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Target
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,V804M]
Ligand
BDBM284646
Substrate
n/a
Meas. Tech.
RET Enzyme Assay
pH
7.4±n/a
IC50
281±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:
BDBM284646
Synonyms:
4-(6-(4-((6- cyanopyridin-3- yl)methyl)piperazin-1- yl)pyridin-3-yl)-6-(1- methyl-1H-pyrazol-4- yl)pyrazolo[1,5- a]pyridine-3- carbonitrile | US10023570, Example 681 | US10174027, Example 681
Type:
Small organic molecule
Emp. Form.:
C28H24N10
Mol. Mass.:
500.5572
SMILES:
Cn1cc(cn1)-c1cc(-c2ccc(nc2)N2CCN(Cc3ccc(nc3)C#N)CC2)c2c(cnn2c1)C#N
Structure:
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