Reaction Details |
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Target | TGF-beta receptor type-1 |
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Ligand | BDBM50593565 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_2209051 (CHEMBL5122000) |
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IC50 | 2200±n/a nM |
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Citation | Ullrich, T; Arista, L; Weiler, S; Teixeira-Fouchard, S; Broennimann, V; Stiefl, N; Head, V; Kramer, I; Guth, S Discovery of a novel 2-aminopyrazine-3-carboxamide as a potent and selective inhibitor of Activin Receptor-Like Kinase-2 (ALK2) for the treatment of fibrodysplasia ossificans progressiva. Bioorg Med Chem Lett64:0 (2022) [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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BDBM50593565 |
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n/a |
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Name | BDBM50593565 |
Synonyms: | CHEMBL5193039 |
Type | Small organic molecule |
Emp. Form. | C29H39ClN6O3 |
Mol. Mass. | 555.111 |
SMILES | Nc1ncc(nc1C(=O)NC12CCC(O)(CC1)CC2)-c1ccc(CN2CCC(CC2)N2CCOCC2)cc1Cl |
Structure |
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