Target
Proto-oncogene tyrosine-protein kinase receptor Ret
Ligand
BDBM305776
Substrate
n/a
Meas. Tech.
Enzyme Assay
IC50
5.00±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  US10881652 Publication Date 1/5/2021 
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:
BDBM305776
Synonyms:
2-chloro-N-(1-(5-(3- cyano-6- methoxypyrazolo[1,5- a]pyridin-4-yl)pyrazin-2- yl)-4-methylpiperidin-4- yl)-5-fluorobenzamide | US10144734, Example 794 | US10172845, Example 794 | US10441581, Example 794 | US10881652, Example 794 | US11648243, Example 794
Type:
Small organic molecule
Emp. Form.:
C26H23ClFN7O2
Mol. Mass.:
519.958
SMILES:
COc1cc(-c2cnc(cn2)N2CCC(C)(CC2)NC(=O)c2cc(F)ccc2Cl)c2c(cnn2c1)C#N
Structure:
Search PDB for entries with ligand similarity: