| Reaction Details |
|---|
 | Report a problem with these data |
| Target | Proto-oncogene tyrosine-protein kinase receptor Ret (aa658-end) |
|---|
| Ligand | BDBM305759 |
|---|
| Substrate/Competitor | n/a |
|---|
| Meas. Tech. | 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 US11648243 Publication Date 5/16/2023 |
|---|
| More Info.: | Get all data from this article, Assay Method |
|---|
| |
| Proto-oncogene tyrosine-protein kinase receptor Ret (aa658-end) |
|---|
| 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: | HCYHKFAHKPPISSAEMTFRRPAQAFPVSYSSSGARRPSLDSMENQVSVDAFKILEDPKW
EFPRKNLVLGKTLGEGEFGKVVKATAFHLKGRAGYTTVAVKMLKENASPSELRDLLSEFN
VLKQVNHPHVIKLYGACSQDGPLLLIMEYAKYGSLRGFLRESRKVGPGYLGSGGSRNSSS
LDHPDERALTMGDLISFAWQISQGMQYLAEMKLVHRDLAARNILVAEGRKMKISDFGLSR
DVYEEDSYVKRSQGRIPVKWMAIESLFDHIYTTQSDVWSFGVLLWEIVTLGGNPYPGIPP
ERLFNLLKTGHRMERPDNCSEEMYRLMLQCWKQEPDKRPVFADISKDLEKMMVKRRDYLD
LAASTPSDSLIYDDGLSEEETPLVDCNNAPLPRALPSTWIENKLYGMSDPNWPGESPVPL
TRADGTNTGFPRYPNDSVYANWMLSPSAAKLMDTFDS
|
|
|
|---|
| BDBM305759 |
|---|
| n/a |
|---|
| Name | BDBM305759 |
|---|
| Synonyms: | 3-chloro-N-(1-(5-(3- cyano-6- ethoxypyrazolo[1,5- a]pyridin-4-yl)pyrazin-2- yl)-4-methylpiperidin-4- yl)-6-methylpicolinamide | US10144734, Example 777 | US10172845, Example 777 | US10441581, Example 777 | US10881652, Example 777 | US11648243, Example 777 |
|---|
| Type | Small organic molecule |
|---|
| Emp. Form. | C27H27ClN8O2 |
|---|
| Mol. Mass. | 531.009 |
|---|
| SMILES | CCOc1cc(-c2cnc(cn2)N2CCC(C)(CC2)NC(=O)c2nc(C)ccc2Cl)c2c(cnn2c1)C#N |
|---|
| Structure | 
|
|---|
Search and Browse
