Reaction Details Report a problem with these data
Target
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,V804M]
Ligand
BDBM305021
Substrate
n/a
Meas. Tech.
A RET Enzyme Assay
IC50
39.3±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,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:
BDBM305021
Synonyms:
4-(6-(4-(4- fluorophenoxy) piperidin-1-yl)pyridin- 3-yl)-6-(2-hydroxy-2- methylpropoxy) pyrazolo[1,5-a] pyridine-3- carbonitrile | US10144734, Example 37 | US10172845, Example 37 | US10441581, Example 37 | US10881652, Example 37 | US11648243, Example 37
Type:
Small organic molecule
Emp. Form.:
C28H28FN5O3
Mol. Mass.:
501.552
SMILES:
CC(C)(O)COc1cc(-c2ccc(nc2)N2CCC(CC2)Oc2ccc(F)cc2)c2c(cnn2c1)C#N
Structure:
Search PDB for entries with ligand similarity: