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Target
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,V804M]
Ligand
BDBM305417
Substrate
n/a
Meas. Tech.
RET Enzyme Assay
IC50
6.20±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:
BDBM305417
Synonyms:
3-chloro-N-(1-(5-(3- cyano-6- methoxypyrazolo[1,5- a]pyridin-4-yl)pyridin-2- yl)-4-methylpiperidin-4- yl)-5-fluoropicolinamide | US10144734, Example 434 | US10172845, Example 434 | US10441581, Example 434 | US10881652, Example 434 | US11648243, Example 434
Type:
Small organic molecule
Emp. Form.:
C26H23ClFN7O2
Mol. Mass.:
519.958
SMILES:
COc1cc(-c2ccc(nc2)N2CCC(C)(CC2)NC(=O)c2ncc(F)cc2Cl)c2c(cnn2c1)C#N
Structure:
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