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Target
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114]
Ligand
BDBM315816
Substrate
n/a
Meas. Tech.
RET Enzyme Assay
IC50
10.6±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  US10172851 Publication Date 1/8/2019 
Target
Name:
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114]
Synonyms:
CDHF12 | CDHR16 | PTC | Proto-oncogene tyrosine-protein kinase receptor Ret | Proto-oncogene tyrosine-protein kinase receptor Ret (aa 658-1114) | RET | RET Kinase (aa 658-1114) | RET51 | RET_HUMAN
Type:
n/a
Mol. Mass.:
51535.16
Organism:
Homo sapiens (Human)
Description:
P07949[658-1114]
Residue:
457
Sequence:
HCYHKFAHKPPISSAEMTFRRPAQAFPVSYSSSGARRPSLDSMENQVSVDAFKILEDPKWEFPRKNLVLGKTLGEGEFGKVVKATAFHLKGRAGYTTVAVKMLKENASPSELRDLLSEFNVLKQVNHPHVIKLYGACSQDGPLLLIVEYAKYGSLRGFLRESRKVGPGYLGSGGSRNSSSLDHPDERALTMGDLISFAWQISQGMQYLAEMKLVHRDLAARNILVAEGRKMKISDFGLSRDVYEEDSYVKRSQGRIPVKWMAIESLFDHIYTTQSDVWSFGVLLWEIVTLGGNPYPGIPPERLFNLLKTGHRMERPDNCSEEMYRLMLQCWKQEPDKRPVFADISKDLEKMMVKRRDYLDLAASTPSDSLIYDDGLSEEETPLVDCNNAPLPRALPSTWIENKLYGMSDPNWPGESPVPLTRADGTNTGFPRYPNDSVYANWMLSPSAAKLMDTFDS
  
Inhibitor
Name:
BDBM315816
Synonyms:
US10172851, Example 459
Type:
Small organic molecule
Emp. Form.:
C29H29N7O3
Mol. Mass.:
523.5857
SMILES:
COc1ccc(CN2C3CC2CN(C3)c2ccc(cn2)-c2cc(OC3CC(O)C3)cn3ncc(C#N)c23)cn1 |(12.28,-2.37,;10.95,-1.6,;9.61,-2.37,;8.28,-1.6,;6.94,-2.37,;6.94,-3.91,;5.61,-4.68,;4.28,-3.91,;2.94,-4.68,;2.94,-3.14,;4.28,-2.37,;2.94,-1.6,;1.61,-2.37,;1.61,-3.91,;.28,-1.6,;-1.06,-2.37,;-2.39,-1.6,;-2.39,-.06,;-1.06,.71,;.28,-.06,;-3.72,.71,;-5.06,-.06,;-6.39,.71,;-7.73,-.06,;-9.06,.71,;-10.55,.31,;-10.95,1.8,;-12.28,2.57,;-9.46,2.19,;-6.39,2.25,;-5.06,3.02,;-4.74,4.52,;-3.21,4.68,;-2.58,3.28,;-1.09,2.88,;.39,2.48,;-3.72,2.25,;8.28,-4.68,;9.61,-3.91,)|
Structure:
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