met Tyrosine Kinase Inhibitor JNJ-38877605 Causes Renal Toxicity through Species-Specific Insoluble Metabolite Formation. Clin Cancer Res. 2015 May 15;21(10):2297-304. | ||||
REF 54 | Role and relevance of TrkB mutations and expression in non-small cell lung cancer. Clin Cancer Res. 2011 May 1;17(9):2638-45. | ||||
REF 55 | A novel c-Met inhibitor, MK8033, synergizes with carboplatin plus paclitaxel to inhibit ovarian cancer cell growth. Oncol Rep. 2013 May;29(5):2011-8. | ||||
REF 56 | Identification and optimization of pyridazinones as potent and selective c-Met kinase inhibitors. Bioorg Med Chem Lett. 2015 Apr 1;25(7):1597-602. | ||||
REF 57 | Sensitivity of selected human tumor models to PF-04217903, a novel selective c-Met kinase inhibitor. Mol Cancer Ther. 2012 Apr;11(4):1036-47. | ||||
REF 58 | The selective intravenous inhibitor of the MET tyrosine kinase SAR125844 inhibits tumor growth in MET-amplified cancer. Mol Cancer Ther. 2015 Feb;14(2):384-94. | ||||
REF 59 | CenterWatch. Drugs in Clinical Trials Database. CenterWatch. 2008. | ||||
REF 60 | Potent and selective inhibitors of the Met [hepatocyte growth factor/scatter factor (HGF/SF) receptor] tyrosine kinase block HGF/SF-induced tumor cell growth and invasion. Mol Cancer Ther. 2003 Nov;2(11):1085-92. | ||||
REF 61 | J Clin Oncol 32:5s, 2014 (suppl; abstr 2507). | ||||
REF 62 | A first-in-human study of AMG 208, an oral MET inhibitor, in adult patients with advanced solid tumors. Oncotarget. 2015 Jul 30;6(21):18693-706. | ||||
REF 63 | J Clin Oncol 32:5s, 2014 (suppl; abstr 2508). | ||||
REF 64 | Beperminogene perplasmid for the treatment of critical limb ischemia. Expert Rev Cardiovasc Ther. 2014 Oct;12(10):1145-56. | ||||
REF 65 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | ||||
REF 66 | E7050: 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 67 | EMD 1214063 and EMD 1204831 constitute a new class of potent and highly selective c-Met inhibitors. Clin Cancer Res. 2013 Jun 1;19(11):2941-51. | ||||
REF 68 | Detection of colorectal polyps in humans using an intravenously administered fluorescent peptide targeted against c-Met. Nat Med. 2015 Aug;21(8):955-61. | ||||
REF 69 | National Cancer Institute Drug Dictionary (drug id 666907). | ||||
REF 70 | LY2801653 is an orally bioavailable multi-kinase inhibitor with potent activity against MET, MST1R, and other oncoproteins, and displays anti-tumor activities in mouse xenograft models. Invest New Drugs. 2013 Aug;31(4):833-44. | ||||
REF 71 | Clinical pipeline report, company report or official report of Eli Lilly. | ||||
REF 72 | Bispecific antibodies rise again. Nat Rev Drug Discov. 2014 Nov;13(11):799-801. doi: 10.1038/nrd4478. | ||||
REF 73 | The c-Met inhibitors: a new class of drugs in the battle against advanced nonsmall-cell lung cancer. Curr Pharm Des. 2012;18(37):6155-68. | ||||
REF 74 | Clinical pipeline report, company report or official report of Hutchison Medi Pharma. | ||||
REF 75 | Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41. |
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