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Target
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114]
Ligand
BDBM305385
Substrate
n/a
Meas. Tech.
A RET Enzyme Assay
IC50
11.7±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:
BDBM305385
Synonyms:
6-(2-(1-methylazetidin-3- yl)ethoxy)-4-(6-(4- (pyridin-2-yloxy)piperidin- 1-yl)pyridin-3- yl)pyrazolo[1,5-a]pyridine- 3-carbonitrile | US10144734, Example 402 | US10172845, Example 402 | US10441581, Example 402 | US10881652, Example 402 | US11648243, Example 402
Type:
Small organic molecule
Emp. Form.:
C29H31N7O2
Mol. Mass.:
509.6021
SMILES:
CN1CC(CCOc2cc(-c3ccc(nc3)N3CCC(CC3)Oc3ccccn3)c3c(cnn3c2)C#N)C1
Structure:
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