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Target
Proto-oncogene tyrosine-protein kinase receptor Ret
Ligand
BDBM50458624
Substrate
n/a
Meas. Tech.
ChEMBL_1764323 (CHEMBL4199570)
IC50
0.700000±n/a nM
Citation
 Schenck Eidam, H; Russell, J; Raha, K; DeMartino, M; Qin, D; Guan, HA; Zhang, Z; Zhen, G; Yu, H; Wu, C; Pan, Y; Joberty, G; Zinn, N; Laquerre, S; Robinson, S; White, A; Giddings, A; Mohammadi, E; Greenwood-Van Meerveld, B; Oliff, A; Kumar, S; Cheung, M Discovery of a First-in-Class Gut-Restricted RET Kinase Inhibitor as a Clinical Candidate for the Treatment of IBS. ACS Med Chem Lett 9:623-628 (2018) [PubMed]  Article 
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:
BDBM50458624
Synonyms:
CHEMBL4205803
Type:
Small organic molecule
Emp. Form.:
C27H31F3N6O
Mol. Mass.:
512.5698
SMILES:
CCN1CCN(Cc2ccc(NC(=O)Nc3ccc(cc3)-c3ccc(NC)nc3)cc2C(F)(F)F)CC1
Structure:
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