Reaction Details |
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Target | TGF-beta receptor type-1 |
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Ligand | BDBM50428286 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_946470 (CHEMBL2340067) |
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IC50 | 3700±n/a nM |
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Citation | Rheault, TR; Stellwagen, JC; Adjabeng, GM; Hornberger, KR; Petrov, KG; Waterson, AG; Dickerson, SH; Mook, RA; Laquerre, SG; King, AJ; Rossanese, OW; Arnone, MR; Smitheman, KN; Kane-Carson, LS; Han, C; Moorthy, GS; Moss, KG; Uehling, DE Discovery of Dabrafenib: A Selective Inhibitor of Raf Kinases with Antitumor Activity against B-Raf-Driven Tumors. ACS Med Chem Lett4:358-62 (2013) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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TGF-beta receptor type-1 |
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Name: | TGF-beta receptor type-1 |
Synonyms: | ALK-5 | ALK5 | Activin A receptor type II-like protein kinase of 53kD | Activin receptor-like kinase 5 | SKR4 | Serine/threonine-protein kinase receptor R4 | TGF-beta receptor type I | TGF-beta type I receptor | TGFBR1 | TGFR-1 | TGFR1_HUMAN | TbetaR-I | Transforming growth factor-beta receptor type I |
Type: | enzyme |
Mol. Mass.: | 55968.24 |
Organism: | Homo sapiens (Human) |
Description: | P36897 |
Residue: | 503 |
Sequence: | MEAAVAAPRPRLLLLVLAAAAAAAAALLPGATALQCFCHLCTKDNFTCVTDGLCFVSVTE
TTDKVIHNSMCIAEIDLIPRDRPFVCAPSSKTGSVTTTYCCNQDHCNKIELPTTVKSSPG
LGPVELAAVIAGPVCFVCISLMLMVYICHNRTVIHHRVPNEEDPSLDRPFISEGTTLKDL
IYDMTTSGSGSGLPLLVQRTIARTIVLQESIGKGRFGEVWRGKWRGEEVAVKIFSSREER
SWFREAEIYQTVMLRHENILGFIAADNKDNGTWTQLWLVSDYHEHGSLFDYLNRYTVTVE
GMIKLALSTASGLAHLHMEIVGTQGKPAIAHRDLKSKNILVKKNGTCCIADLGLAVRHDS
ATDTIDIAPNHRVGTKRYMAPEVLDDSINMKHFESFKRADIYAMGLVFWEIARRCSIGGI
HEDYQLPYYDLVPSDPSVEEMRKVVCEQKLRPNIPNRWQSCEALRVMAKIMRECWYANGA
ARLTALRIKKTLSQLSQQEGIKM
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BDBM50428286 |
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n/a |
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Name | BDBM50428286 |
Synonyms: | DABRAFENIB | GSK2118436A |
Type | Small organic molecule |
Emp. Form. | C23H20F3N5O2S2 |
Mol. Mass. | 519.562 |
SMILES | CC(C)(C)c1nc(c(s1)-c1ccnc(N)n1)-c1cccc(NS(=O)(=O)c2c(F)cccc2F)c1F |
Structure |
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