Reaction Details Report a problem with these data
Target
Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114]
Ligand
BDBM305283
Substrate
n/a
Meas. Tech.
A RET Enzyme Assay
IC50
6.80±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:
BDBM305283
Synonyms:
US10144734, Example 299 | US10172845, Example 299 | US10441581, Example 299 | US10881652, Example 299 | US11648243, Example 299
Type:
Small organic molecule
Emp. Form.:
C30H30F2N6O3
Mol. Mass.:
560.5944
SMILES:
CC(C)(O)COc1cc(-c2ccc(nc2)N2CCC(C)(CC2)C(=O)Nc2c(F)cccc2F)c2c(cnn2c1)C#N