Reaction Details Report a problem with these data
Target
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114]
Ligand
BDBM305757
Substrate
n/a
Meas. Tech.
A RET Enzyme Assay
IC50
3.00±n/a nM
Citation
Andrews, SW; Aronow, S; Blake, JF; Brandhuber, BJ; Collier, J; Cook, A; Haas, J; Jiang, Y; Kolakowski, GR; McFaddin, EA; McKenney, ML; McNulty, OT; Metcalf, AT; Moreno, DA; Ramann, GA; Tang, TP; Ren, L; Walls, SM Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors US Patent US10172845 Publication Date 1/8/2019
More Info.:
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:
BDBM305757
Synonyms:
3-chloro-N-(1-(5-(3- cyano-6- ethoxypyrazolo[1,5- a]pyridin-4-yl)pyrazin-2- yl)-4-methylpiperidin-4- yl)-5-fluoropicolinamide | US10144734, Example 775 | US10172845, Example 775 | US10441581, Example 775 | US10881652, Example 775 | US11648243, Example 775
Type:
Small organic molecule
Emp. Form.:
C26H24ClFN8O2
Mol. Mass.:
534.973
SMILES:
CCOc1cc(-c2cnc(cn2)N2CCC(C)(CC2)NC(=O)c2ncc(F)cc2Cl)c2c(cnn2c1)C#N