| Reaction Details |
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 | Report a problem with these data |
| Target | Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,V804M] |
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| Ligand | BDBM305765 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | RET Enzyme Assay |
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| IC50 | 3.00±n/a nM |
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| 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 US10441581 Publication Date 10/15/2019 |
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| More Info.: | Get all data from this article, Assay Method |
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| Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,V804M] |
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| Name: | Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,V804M] |
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| 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 |
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| Type: | Enzyme Catalytic Domain |
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| Mol. Mass.: | 51567.23 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P07949[658-1114,V804M] |
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| Residue: | 457 |
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| Sequence: | HCYHKFAHKPPISSAEMTFRRPAQAFPVSYSSSGARRPSLDSMENQVSVDAFKILEDPKW
EFPRKNLVLGKTLGEGEFGKVVKATAFHLKGRAGYTTVAVKMLKENASPSELRDLLSEFN
VLKQVNHPHVIKLYGACSQDGPLLLIMEYAKYGSLRGFLRESRKVGPGYLGSGGSRNSSS
LDHPDERALTMGDLISFAWQISQGMQYLAEMKLVHRDLAARNILVAEGRKMKISDFGLSR
DVYEEDSYVKRSQGRIPVKWMAIESLFDHIYTTQSDVWSFGVLLWEIVTLGGNPYPGIPP
ERLFNLLKTGHRMERPDNCSEEMYRLMLQCWKQEPDKRPVFADISKDLEKMMVKRRDYLD
LAASTPSDSLIYDDGLSEEETPLVDCNNAPLPRALPSTWIENKLYGMSDPNWPGESPVPL
TRADGTNTGFPRYPNDSVYANWMLSPSAAKLMDTFDS
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| BDBM305765 |
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| n/a |
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| Name | BDBM305765 |
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| Synonyms: | 2-chloro-N-(1-(5-(3- cyano-6- hydroxypyrazolo [1,5-a]pyridin- 4-yl)pyrazin-2-yl)-4- methylpiperidin-4- yl)-6- methylbenzamide | US10144734, Example 783 | US10172845, Example 783 | US10441581, Example 783 | US10881652, Example 783 | US11648243, Example 783 |
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| Type | Small organic molecule |
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| Emp. Form. | C26H24ClN7O2 |
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| Mol. Mass. | 501.967 |
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| SMILES | Cc1cccc(Cl)c1C(=O)NC1(C)CCN(CC1)c1cnc(cn1)-c1cc(O)cn2ncc(C#N)c12 |
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| Structure | 
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