Target
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114]
Ligand
BDBM296212
Substrate
n/a
Meas. Tech.
RET Enzyme Assay
IC50
11.4±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  US10172851 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:
BDBM296212
Synonyms:
US10112942, Example 19 | US10137124, Example 19 | US10172851, Example 19 | US10555944, Example 19 | US10953005, Example 19
Type:
Small organic molecule
Emp. Form.:
C30H33N7O
Mol. Mass.:
507.6293
SMILES:
CN1CC(CCOc2cc(-c3ccc(nc3)N3CCN(Cc4ccccc4)CC3)c3c(cnn3c2)C#N)C1
Structure:
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