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Target
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,V804M]
Ligand
BDBM284453
Substrate
n/a
Meas. Tech.
RET Enzyme Assay
pH
7.4±n/a
IC50
47.3±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,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:
BDBM284453
Synonyms:
4-(6-(4-((3- methoxypyridin-2- yl)methyl)piperazin-1- yl)pyridin-3-yl)-6-(1- methyl-1H-pyrazol-4- yl)pyrazolo[1,5-a]pyridine- 3-carbonitrile formate | US10023570, Example 463 | US10174027, Example 463
Type:
Small organic molecule
Emp. Form.:
C28H27N9O
Mol. Mass.:
505.5737
SMILES:
COc1cccnc1CN1CCN(CC1)c1ccc(cn1)-c1cc(cn2ncc(C#N)c12)-c1cnn(C)c1
Structure:
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