| Reaction Details |
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 | Report a problem with these data |
| Target | Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R] |
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| Ligand | BDBM296241 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | RET G810R Mutant Assay |
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| IC50 | 182±n/a nM |
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| Citation |  Andrews, SW; Aronow, S; Blake, JF; Brandhuber, BJ; Cook, A; Haas, J; Jiang, Y; Kolakowski, GR; McFaddin, EA; McKenney, ML; McNulty, OT; Metcalf, AT; Moreno, DA; Tang, TP; Ren, L Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors US Patent US10555944 Publication Date 2/11/2020 |
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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,G810R] |
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| Name: | Proto-oncogene tyrosine-protein kinase receptor Ret [658-1114,G810R] |
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| Synonyms: | CDHF12 | CDHR16 | PTC | Proto-oncogene tyrosine-protein kinase receptor Ret (G810R) | RET | RET51 | RET_HUMAN |
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| Type: | Enzyme Catalytic Domain |
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| Mol. Mass.: | 51635.31 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P07949[658-1114,G810R] |
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| Residue: | 457 |
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| Sequence: | HCYHKFAHKPPISSAEMTFRRPAQAFPVSYSSSGARRPSLDSMENQVSVDAFKILEDPKW
EFPRKNLVLGKTLGEGEFGKVVKATAFHLKGRAGYTTVAVKMLKENASPSELRDLLSEFN
VLKQVNHPHVIKLYGACSQDGPLLLIVEYAKYRSLRGFLRESRKVGPGYLGSGGSRNSSS
LDHPDERALTMGDLISFAWQISQGMQYLAEMKLVHRDLAARNILVAEGRKMKISDFGLSR
DVYEEDSYVKRSQGRIPVKWMAIESLFDHIYTTQSDVWSFGVLLWEIVTLGGNPYPGIPP
ERLFNLLKTGHRMERPDNCSEEMYRLMLQCWKQEPDKRPVFADISKDLEKMMVKRRDYLD
LAASTPSDSLIYDDGLSEEETPLVDCNNAPLPRALPSTWIENKLYGMSDPNWPGESPVPL
TRADGTNTGFPRYPNDSVYANWMLSPSAAKLMDTFDS
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| BDBM296241 |
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| n/a |
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| Name | BDBM296241 |
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| Synonyms: | US10112942, Example 48 | US10137124, Example 48 | US10172851, Example 48 | US10555944, Example 48 | US10953005, Example 48 |
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| Type | Small organic molecule |
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| Emp. Form. | C27H27N7O2 |
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| Mol. Mass. | 481.549 |
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| SMILES | CCOc1cc(-c2ccc(nc2)N2CC3CC(C2)N3Cc2ccc(OC)nc2)c2c(cnn2c1)C#N |
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| Structure | 
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