Target
Proto-oncogene tyrosine-protein kinase receptor Ret
Ligand
BDBM296696
Substrate
n/a
Meas. Tech.
RET Enzyme Assay
pH
7.4±n/a
IC50
4.50±n/a nM
Comments
extracted
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  US10112942 Publication Date 10/30/2018 
Target
Name:
Proto-oncogene tyrosine-protein kinase receptor Ret
Synonyms:
CDHF12 | CDHR16 | Cadherin family member 12 | PTC | Proto-oncogene c-Ret | RET | RET51 | RET_HUMAN | Tyrosine-protein kinase Ret (RET)
Type:
Protein
Mol. Mass.:
124318.29
Organism:
Homo sapiens (Human)
Description:
P07949
Residue:
1114
Sequence:
MAKATSGAAGLRLLLLLLLPLLGKVALGLYFSRDAYWEKLYVDQAAGTPLLYVHALRDAPEEVPSFRLGQHLYGTYRTRLHENNWICIQEDTGLLYLNRSLDHSSWEKLSVRNRGFPLLTVYLKVFLSPTSLREGECQWPGCARVYFSFFNTSFPACSSLKPRELCFPETRPSFRIRENRPPGTFHQFRLLPVQFLCPNISVAYRLLEGEGLPFRCAPDSLEVSTRWALDREQREKYELVAVCTVHAGAREEVVMVPFPVTVYDEDDSAPTFPAGVDTASAVVEFKRKEDTVVATLRVFDADVVPASGELVRRYTSTLLPGDTWAQQTFRVEHWPNETSVQANGSFVRATVHDYRLVLNRNLSISENRTMQLAVLVNDSDFQGPGAGVLLLHFNVSVLPVSLHLPSTYSLSVSRRARRFAQIGKVCVENCQAFSGINVQYKLHSSGANCSTLGVVTSAEDTSGILFVNDTKALRRPKCAELHYMVVATDQQTSRQAQAQLLVTVEGSYVAEEAGCPLSCAVSKRRLECEECGGLGSPTGRCEWRQGDGKGITRNFSTCSPSTKTCPDGHCDVVETQDINICPQDCLRGSIVGGHEPGEPRGIKAGYGTCNCFPEEEKCFCEPEDIQDPLCDELCRTVIAAAVLFSFIVSVLLSAFCIHCYHKFAHKPPISSAEMTFRRPAQAFPVSYSSSGARRPSLDSMENQVSVDAFKILEDPKWEFPRKNLVLGKTLGEGEFGKVVKATAFHLKGRAGYTTVAVKMLKENASPSELRDLLSEFNVLKQVNHPHVIKLYGACSQDGPLLLIVEYAKYGSLRGFLRESRKVGPGYLGSGGSRNSSSLDHPDERALTMGDLISFAWQISQGMQYLAEMKLVHRDLAARNILVAEGRKMKISDFGLSRDVYEEDSYVKRSQGRIPVKWMAIESLFDHIYTTQSDVWSFGVLLWEIVTLGGNPYPGIPPERLFNLLKTGHRMERPDNCSEEMYRLMLQCWKQEPDKRPVFADISKDLEKMMVKRRDYLDLAASTPSDSLIYDDGLSEEETPLVDCNNAPLPRALPSTWIENKLYGMSDPNWPGESPVPLTRADGTNTGFPRYPNDSVYANWMLSPSAAKLMDTFDS
  
Inhibitor
Name:
BDBM296696
Synonyms:
US10112942, Example 431 | US10137124, Example 431 | US10172851, Example 431 | US10555944, Example 431 | US10953005, Example 431
Type:
Small organic molecule
Emp. Form.:
C28H29N7O3
Mol. Mass.:
511.575
SMILES:
COCCOc1cc(-c2ccc(nc2)N2CC3CC(C2)N3Cc2ccc(OC)nc2)c2c(cnn2c1)C#N
Structure:
Search PDB for entries with ligand similarity: