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Target
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114]
Ligand
BDBM283987
Substrate
n/a
Meas. Tech.
RET Enzyme Assay
pH
7.4±n/a
IC50
4.40±n/a nM
Comments
extracted
Citation
 Andrews, SW; Blake, JF; Chicarelli, MJ; Golos, A; Haas, J; Jiang, Y; Kolakowski, GR Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors US Patent  US10023570 Publication Date 7/17/2018 
Target
Name:
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114]
Synonyms:
CDHF12 | CDHR16 | PTC | Proto-oncogene tyrosine-protein kinase receptor Ret | Proto-oncogene tyrosine-protein kinase receptor Ret (aa 658-1114) | RET | RET Kinase (aa 658-1114) | RET51 | RET_HUMAN
Type:
n/a
Mol. Mass.:
51535.16
Organism:
Homo sapiens (Human)
Description:
P07949[658-1114]
Residue:
457
Sequence:
HCYHKFAHKPPISSAEMTFRRPAQAFPVSYSSSGARRPSLDSMENQVSVDAFKILEDPKWEFPRKNLVLGKTLGEGEFGKVVKATAFHLKGRAGYTTVAVKMLKENASPSELRDLLSEFNVLKQVNHPHVIKLYGACSQDGPLLLIVEYAKYGSLRGFLRESRKVGPGYLGSGGSRNSSSLDHPDERALTMGDLISFAWQISQGMQYLAEMKLVHRDLAARNILVAEGRKMKISDFGLSRDVYEEDSYVKRSQGRIPVKWMAIESLFDHIYTTQSDVWSFGVLLWEIVTLGGNPYPGIPPERLFNLLKTGHRMERPDNCSEEMYRLMLQCWKQEPDKRPVFADISKDLEKMMVKRRDYLDLAASTPSDSLIYDDGLSEEETPLVDCNNAPLPRALPSTWIENKLYGMSDPNWPGESPVPLTRADGTNTGFPRYPNDSVYANWMLSPSAAKLMDTFDS
  
Inhibitor
Name:
BDBM283987
Synonyms:
(R)-6-(1-methyl-1H- pyrazol-4-yl)-4-(6-(4- (2- phenylpropanoyl)piperazin- 1-yl)pyridin-3- yl)pyrazolo[1,5- a]pyridine-3- carbonitrile | US10023570, Example 14 | US10174027, Example 14
Type:
Small organic molecule
Emp. Form.:
C30H28N8O
Mol. Mass.:
516.5963
SMILES:
C[C@@H](C(=O)N1CCN(CC1)c1ccc(cn1)-c1cc(cn2ncc(C#N)c12)-c1cnn(C)c1)c1ccccc1 |r|
Structure:
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