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Target
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114]
Ligand
BDBM284374
Substrate
n/a
Meas. Tech.
RET Enzyme Assay
pH
7.4±n/a
IC50
5.50±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:
BDBM284374
Synonyms:
4-(6-(4-(6,6-dimethyl- 3- azabicyclo[3.1.0]hexane- 3-carbonyl)piperazin- 1-yl)pyridin-3-yl)-6-(1- methyl-1H-pyrazol-4- yl)pyrazolo[1,5-a]pyridine-3- carbonitrile | US10023570, Example 384 | US10174027, Example 384
Type:
Small organic molecule
Emp. Form.:
C29H31N9O
Mol. Mass.:
521.6161
SMILES:
Cn1cc(cn1)-c1cc(-c2ccc(nc2)N2CCN(CC2)C(=O)N2CC3C(C2)C3(C)C)c2c(cnn2c1)C#N
Structure:
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