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TargetProto-oncogene tyrosine-protein kinase receptor Ret [V804M]
LigandBDBM50389730
Substrate/Competitorn/a
Meas. Tech.RET and KDR Enzyme Assay
IC50 1870±n/a nM
Citation Jordan, AMNewton, RWaszkowycz, BSutton, JMHynd, GPaoletta, SFordyce, EA Heterocyclic compounds as RET kinase inhibitors US Patent US11661423 Publication Date 5/30/2023
More Info.:Get all data from this article,  Assay Method
 
Proto-oncogene tyrosine-protein kinase receptor Ret [V804M]
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:
MAKATSGAAGLRLLLLLLLPLLGKVALGLYFSRDAYWEKLYVDQAAGTPLLYVHALRDAP
EEVPSFRLGQHLYGTYRTRLHENNWICIQEDTGLLYLNRSLDHSSWEKLSVRNRGFPLLT
VYLKVFLSPTSLREGECQWPGCARVYFSFFNTSFPACSSLKPRELCFPETRPSFRIRENR
PPGTFHQFRLLPVQFLCPNISVAYRLLEGEGLPFRCAPDSLEVSTRWALDREQREKYELV
AVCTVHAGAREEVVMVPFPVTVYDEDDSAPTFPAGVDTASAVVEFKRKEDTVVATLRVFD
ADVVPASGELVRRYTSTLLPGDTWAQQTFRVEHWPNETSVQANGSFVRATVHDYRLVLNR
NLSISENRTMQLAVLVNDSDFQGPGAGVLLLHFNVSVLPVSLHLPSTYSLSVSRRARRFA
QIGKVCVENCQAFSGINVQYKLHSSGANCSTLGVVTSAEDTSGILFVNDTKALRRPKCAE
LHYMVVATDQQTSRQAQAQLLVTVEGSYVAEEAGCPLSCAVSKRRLECEECGGLGSPTGR
CEWRQGDGKGITRNFSTCSPSTKTCPDGHCDVVETQDINICPQDCLRGSIVGGHEPGEPR
GIKAGYGTCNCFPEEEKCFCEPEDIQDPLCDELCRTVIAAAVLFSFIVSVLLSAFCIHCY
HKFAHKPPISSAEMTFRRPAQAFPVSYSSSGARRPSLDSMENQVSVDAFKILEDPKWEFP
RKNLVLGKTLGEGEFGKVVKATAFHLKGRAGYTTVAVKMLKENASPSELRDLLSEFNVLK
QVNHPHVIKLYGACSQDGPLLLIMEYAKYGSLRGFLRESRKVGPGYLGSGGSRNSSSLDH
PDERALTMGDLISFAWQISQGMQYLAEMKLVHRDLAARNILVAEGRKMKISDFGLSRDVY
EEDSYVKRSQGRIPVKWMAIESLFDHIYTTQSDVWSFGVLLWEIVTLGGNPYPGIPPERL
FNLLKTGHRMERPDNCSEEMYRLMLQCWKQEPDKRPVFADISKDLEKMMVKRRDYLDLAA
STPSDSLIYDDGLSEEETPLVDCNNAPLPRALPSTWIENKLYGMSDPNWPGESPVPLTRA
DGTNTGFPRYPNDSVYANWMLSPSAAKLMDTFDS
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50389730
n/a
NameBDBM50389730
Synonyms:CHEMBL2069946 | US10172858, Table 2.7 | US10544104, Compound 24 | US10844067, Example 44 | US11247972, Compound 24 | US11661423, Example 44 | US9765037, Compound 24 | US9828378, # 7
TypeSmall organic molecule
Emp. Form.C16H16N6
Mol. Mass.292.3384
SMILESCC(C)n1nc(-c2cc3ccccc3[nH]2)c2c(N)ncnc12
Structure
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