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Target
Proto-oncogene tyrosine-protein kinase receptor Ret [V804M]
Ligand
BDBM16673
Substrate
n/a
Meas. Tech.
RET Wild Type Assay at KM
IC50
32.4±n/a nM
Citation
 Brubaker, JD; Guzi, T; Wilson, KJ; Dipietro, LV; Zhang, Y; Wilson, D; Fleming, PE Compounds useful for treating disorders related to RET US Patent  US10227329 Publication Date 3/12/2019 
Target
Name:
Proto-oncogene tyrosine-protein kinase receptor Ret [V804M]
Synonyms:
CDHF12 | CDHR16 | PTC | Proto-oncogene tyrosine-protein kinase receptor Ret (V804M) | RET | RET kinase mutant (V804M) | RET51 | RET_HUMAN | ret enzyme (v804m)
Type:
Enzyme Catalytic Domain
Mol. Mass.:
124350.36
Organism:
Homo sapiens (Human)
Description:
P07949[V804M]
Residue:
1114
Sequence:
MAKATSGAAGLRLLLLLLLPLLGKVALGLYFSRDAYWEKLYVDQAAGTPLLYVHALRDAPEEVPSFRLGQHLYGTYRTRLHENNWICIQEDTGLLYLNRSLDHSSWEKLSVRNRGFPLLTVYLKVFLSPTSLREGECQWPGCARVYFSFFNTSFPACSSLKPRELCFPETRPSFRIRENRPPGTFHQFRLLPVQFLCPNISVAYRLLEGEGLPFRCAPDSLEVSTRWALDREQREKYELVAVCTVHAGAREEVVMVPFPVTVYDEDDSAPTFPAGVDTASAVVEFKRKEDTVVATLRVFDADVVPASGELVRRYTSTLLPGDTWAQQTFRVEHWPNETSVQANGSFVRATVHDYRLVLNRNLSISENRTMQLAVLVNDSDFQGPGAGVLLLHFNVSVLPVSLHLPSTYSLSVSRRARRFAQIGKVCVENCQAFSGINVQYKLHSSGANCSTLGVVTSAEDTSGILFVNDTKALRRPKCAELHYMVVATDQQTSRQAQAQLLVTVEGSYVAEEAGCPLSCAVSKRRLECEECGGLGSPTGRCEWRQGDGKGITRNFSTCSPSTKTCPDGHCDVVETQDINICPQDCLRGSIVGGHEPGEPRGIKAGYGTCNCFPEEEKCFCEPEDIQDPLCDELCRTVIAAAVLFSFIVSVLLSAFCIHCYHKFAHKPPISSAEMTFRRPAQAFPVSYSSSGARRPSLDSMENQVSVDAFKILEDPKWEFPRKNLVLGKTLGEGEFGKVVKATAFHLKGRAGYTTVAVKMLKENASPSELRDLLSEFNVLKQVNHPHVIKLYGACSQDGPLLLIMEYAKYGSLRGFLRESRKVGPGYLGSGGSRNSSSLDHPDERALTMGDLISFAWQISQGMQYLAEMKLVHRDLAARNILVAEGRKMKISDFGLSRDVYEEDSYVKRSQGRIPVKWMAIESLFDHIYTTQSDVWSFGVLLWEIVTLGGNPYPGIPPERLFNLLKTGHRMERPDNCSEEMYRLMLQCWKQEPDKRPVFADISKDLEKMMVKRRDYLDLAASTPSDSLIYDDGLSEEETPLVDCNNAPLPRALPSTWIENKLYGMSDPNWPGESPVPLTRADGTNTGFPRYPNDSVYANWMLSPSAAKLMDTFDS
  
Inhibitor
Name:
BDBM16673
Synonyms:
4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)phenoxy]-N-methylpyridine-2-carboxamide | 4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]phenoxy]-N-methyl-picolinamide;tosylic acid | BAY 43-9006 | BAY 439006 | BAY439006 | CHEMBL1336 | Hit compound, 8 | Nexavar | Sorafenib | Sorafenib, 4 | US10183928, Sorafenib | US10202365, Compound Sorafenib | US10227329, Compound Sorafenib | US10584114, Compound Sorafenib | US10774070, Compound Sorafenib | US10980809, Example Sorafenib | US11279688, Compound Sorafenib | US11505527, Compound Sorafenib | US9029401, Sorafenib | US9469639, Sorafenib | US9902709, Comparative example 1 | Xarelto | cid_216239
Type:
Small organic molecule
Emp. Form.:
C21H16ClF3N4O3
Mol. Mass.:
464.825
SMILES:
CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(c3)C(F)(F)F)cc2)ccn1
Structure:
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