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Target
Vascular endothelial growth factor receptor 3
Ligand
BDBM16673
Substrate
Poly (E:Y)
Meas. Tech.
Time-resolved fluorescence energy transfer assay
pH
7.5±n/a
Temperature
295.15±n/a K
IC50
20±6 nM
Citation
 Wilhelm, SM; Carter, C; Tang, L; Wilkie, D; McNabola, A; Rong, H; Chen, C; Zhang, X; Vincent, P; McHugh, M; Cao, Y; Shujath, J; Gawlak, S; Eveleigh, D; Rowley, B; Liu, L; Adnane, L; Lynch, M; Auclair, D; Taylor, I; Gedrich, R; Voznesensky, A; Riedl, B; Post, LE; Bollag, G; Trail, PA BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis. Cancer Res 64:7099-109 (2004) [PubMed]  Article 
Target
Name:
Vascular endothelial growth factor receptor 3
Synonyms:
Flt-4 | Flt4 | Fms-like tyrosine kinase 4 | Tyrosine-protein kinase receptor FLT4 | VEGFR-3 | VGFR3_MOUSE | Vegfr3
Type:
Kinase domain
Mol. Mass.:
153007.70
Organism:
Mus musculus (mouse)
Description:
P35917
Residue:
1363
Sequence:
MQPGAALNLRLWLCLGLLQGLANGYSMTPPTLNITEDSYVIDTGDSLSISCRGQHPLEWTWPGAQEVLTTGGKDSEDTRVVHDCEGTEARPYCKVLLLAQTHANNTGSYHCYYKYIKARIEGTTAASTYVFVRDFKHPFINKPDTLLVNRKDSMWVPCLVSIPGLNITLRSQSSALHPDGQEVLWDDRRGMRVPTQLLRDALYLQCETTWGDQNFLSNLFVVHITGNELYDIQLYPKKSMELLVGEKLVLNCTVWAEFDSGVTFDWDYPGKQAERAKWVPERRSQQTHTELSSILTIHNVSQNDLGPYVCEANNGIQRFRESTEVIVHEKPFISVEWLKGPVLEATAGDELVKLPVKLAAYPPPEFQWYKDRKAVTGRHNPHALVLKEVTEASAGVYTLALWNSAAGLRQNISLELVVNVPPHIHEKEASSPSIYSRHSRQTLTCTAYGVPQPLSVQWHWRPWTPCKTFAQRSLRRRQQRDGMPQCRDWKEVTTQDAVNPIESLDSWTEFVEGKNKTVSKLVIQDANVSAMYKCVVVNKVGQDERLIYFYVTTIPDGFSIESEPSEDPLEGQSVRLSCRADNYTYEHLRWYRLNLSTLHDAQGNPLLLDCKNVHLFATPLEANLEEAEPGARHATLSLNIPRVAPEDEGDYVCEVQDRRSQDKHCHKKYLSVQALEAPRLTQNLTDLLVNVSDSLEMRCPVAGAHVPSIVWYKDERLLEKESGIDLADSNQRLSIQRVREEDAGRYLCSVCNAKGCVNSSASVAVEGSEDKGSMEIVILIGTGVIAVFFWVLLLLIFCNMKRPAHADIKTGYLSIIMDPGEVPLEEQCEYLSYDASQWEFPRERLHLGRVLGHGAFGKVVEASAFGINKGSSCDTVAVKMLKEGATASEHRALMSELKILIHIGNHLNVVNLLGACTKPNGPLMVIVEFCKYGNLSNFLRVKRDTFNPYAEKSPEQRRRFRAMVEGAKADRRRPGSSDRALFTRFLMGKGSARRAPLVQEAEDLWLSPLTMEDLVCYSFQVARGMEFLASRKCIHRDLAARNILLSESDIVKICDFGLARDIYKDPDYVRKGSARLPLKWMAPESIFDKVYTTQSDVWSFGVLLWEIFSLGASPYPGVQINEEFCQRLKDGTRMRAPELATPAIRHIMQSCWSGDPKARPAFSDLVEILGDLLQGGGWQEEEEERMALHSSQSSEEDGFMQASTTALHITEADADDSPPSMHCHSLAARYYNCVSFPGRLARGTKTPGSSRMKTFEELPMTPTTYKASMDNQTDSGMVLASEEFEELESRHRPEGSFSCKGPGQHMDIPRGHPDPQGRRRRPTQGAQGGKVFYNNEYGEVSQPCTEGDCCPSAGSTFFADSSY
  
Inhibitor
Name:
BDBM16673
Synonyms:
4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)phenoxy]-N-methylpyridine-2-carboxamide | 4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]phenoxy]-N-methyl-picolinamide;tosylic acid | BAY 43-9006 | BAY 439006 | BAY439006 | CHEMBL1336 | Hit compound, 8 | Nexavar | Sorafenib | Sorafenib, 4 | US10183928, Sorafenib | US10202365, Compound Sorafenib | US10227329, Compound Sorafenib | US10584114, Compound Sorafenib | US10774070, Compound Sorafenib | US10980809, Example Sorafenib | US11279688, Compound Sorafenib | US11505527, Compound Sorafenib | US9029401, Sorafenib | US9469639, Sorafenib | US9902709, Comparative example 1 | Xarelto | cid_216239
Type:
Small organic molecule
Emp. Form.:
C21H16ClF3N4O3
Mol. Mass.:
464.825
SMILES:
CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(c3)C(F)(F)F)cc2)ccn1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Poly (E:Y)
Synonyms:
poly GT-biotin
Type:
Random copolymer
Mol. Mass.:
358.43
Organism:
n/a
Description:
n/a
Residue:
3
Sequence:
NA