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Target
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114]
Ligand
BDBM296812
Substrate
n/a
Meas. Tech.
RET Enzyme Assay
IC50
5.00±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:
BDBM296812
Synonyms:
6-ethoxy-4-(5-(6-(3- fluoro-4- methoxybenzyl)-3,6- diazabicyclo[3.1.1] heptan-3-yl)pyrazin-2- yl)pyrazolo[1,5- a]pyridine-3- carbonitrile | US10112942, Example 547 | US10137124, Example 547 | US10172851, Example 547 | US10555944, Example 547 | US10953005, Example 547
Type:
Small organic molecule
Emp. Form.:
C27H26FN7O2
Mol. Mass.:
499.5394
SMILES:
CCOc1cc(-c2cnc(cn2)N2CC3CC(C2)N3Cc2ccc(OC)c(F)c2)c2c(cnn2c1)C#N
Structure:
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