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Target
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]
Ligand
BDBM296520
Substrate
n/a
Meas. Tech.
RET G810R Mutant Assay
IC50
104±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:
BDBM296520
Synonyms:
US10112942, Example 254 | US10137124, Example 254 | US10172851, Example 254 | US10555944, Example 254 | US10953005, Example 254
Type:
Small organic molecule
Emp. Form.:
C27H26ClN7O2
Mol. Mass.:
515.994
SMILES:
CCOc1cc(-c2ccc(nc2)N2CCN(CC2)C(=O)[C@H](N)c2cccc(Cl)c2)c2c(cnn2c1)C#N |r|
Structure:
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