Reaction Details Report a problem with these data
Target
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114]
Ligand
BDBM284230
Substrate
n/a
Meas. Tech.
RET Enzyme Assay
pH
7.4±n/a
IC50
15.0±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:
BDBM284230
Synonyms:
1-(5-(3-cyano-6-(1- methyl-1H-pyrazol-4- yl)pyrazolo[1,5- a]pyridin-4-yl)pyridin- 2-yl)-N-((1r,3r)-3- methoxycyclobutyl) piperidine-4- carboxamide | US10023570, Example 240 | US10174028, Example 240
Type:
Small organic molecule
Emp. Form.:
C28H30N8O2
Mol. Mass.:
510.5902
SMILES:
CO[C@H]1CC(C1)NC(=O)C1CCN(CC1)c1ccc(cn1)-c1cc(cn2ncc(C#N)c12)-c1cnn(C)c1 |r,wD:2.1,(10.8,-6,;9.46,-6.77,;8.13,-6,;7.73,-4.51,;6.24,-4.91,;6.64,-6.4,;4.91,-4.14,;4.91,-2.6,;6.24,-1.83,;3.58,-1.83,;2.24,-2.6,;.91,-1.83,;.91,-.29,;2.24,.48,;3.58,-.29,;-.43,.48,;-.43,2.02,;-1.76,2.79,;-3.09,2.02,;-3.09,.48,;-1.76,-.29,;-4.43,2.79,;-5.76,2.02,;-7.09,2.79,;-7.09,4.33,;-5.76,5.1,;-5.44,6.61,;-3.91,6.77,;-3.28,5.36,;-1.79,4.96,;-.31,4.56,;-4.43,4.33,;-8.43,2.02,;-9.89,2.5,;-10.8,1.25,;-9.89,0,;-10.66,-1.33,;-8.43,.48,)|
Structure:
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