Target
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114]
Ligand
BDBM296351
Substrate
n/a
Meas. Tech.
Enzyme Assay
IC50
124±n/a nM
Citation
 Andrews, SWAronow, SBlake, JFBrandhuber, BJCook, AHaas, JJiang, YKolakowski, GRMcFaddin, EAMcKenney, MLMcNulty, OTMetcalf, ATMoreno, DATang, TPRen, 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]
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:
BDBM296351
Synonyms:
6- (cyclobutylmethoxy)- 4-(6-(4-((6- methoxypyridin- 3- yl)methyl) piperazin-1-yl) pyridin-3- yl)pyrazolo[1,5- a]pyridine-3- carbonitrile | US10112942, Example 84 | US10137124, Example 84 | US10172851, Example 84 | US10555944, Example 84 | US10953005, Example 84
Type:
Small organic molecule
Emp. Form.:
C29H31N7O2
Mol. Mass.:
509.6021
SMILES:
COc1ccc(CN2CCN(CC2)c2ccc(cn2)-c2cc(OCC3CCC3)cn3ncc(C#N)c23)cn1
Structure:
Search PDB for entries with ligand similarity: