Reaction Details Report a problem with these data
Target
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]
Ligand
BDBM296818
Substrate
n/a
Meas. Tech.
RET G810R Mutant Assay
IC50
153±n/a nM
Citation
 Andrews, SW; Aronow, S; Blake, JF; Brandhuber, BJ; Cook, A; Haas, J; Jiang, Y; Kolakowski, GR; McFaddin, EA; McKenney, ML; McNulty, OT; Metcalf, AT; Moreno, DA; Tang, TP; Ren, L Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors US Patent  US10555944 Publication Date 2/11/2020 
Target
Name:
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R]
Synonyms:
CDHF12 | CDHR16 | PTC | Proto-oncogene tyrosine-protein kinase receptor Ret (G810R) | RET | RET51 | RET_HUMAN
Type:
Enzyme Catalytic Domain
Mol. Mass.:
51635.31
Organism:
Homo sapiens (Human)
Description:
P07949[658-1114,G810R]
Residue:
457
Sequence:
HCYHKFAHKPPISSAEMTFRRPAQAFPVSYSSSGARRPSLDSMENQVSVDAFKILEDPKWEFPRKNLVLGKTLGEGEFGKVVKATAFHLKGRAGYTTVAVKMLKENASPSELRDLLSEFNVLKQVNHPHVIKLYGACSQDGPLLLIVEYAKYRSLRGFLRESRKVGPGYLGSGGSRNSSSLDHPDERALTMGDLISFAWQISQGMQYLAEMKLVHRDLAARNILVAEGRKMKISDFGLSRDVYEEDSYVKRSQGRIPVKWMAIESLFDHIYTTQSDVWSFGVLLWEIVTLGGNPYPGIPPERLFNLLKTGHRMERPDNCSEEMYRLMLQCWKQEPDKRPVFADISKDLEKMMVKRRDYLDLAASTPSDSLIYDDGLSEEETPLVDCNNAPLPRALPSTWIENKLYGMSDPNWPGESPVPLTRADGTNTGFPRYPNDSVYANWMLSPSAAKLMDTFDS
  
Inhibitor
Name:
BDBM296818
Synonyms:
US10112942, Example 553 | US10137124, Example 553 | US10172851, Example 553 | US10555944, Example 553 | US10953005, Example 553
Type:
Small organic molecule
Emp. Form.:
C28H28FN9O2
Mol. Mass.:
541.5794
SMILES:
COc1ccc(CN2C3CC2CN(C3)c2cnc(cn2)-c2cc(OCC3(F)CNC3)cn3ncc(C#N)c23)cn1
Structure:
Search PDB for entries with ligand similarity: