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MET proto-oncogene, receptor tyrosine kinase

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Target id: 1815

Nomenclature: MET proto-oncogene, receptor tyrosine kinase

Abbreviated Name: MET

Family: Type X RTKs: HGF (hepatocyte growth factor) receptor family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 1390 7q31 MET MET proto-oncogene, receptor tyrosine kinase
Mouse 1 1379 6 7.83 cM Met met proto-oncogene
Rat 1 1382 4q21 Met MET proto-oncogene, receptor tyrosine kinase
Previous and Unofficial Names Click here for help
RCCP2 | c-Met | HGF receptor | HGF/SF receptor | scatter factor receptor | Par4 | hepatocyte growth factor receptor | mesenchymal-epithelial transition factor (c-Met) receptor | MET proto-oncogene
Database Links Click here for help
Alphafold P08581 (Hs), P16056 (Mm), P97523 (Rn)
BRENDA 2.7.10.1
CATH/Gene3D 2.60.40.10, 2.130.10.10
ChEMBL Target CHEMBL3717 (Hs), CHEMBL5585 (Mm)
DrugBank Target P08581 (Hs)
Ensembl Gene ENSG00000105976 (Hs), ENSMUSG00000009376 (Mm), ENSRNOG00000052745 (Rn)
Entrez Gene 4233 (Hs), 17295 (Mm)
Human Protein Atlas ENSG00000105976 (Hs)
KEGG Enzyme 2.7.10.1
KEGG Gene hsa:4233 (Hs), mmu:17295 (Mm)
OMIM 164860 (Hs)
Orphanet ORPHA123201 (Hs)
Pharos P08581 (Hs)
RefSeq Nucleotide NM_000245 (Hs), NM_008591 (Mm), NM_031517 (Rn)
RefSeq Protein NP_000236 (Hs), NP_032617 (Mm), NP_113705 (Rn)
SynPHARM 81931 (in complex with AM7)
78753 (in complex with crizotinib)
79023 (in complex with crizotinib)
81202 (in complex with foretinib)
79050 (in complex with foretinib)
84917 (in complex with merestinib)
84918 (in complex with merestinib)
81064 (in complex with SGX-523)
81205 (in complex with SGX-523)
83121 (in complex with tepotinib)
UniProtKB P08581 (Hs), P16056 (Mm), P97523 (Rn)
Wikipedia MET (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  x-ray structure of c-Met with inhibitor.
PDB Id:  2RFN
Ligand:  AM7
Resolution:  2.5Å
Species:  Human
References:  4
Image of receptor 3D structure from RCSB PDB
Description:  CRYSTAL STRUCTURE OF THE TYROSINE KINASE DOMAIN OF THE HEPATOCYTE GROWTH FACTOR RECEPTOR C-MET
PDB Id:  1R1W
Resolution:  1.8Å
Species:  Human
References:  44
Image of receptor 3D structure from RCSB PDB
Description:  Identification and optimization of pyridazinones as potent and selective c-Met kinase inhibitors.
PDB Id:  4R1V
Ligand:  tepotinib
Resolution:  1.2Å
Species:  Human
References:  20
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of c-Met in complex with triazolopyridazine inhibitor 2.
PDB Id:  4DEG
Ligand:  AMG-337
Resolution:  2.0Å
Species:  Human
References:  7
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of c-Met in complex with LY2801653 (merestinib).
PDB Id:  4EEV
Ligand:  merestinib
Resolution:  1.8Å
Species:  Human
References:  55
Enzyme Reaction Click here for help
EC Number: 2.7.10.1
Natural/Endogenous Ligands Click here for help
hepatocyte growth factor {Sp: Human}

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Activators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
terevalefim Small molecule or natural product Hs Activation - - 9
⤷ [9]
Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
SGX-523 Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Inhibition 9.7 pKd 19
⤷ pKd 9.7 (Kd 1.9x10-10 M) [19]
PHA-665752 Small molecule or natural product Primary target of this compound Hs Inhibition 9.6 pKd 19
⤷ pKd 9.6 (Kd 2.7x10-10 M) [19]
foretinib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.9 pKd 19
⤷ pKd 8.9 (Kd 1.4x10-9 M) [19]
crizotinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 8.7 pKi 17
⤷ pKi 8.7 (Ki 2x10-9 M) [17]
merestinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 8.7 pKi 55
⤷ pKi 8.7 (Ki 2x10-9 M) [55]
PHA-665752 Small molecule or natural product Primary target of this compound Hs Inhibition 8.4 pKi 14
⤷ pKi 8.4 (Ki 4x10-9 M) [14]
pamufetinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.4 pKi 22
⤷ pKi 7.4 (Ki 3.9x10-8 M) [22]
tivantinib Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Inhibition 6.4 pKi 37
⤷ pKi 6.4 (Ki 3.55x10-7 M) [37]
capmatinib Small molecule or natural product Approved drug Primary target of this compound Hs Inhibition 9.9 pIC50 33
⤷ pIC50 9.9 (IC50 1.3x10-10 M) [33]
vilzemetkib Small molecule or natural product Hs Inhibition 9.8 pIC50 12
⤷ pIC50 9.8 (IC50 1.74x10-10 M) [12]
gumarontinib Small molecule or natural product Hs Inhibition 9.4 pIC50 1
⤷ pIC50 9.4 (IC50 4.2x10-10 M) [1]
Description: Inhibition of the kinase activity of purified c-Met using ELISA kinase assay.
foretinib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 9.3 – 9.4 pIC50 32,38
⤷ pIC50 9.3 – 9.4 (IC50 5x10-10 – 4x10-10 M) [32,38]
ensartinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 9.1 pIC50 34
⤷ pIC50 9.1 (IC50 7.4x10-10 M) [34]
Description: Result from DiscoveRx KINOMEscan® selectivity screen.
elzovantinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 9.1 pIC50 16
⤷ pIC50 9.1 (IC50 7.6x10-10 M) [16]
crizotinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 9.1 pIC50 48
⤷ pIC50 9.1 (IC50 7.8x10-10 M) [48]
cabozantinib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.9 pIC50 54
⤷ pIC50 8.9 (IC50 1.3x10-9 M) [54]
MK-2461 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.6 pIC50 40
⤷ pIC50 8.6 (IC50 2.5x10-9 M) [40]
altiratinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Guide to Malaria Pharmacology Ligand Hs Inhibition 8.6 pIC50 21
⤷ pIC50 8.6 (IC50 2.7x10-9 M) [21]
dalmelitinib Small molecule or natural product Hs Inhibition 8.5 pIC50 57
⤷ pIC50 8.5 (IC50 2.9x10-9 M) [57]
Description: Determined in a biochemical enzyme inhibition assay
D6808 Small molecule or natural product Ligand has a PDB structure Hs Inhibition 8.5 pIC50 49
⤷ pIC50 8.5 (IC50 2.9x10-9 M) [49]
tepotinib Small molecule or natural product Approved drug Primary target of this compound Ligand has a PDB structure Hs Inhibition 8.5 pIC50 6
⤷ pIC50 8.5 (IC50 3x10-9 M) [6]
Description: Measured in a flash-plate assay using recombinant human c-Met kinase domain and a biotinylated peptide substrate.
vabametkib Small molecule or natural product Hs Inhibition 8.5 pIC50 28
⤷ pIC50 8.5 (IC50 3x10-9 M) [28]
OMO-1 Small molecule or natural product Hs Inhibition 7.9 – 9.0 pIC50 35
⤷ pIC50 9.0 (IC50 1x10-9 M) [35]
Description: Inhibition of c-Met autophosphorylation measured in a time resolved fluorescence assay (DELFIA).
pIC50 7.9 (IC50 1.2x10-8 M) [35]
Description: Inhibition of HGF stimulated c-Met phosphorylation in a cell-based assay.
BMS-777607 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.4 pIC50 46
⤷ pIC50 8.4 (IC50 3.9x10-9 M) [46]
SGX-523 Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Inhibition 8.4 pIC50 10
⤷ pIC50 8.4 (IC50 4x10-9 M) [10]
merestinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 8.3 pIC50 55
⤷ pIC50 8.3 (IC50 4.7x10-9 M) [55]
Description: Inhibition of in vitro biochemical activity by EMD Millipore assay.
AMG-337 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.3 pIC50 8
⤷ pIC50 8.3 (IC50 5x10-9 M) [8]
Description: Biochemically assessed value.
savolitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibition 8.3 pIC50 29
⤷ pIC50 8.3 (IC50 5x10-9 M) [29]
compound 1o [PMID: 24210504] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.1 pIC50 13
⤷ pIC50 8.1 (IC50 8x10-9 M) [13]
SU11274 Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Inhibition 8.0 pIC50 50
⤷ pIC50 8.0 (IC50 1x10-8 M) [50]
Description: Assay used a GST fusion with the cytoplasmic domain of human Met.
compound 27 [PMID: 21123062] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.0 pIC50 51
⤷ pIC50 8.0 (IC50 1x10-8 M) [51]
zanzalintinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition >8.0 pIC50 3
⤷ pIC50 >8.0 (IC50 <1x10-8 M) [3]
Description: Inhibition of substrate phosphorylation by human c-MET (residues R974-S1390 with A1209G and V1290L) in vitro
golvatinib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.8 pIC50 39
⤷ pIC50 7.8 (IC50 1.4x10-8 M) [39]
Description: Measured as inhibition of c-MET phosphorylation in MKN45 cells
compound 19a [PMID: 30503936] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.8 pIC50 43
⤷ pIC50 7.8 (IC50 1.5x10-8 M) [43]
AM7 Small molecule or natural product Ligand has a PDB structure Hs Inhibition 7.8 pIC50 4
⤷ pIC50 7.8 (IC50 1.7x10-8 M) [4]
ningetinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.7 pIC50 53
⤷ pIC50 7.7 (IC50 1.9x10-8 M) [53]
sitravatinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.7 pIC50 41
⤷ pIC50 7.7 (IC50 2x10-8 M) [41]
Description: In a biochemical enzyme activity assay.
compound R-16 [PMID: 21967808] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.6 pIC50 36
⤷ pIC50 7.6 (IC50 2.4x10-8 M) [36]
glesatinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.5 pIC50 15
⤷ pIC50 7.5 (IC50 2.9x10-8 M) [15]
compound 16 [PMID: 18945615] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.1 pIC50 45
⤷ pIC50 7.1 (IC50 8.5x10-8 M) [45]
compound 8i [PMID: 22765894] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.3 pIC50 56
⤷ pIC50 6.3 (IC50 4.63x10-7 M) [56]
RIPK3 inhibitor 18 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 6.0 pIC50 24
⤷ pIC50 6.0 (IC50 1.1x10-6 M) [24]
alectinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition <5.3 pIC50 30
⤷ pIC50 <5.3 (IC50 >5x10-6 M) [30]
vebreltinib Small molecule or natural product Hs Inhibition - - 25
⤷ [25]
Description: PLB-1001 inhibited MET activity by 95% in a LANCE enzyme assay
Inhibitor Comments
Tepotinib was shown to have an IC50 of <1nM in an in vitro study with recombinant human MET [20]. Tanespimycin is reported as a femtomolar inhibitor of MET-induced urokinase plasminogen activation (uPA) pathway [47].
Antibodies
Key to terms and symbols Click column headers to sort
Antibody Sp. Action Value Parameter Reference
amivantamab Peptide Approved drug Primary target of this compound Click here for species-specific activity table Hs Binding 10.4 pKd 27
⤷ pKd 10.4 (Kd 4x10-11 M) [27]
Description: Binding affinity determined by surface plasmon resonance.
emibetuzumab Peptide Primary target of this compound Hs Binding >10.0 pKd 18
⤷ pKd >10.0 (Kd <1x10-10 M) [18]
Description: binding constant for hMET extracellular domain measured using proprietary BIACore® technology
onartuzumab Peptide Primary target of this compound Hs Binding 8.4 pIC50 26,31
⤷ pIC50 8.4 (IC50 4.3x10-9 M) [26,31]
Other Binding Ligands
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Value Parameter Reference
GE-137 Peptide Primary target of this compound Ligand is labelled Hs Binding 8.5 pKd 11
⤷ pKd 8.5 (Kd 3x10-9 M) [11]
Description: In vitro fluorescence polarization assay.
DiscoveRx KINOMEscan® screen Click here for help
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan
Reference: 19,52
Key to terms and symbols Click column headers to sort
Target used in screen: MET
Ligand Sp. Type Action Value Parameter
SGX-523 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.7 pKd
PHA-665752 Small molecule or natural product Hs Inhibitor Inhibition 9.6 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.9 pKd
crizotinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.7 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 6.8 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.8 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.7 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.6 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.5 pKd
cediranib Small molecule or natural product Hs Inhibitor Inhibition 6.4 pKd
Target used in screen: MET(M1250T)
Ligand Sp. Type Action Value Parameter
crizotinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 9.3 pKd
PHA-665752 Small molecule or natural product Hs Inhibitor Inhibition 9.2 pKd
SGX-523 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.1 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.0 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.2 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 7.0 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.9 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 6.7 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.6 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.3 pKd
Target used in screen: MET(Y1235D)
Ligand Sp. Type Action Value Parameter
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.1 pKd
PHA-665752 Small molecule or natural product Hs Inhibitor Inhibition 9.1 pKd
crizotinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.8 pKd
SGX-523 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.4 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.4 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.8 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.7 pKd
tozasertib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.4 pKd
cediranib Small molecule or natural product Hs Inhibitor Inhibition 6.3 pKd
Ki-20227 Small molecule or natural product Hs Inhibitor Inhibition 6.3 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen Click here for help
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.

http://www.millipore.com/techpublications/tech1/pf3036
http://www.reactionbiology.com/webapps/main/pages/kinase.aspx

Reference: 2,23
Key to terms and symbols Click column headers to sort
Target used in screen: Met/c-MET
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
SU11274 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 1.2 2.0 0.0
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 32.7 4.0 1.0
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 40.4 3.0 0.0
K-252a Small molecule or natural product Hs Inhibitor Inhibition 53.2 6.0 13.0
PDGF RTK inhibitor Small molecule or natural product Hs Inhibitor Inhibition 60.4 28.0 4.0
GSK-3beta inhibitor I Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 64.2 141.0 95.0
GSK-3 inhibitor IX Small molecule or natural product Hs Inhibitor Inhibition 70.0 118.0 97.0
tozasertib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 70.9
erlotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 71.4
Cdk2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 73.2 122.0 85.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Immunopharmacology Comments
The leucine-rich repeat (LRR)-containing protein InlB of Listeria monocytogenes is reported to mediate bacterial entry in to non-phagocytic host cells by binding to the MET proto-oncogene, receptor tyrosine kinase (MET, or hepatocyte growth factor receptor, HGFR) [5]. Tanespimycin (a potent inhibitor of MET [47], in addition to Hsp90) has reported efficacy against intracellular infection of non-phagocytic cells by L. monocytogenes [42].
Immuno Process Associations
Immuno Process:  Barrier integrity
Immuno Process:  Cytokine production & signalling
Immuno Process:  Inflammation
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Pediatric hepatocellular carcinoma
Disease Ontology: DOID:684
OMIM: 114550
Orphanet: ORPHA33402
Disease:  Renal cell carcinoma, papillary, 1; RCCP1
Synonyms: Hereditary papillary renal cell carcinoma [Orphanet: ORPHA47044]
Papillary renal cell carcinoma [Disease Ontology: DOID:4465]
Disease Ontology: DOID:4465
OMIM: 605074
Orphanet: ORPHA47044

References

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2. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat Biotechnol, 29 (11): 1039-45. [PMID:22037377]

3. Bannen LC, Bui M, Jiang F, Tso K, Wang Y, Xu W. (2019) Compounds for the treatment of kinase-dependent disorders. Patent number: WO2019148044A1. Assignee: Exelixis, Inc.. Priority date: 26/01/2018. Publication date: 01/08/2019.

4. Bellon SF, Kaplan-Lefko P, Yang Y, Zhang Y, Moriguchi J, Rex K, Johnson CW, Rose PE, Long AM, O'Connor AB et al.. (2008) c-Met inhibitors with novel binding mode show activity against several hereditary papillary renal cell carcinoma-related mutations. J Biol Chem, 283 (5): 2675-83. [PMID:18055465]

5. Bierne H, Cossart P. (2002) InlB, a surface protein of Listeria monocytogenes that behaves as an invasin and a growth factor. J Cell Sci, 115 (Pt 17): 3357-67. [PMID:12154067]

6. Bladt F, Faden B, Friese-Hamim M, Knuehl C, Wilm C, Fittschen C, Grädler U, Meyring M, Dorsch D, Jaehrling F et al.. (2013) EMD 1214063 and EMD 1204831 constitute a new class of potent and highly selective c-Met inhibitors. Clin Cancer Res, 19 (11): 2941-51. [PMID:23553846]

7. Bode CM, Boezio AA, Albrecht BK, Bellon SF, Berry L, Broome MA, Choquette D, Dussault I, Lewis RT, Lin MH et al.. (2012) Discovery and optimization of a potent and selective triazolopyridinone series of c-Met inhibitors. Bioorg Med Chem Lett, 22 (12): 4089-93. [PMID:22595176]

8. Boezio AA, Berry L, Albrecht BK, Bauer D, Bellon SF, Bode C, Chen A, Choquette D, Dussault I, Fang M et al.. (2009) Discovery and optimization of potent and selective triazolopyridazine series of c-Met inhibitors. Bioorg Med Chem Lett, 19 (22): 6307-12. [PMID:19819693]

9. Bromberg JS, Weir MR, Gaber AO, Yamin MA, Goldberg ID, Mayne TJ, Cal W, Cooper M. (2021) Renal Function Improvement Following ANG-3777 Treatment in Patients at High Risk for Delayed Graft Function After Kidney Transplantation. Transplantation, 105 (2): 443-450. [PMID:32265417]

10. Buchanan SG, Hendle J, Lee PS, Smith CR, Bounaud PY, Jessen KA, Tang CM, Huser NH, Felce JD, Froning KJ et al.. (2009) SGX523 is an exquisitely selective, ATP-competitive inhibitor of the MET receptor tyrosine kinase with antitumor activity in vivo. Mol Cancer Ther, 8 (12): 3181-90. [PMID:19934279]

11. Burggraaf J, Kamerling IM, Gordon PB, Schrier L, de Kam ML, Kales AJ, Bendiksen R, Indrevoll B, Bjerke RM, Moestue SA et al.. (2015) Detection of colorectal polyps in humans using an intravenously administered fluorescent peptide targeted against c-Met. Nat Med, 21 (8): 955-61. [PMID:26168295]

12. Chen GP. (2012) Compounds As c-Met Kinase Inhibitors. Patent number: US20120123126A1. Assignee: Chen GP. Priority date: 08/09/2011. Publication date: 17/05/2012.

13. Cho SY, Lee BH, Jung H, Yun CS, Ha JD, Kim HR, Chae CH, Lee JH, Seo HW, Oh KS. (2013) 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, 23 (24): 6711-6. [PMID:24210504]

14. Christensen JG, Schreck R, Burrows J, Kuruganti P, Chan E, Le P, Chen J, Wang X, Ruslim L, Blake R et al.. (2003) A selective small molecule inhibitor of c-Met kinase inhibits c-Met-dependent phenotypes in vitro and exhibits cytoreductive antitumor activity in vivo. Cancer Res, 63 (21): 7345-55. [PMID:14612533]

15. Claridge S, Raeppel F, Granger MC, Bernstein N, Saavedra O, Zhan L, Llewellyn D, Wahhab A, Deziel R, Rahil J et al.. (2008) Discovery of a novel and potent series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases. Bioorg Med Chem Lett, 18 (9): 2793-8. [PMID:18434145]

16. Cui JJ, Rogers EW, Ung J, Whitten J, Zhai D, Deng W, Zhang X, Huang Z, Liu J, Zhang H. (2019) Macrocyclic compounds and uses thereof. Patent number: WO2019023417A1. Assignee: Tp Therapeutics, Inc.. Priority date: 28/07/2017. Publication date: 31/01/2019.

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How to cite this page

Type X RTKs: HGF (hepatocyte growth factor) receptor family: MET proto-oncogene, receptor tyrosine kinase. Last modified on 06/03/2024. Accessed on 19/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=1815.