| Reaction Details |
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 | Report a problem with these data |
| Target | TGF-beta receptor type-1 [4-503,T204D] |
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| Ligand | BDBM21513 |
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| Substrate/Competitor | TGF-beta receptor type I |
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| Meas. Tech. | Enzyme Assay and Luciferase Reporter Assay |
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| pH | 7.5±n/a |
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| Temperature | 303.15±n/a K |
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| IC50 | 72±53 nM |
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| EC50 | 17±1 nM |
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| Citation |  Li, HY; McMillen, WT; Heap, CR; McCann, DJ; Yan, L; Campbell, RM; Mundla, SR; King, CH; Dierks, EA; Anderson, BD; Britt, KS; Huss, KL; Voss, MD; Wang, Y; Clawson, DK; Yingling, JM; Sawyer, JS Optimization of a Dihydropyrrolopyrazole Series of Transforming Growth Factor-beta Type I Receptor Kinase Domain Inhibitors: Discovery of an Orally Bioavailable Transforming Growth Factor-beta Receptor Type I Inhibitor as Antitumor Agent. J Med Chem51:2302-2306 (2008) [PubMed] Article |
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| More Info.: | Get all data from this article, Solution Info, Assay Method |
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| TGF-beta receptor type-1 [4-503,T204D] |
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| Name: | TGF-beta receptor type-1 [4-503,T204D] |
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| Synonyms: | ALK5 | SKR4 | TGF-beta receptor type-1 T204D | TGFBR1 | TGFR-1 T204D | TGFR1_HUMAN |
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| Type: | Enzyme Catalytic Domain |
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| Mol. Mass.: | 55650.84 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P36897 T204D |
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| Residue: | 500 |
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| Sequence: | AVAAPRPRLLLLVLAAAAAAAAALLPGATALQCFCHLCTKDNFTCVTDGLCFVSVTETTD
KVIHNSMCIAEIDLIPRDRPFVCAPSSKTGSVTTTYCCNQDHCNKIELPTTVKSSPGLGP
VELAAVIAGPVCFVCISLMLMVYICHNRTVIHHRVPNEEDPSLDRPFISEGTTLKDLIYD
MTTSGSGSGLPLLVQRTIARDIVLQESIGKGRFGEVWRGKWRGEEVAVKIFSSREERSWF
REAEIYQTVMLRHENILGFIAADNKDNGTWTQLWLVSDYHEHGSLFDYLNRYTVTVEGMI
KLALSTASGLAHLHMEIVGTQGKPAIAHRDLKSKNILVKKNGTCCIADLGLAVRHDSATD
TIDIAPNHRVGTKRYMAPEVLDDSINMKHFESFKRADIYAMGLVFWEIARRCSIGGIHED
YQLPYYDLVPSDPSVEEMRKVVCEQKLRPNIPNRWQSCEALRVMAKIMRECWYANGAARL
TALRIKKTLSQLSQQEGIKM
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| BDBM21513 |
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| TGF-beta receptor type I |
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| Name: | TGF-beta receptor type I |
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| Synonyms: | ALK5 | ALK5(T204D) | SKR4 | TGFBR1 | TGFR1_HUMAN |
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| Type: | Receptor intracellular domain |
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| Mol. Mass.: | 40581.62 |
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| Organism: | Homo sapiens (Human) |
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| Description: | The autophosphorylation substrate. |
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| Residue: | 356 |
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| Sequence: | CHNRTVIHHRVPNEEDPSLDRPFISEGTTLKDLIYDMTTSGSGSGLPLLVQRTIARDIVL
QESIGKGRFGEVWRGKWRGEEVAVKIFSSREERSWFREAEIYQTVMLRHENILGFIAADN
KDNGTWTQLWLVSDYHEHGSLFDYLNRYTVTVEGMIKLALSTASGLAHLHMEIVGTQGKP
AIAHRDLKSKNILVKKNGTCCIADLGLAVRHDSATDTIDIAPNHRVGTKRYMAPEVLDDS
INMKHFESFKRADIYAMGLVFWEIARRCSIGGIHEDYQLPYYDLVPSDPSVEEMRKVVCE
QKLRPNIPNRWQSCEALRVMAKIMRECWYANGAARLTALRIKKTLSQLSQQEGIKM
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