Target
Proto-oncogene tyrosine-protein kinase receptor Ret [G810R]
Ligand
BDBM305730
Substrate
n/a
Meas. Tech.
RET G810R Mutant Assay
IC50
1999±n/a nM
Citation
 Andrews, SWAronow, SBlake, JFBrandhuber, BJCollier, JCook, AHaas, JJiang, YKolakowski, GRMcFaddin, EAMcKenney, MLMcNulty, OTMetcalf, ATMoreno, DARamann, GATang, TPRen, LWalls, SM Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors US Patent  US10144734 Publication Date 12/4/2018 
Target
Name:
Proto-oncogene tyrosine-protein kinase receptor Ret [G810R]
Synonyms:
CDHF12 | CDHR16 | PTC | Proto-oncogene tyrosine-protein kinase receptor Ret (G810R) | RET | RET Kinase (G810R) | RET kinase mutant (G810R) | RET51 | RET_HUMAN | ret enzyme (g810r)
Type:
Enzyme Catalytic Domain
Mol. Mass.:
124418.43
Organism:
Homo sapiens (Human)
Description:
P07949[G810R]
Residue:
1114
Sequence:
MAKATSGAAGLRLLLLLLLPLLGKVALGLYFSRDAYWEKLYVDQAAGTPLLYVHALRDAPEEVPSFRLGQHLYGTYRTRLHENNWICIQEDTGLLYLNRSLDHSSWEKLSVRNRGFPLLTVYLKVFLSPTSLREGECQWPGCARVYFSFFNTSFPACSSLKPRELCFPETRPSFRIRENRPPGTFHQFRLLPVQFLCPNISVAYRLLEGEGLPFRCAPDSLEVSTRWALDREQREKYELVAVCTVHAGAREEVVMVPFPVTVYDEDDSAPTFPAGVDTASAVVEFKRKEDTVVATLRVFDADVVPASGELVRRYTSTLLPGDTWAQQTFRVEHWPNETSVQANGSFVRATVHDYRLVLNRNLSISENRTMQLAVLVNDSDFQGPGAGVLLLHFNVSVLPVSLHLPSTYSLSVSRRARRFAQIGKVCVENCQAFSGINVQYKLHSSGANCSTLGVVTSAEDTSGILFVNDTKALRRPKCAELHYMVVATDQQTSRQAQAQLLVTVEGSYVAEEAGCPLSCAVSKRRLECEECGGLGSPTGRCEWRQGDGKGITRNFSTCSPSTKTCPDGHCDVVETQDINICPQDCLRGSIVGGHEPGEPRGIKAGYGTCNCFPEEEKCFCEPEDIQDPLCDELCRTVIAAAVLFSFIVSVLLSAFCIHCYHKFAHKPPISSAEMTFRRPAQAFPVSYSSSGARRPSLDSMENQVSVDAFKILEDPKWEFPRKNLVLGKTLGEGEFGKVVKATAFHLKGRAGYTTVAVKMLKENASPSELRDLLSEFNVLKQVNHPHVIKLYGACSQDGPLLLIVEYAKYRSLRGFLRESRKVGPGYLGSGGSRNSSSLDHPDERALTMGDLISFAWQISQGMQYLAEMKLVHRDLAARNILVAEGRKMKISDFGLSRDVYEEDSYVKRSQGRIPVKWMAIESLFDHIYTTQSDVWSFGVLLWEIVTLGGNPYPGIPPERLFNLLKTGHRMERPDNCSEEMYRLMLQCWKQEPDKRPVFADISKDLEKMMVKRRDYLDLAASTPSDSLIYDDGLSEEETPLVDCNNAPLPRALPSTWIENKLYGMSDPNWPGESPVPLTRADGTNTGFPRYPNDSVYANWMLSPSAAKLMDTFDS
  
Inhibitor
Name:
BDBM305730
Synonyms:
4-(6-(4-(4-fluorobenzyl)- 4-hydroxypiperidin-1- yl)pyridin-3-yl)-6-(2- hydroxy-2- methylpropoxy) pyrazolo[1,5-a] pyridine-3-carbonitrile | US10144734, Example 748 | US10172845, Example 748 | US10441581, Example 748 | US10881652, Example 748 | US11648243, Example 748
Type:
Small organic molecule
Emp. Form.:
C29H30FN5O3
Mol. Mass.:
515.5786
SMILES:
CC(C)(O)COc1cc(-c2ccc(nc2)N2CCC(O)(Cc3ccc(F)cc3)CC2)c2c(cnn2c1)C#N
Structure:
Search PDB for entries with ligand similarity: