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Target
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114]
Ligand
BDBM305327
Substrate
n/a
Meas. Tech.
A RET Enzyme Assay
IC50
15.1±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  US10172845 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:
BDBM305327
Synonyms:
N-(1-(5-(3-cyano-6- ethoxypyrazolo[1,5- a]pyridin-4-yl)pyridin-2- yl)-4- (hydroxymethyl)piperidin- 4-yl)-3-fluoropicolinamide | US10144734, Example 343 | US10172845, Example 343 | US10441581, Example 343 | US10881652, Example 343 | US11648243, Example 343
Type:
Small organic molecule
Emp. Form.:
C27H26FN7O3
Mol. Mass.:
515.5388
SMILES:
CCOc1cc(-c2ccc(nc2)N2CCC(CO)(CC2)NC(=O)c2ncccc2F)c2c(cnn2c1)C#N
Structure:
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