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Target
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]
Ligand
BDBM296725
Substrate
n/a
Meas. Tech.
RET G810R Mutant Assay
IC50
208±n/a nM
Citation
 Andrews, SW; Aronow, S; Blake, JF; Brandhuber, BJ; Cook, A; Haas, J; Jiang, Y; Kolakowski, GR; McFaddin, EA; McKenney, ML; McNulty, OT; Metcalf, AT; Moreno, DA; Tang, TP; Ren, L Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors US Patent  US10555944 Publication Date 2/11/2020 
Target
Name:
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]
Synonyms:
CDHF12 | CDHR16 | PTC | Proto-oncogene tyrosine-protein kinase receptor Ret (G810R) | RET | RET51 | RET_HUMAN
Type:
Enzyme Catalytic Domain
Mol. Mass.:
51635.31
Organism:
Homo sapiens (Human)
Description:
P07949[658-1114,G810R]
Residue:
457
Sequence:
HCYHKFAHKPPISSAEMTFRRPAQAFPVSYSSSGARRPSLDSMENQVSVDAFKILEDPKWEFPRKNLVLGKTLGEGEFGKVVKATAFHLKGRAGYTTVAVKMLKENASPSELRDLLSEFNVLKQVNHPHVIKLYGACSQDGPLLLIVEYAKYRSLRGFLRESRKVGPGYLGSGGSRNSSSLDHPDERALTMGDLISFAWQISQGMQYLAEMKLVHRDLAARNILVAEGRKMKISDFGLSRDVYEEDSYVKRSQGRIPVKWMAIESLFDHIYTTQSDVWSFGVLLWEIVTLGGNPYPGIPPERLFNLLKTGHRMERPDNCSEEMYRLMLQCWKQEPDKRPVFADISKDLEKMMVKRRDYLDLAASTPSDSLIYDDGLSEEETPLVDCNNAPLPRALPSTWIENKLYGMSDPNWPGESPVPLTRADGTNTGFPRYPNDSVYANWMLSPSAAKLMDTFDS
  
Inhibitor
Name:
BDBM296725
Synonyms:
US10112942, Example 460 | US10137124, Example 460 | US10172851, Example 460 | US10555944, Example 460 | US10953005, Example 460
Type:
Small organic molecule
Emp. Form.:
C30H31N7O3
Mol. Mass.:
537.6122
SMILES:
COc1ccc(CN2C3CC2CN(C3)c2ccc(cn2)-c2cc(OC[C@@H]3C[C@H](O)C3)cn3ncc(C#N)c23)cn1 |r,wU:25.27,27.30,(12.95,-2.37,;11.61,-1.6,;10.28,-2.37,;8.94,-1.6,;7.61,-2.37,;7.61,-3.91,;6.28,-4.68,;4.94,-3.91,;3.61,-4.68,;3.61,-3.14,;4.94,-2.37,;3.61,-1.6,;2.28,-2.37,;2.28,-3.91,;.94,-1.6,;-.39,-2.37,;-1.72,-1.6,;-1.72,-.06,;-.39,.71,;.94,-.06,;-3.06,.71,;-4.39,-.06,;-5.72,.71,;-7.06,-.06,;-8.39,.71,;-9.73,-.06,;-11.21,.34,;-11.61,-1.15,;-12.95,-1.92,;-10.12,-1.55,;-5.72,2.25,;-4.39,3.02,;-4.07,4.52,;-2.54,4.68,;-1.91,3.28,;-.43,2.88,;1.06,2.48,;-3.06,2.25,;8.94,-4.68,;10.28,-3.91,)|
Structure:
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