Target
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,V804M]
Ligand
BDBM305711
Substrate
n/a
Meas. Tech.
RET Enzyme Assay
IC50
7.00±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  US10441581 Publication Date 10/15/2019 
Target
Name:
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,V804M]
Synonyms:
CDHF12 | CDHR16 | PTC | Proto-oncogene tyrosine-protein kinase receptor Ret (658-end) | Proto-oncogene tyrosine-protein kinase receptor Ret (V804M) | RET | RET Kinase (V804M) (aa658-end) | RET51 | RET_HUMAN
Type:
Enzyme Catalytic Domain
Mol. Mass.:
51567.23
Organism:
Homo sapiens (Human)
Description:
P07949[658-1114,V804M]
Residue:
457
Sequence:
HCYHKFAHKPPISSAEMTFRRPAQAFPVSYSSSGARRPSLDSMENQVSVDAFKILEDPKWEFPRKNLVLGKTLGEGEFGKVVKATAFHLKGRAGYTTVAVKMLKENASPSELRDLLSEFNVLKQVNHPHVIKLYGACSQDGPLLLIMEYAKYGSLRGFLRESRKVGPGYLGSGGSRNSSSLDHPDERALTMGDLISFAWQISQGMQYLAEMKLVHRDLAARNILVAEGRKMKISDFGLSRDVYEEDSYVKRSQGRIPVKWMAIESLFDHIYTTQSDVWSFGVLLWEIVTLGGNPYPGIPPERLFNLLKTGHRMERPDNCSEEMYRLMLQCWKQEPDKRPVFADISKDLEKMMVKRRDYLDLAASTPSDSLIYDDGLSEEETPLVDCNNAPLPRALPSTWIENKLYGMSDPNWPGESPVPLTRADGTNTGFPRYPNDSVYANWMLSPSAAKLMDTFDS
  
Inhibitor
Name:
BDBM305711
Synonyms:
US10144734, Example 729 | US10172845, Example 729 | US10441581, Example 729 | US10881652, Example 729 | US11648243, Example 729
Type:
Small organic molecule
Emp. Form.:
C26H25ClN8O2
Mol. Mass.:
516.982
SMILES:
CCOc1cc(-c2ccc(nc2)N2CC[C@H](NC(=O)c3ncccc3Cl)[C@@H](N)C2)c2c(cnn2c1)C#N |r|
Structure:
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