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Target
Proto-oncogene tyrosine-protein kinase receptor Ret
Ligand
BDBM347313
Substrate
n/a
Meas. Tech.
ChEMBL_1764327 (CHEMBL4199574)
IC50
9.4±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:
BDBM347313
Synonyms:
2-(4-(4-Ethoxy-6-oxo-1,6-dihydropyridin-3-yl)-2-fluorophenyl)-N-(4-(3-hydroxy-2,2-dimethylpropyl)-3-(trifluoromethyl)phenyl)acetamide | US9789100, Example 3
Type:
Small organic molecule
Emp. Form.:
C27H28F4N2O4
Mol. Mass.:
520.5158
SMILES:
CCOc1cc(=O)[nH]cc1-c1ccc(CC(=O)Nc2ccc(CC(C)(C)CO)c(c2)C(F)(F)F)c(F)c1
Structure:
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