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Target
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,V804M]
Ligand
BDBM305707
Substrate
n/a
Meas. Tech.
RET Enzyme Assay
IC50
4.00±n/a nM
Citation
 Andrews, SW; Aronow, S; Blake, JF; Brandhuber, BJ; Collier, J; Cook, A; Haas, J; Jiang, Y; Kolakowski, GR; McFaddin, EA; McKenney, ML; McNulty, OT; Metcalf, AT; Moreno, DA; Ramann, GA; Tang, TP; Ren, L; Walls, SM Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors US Patent  US10441581 Publication Date 10/15/2019 
Target
Name:
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,V804M]
Synonyms:
CDHF12 | CDHR16 | PTC | Proto-oncogene tyrosine-protein kinase receptor Ret (658-end) | Proto-oncogene tyrosine-protein kinase receptor Ret (V804M) | RET | RET Kinase (V804M) (aa658-end) | RET51 | RET_HUMAN
Type:
Enzyme Catalytic Domain
Mol. Mass.:
51567.23
Organism:
Homo sapiens (Human)
Description:
P07949[658-1114,V804M]
Residue:
457
Sequence:
HCYHKFAHKPPISSAEMTFRRPAQAFPVSYSSSGARRPSLDSMENQVSVDAFKILEDPKWEFPRKNLVLGKTLGEGEFGKVVKATAFHLKGRAGYTTVAVKMLKENASPSELRDLLSEFNVLKQVNHPHVIKLYGACSQDGPLLLIMEYAKYGSLRGFLRESRKVGPGYLGSGGSRNSSSLDHPDERALTMGDLISFAWQISQGMQYLAEMKLVHRDLAARNILVAEGRKMKISDFGLSRDVYEEDSYVKRSQGRIPVKWMAIESLFDHIYTTQSDVWSFGVLLWEIVTLGGNPYPGIPPERLFNLLKTGHRMERPDNCSEEMYRLMLQCWKQEPDKRPVFADISKDLEKMMVKRRDYLDLAASTPSDSLIYDDGLSEEETPLVDCNNAPLPRALPSTWIENKLYGMSDPNWPGESPVPLTRADGTNTGFPRYPNDSVYANWMLSPSAAKLMDTFDS
  
Inhibitor
Name:
BDBM305707
Synonyms:
N-((3S,4S)-1-(5-(3-cyano- 6-ethoxypyrazolo[1,5- a]pyridin-4-yl)pyridin-2- yl)-3-hydroxypiperidin-4- yl)-5-fluoro-2- methylbenzamide | US10144734, Example 725 | US10172845, Example 725 | US10441581, Example 725 | US10881652, Example 725 | US11648243, Example 725
Type:
Small organic molecule
Emp. Form.:
C28H27FN6O3
Mol. Mass.:
514.5508
SMILES:
CCOc1cc(-c2ccc(nc2)N2CC[C@H](NC(=O)c3cc(F)ccc3C)[C@@H](O)C2)c2c(cnn2c1)C#N |r|
Structure:
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