Reaction Details |
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Target | TGF-beta receptor type-1 |
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Ligand | BDBM50405406 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_2265106 |
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IC50 | 41±n/a nM |
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Citation | Pujala, B; Ramachandran, SA; Sonawane, M; Kamble, MM; Panpatil, D; Adhikari, S; Soni, S; Subbareddy, V; Shinde, BU; Nayak, AK; Bansal, C; Gupta, A; Mukherjee, K; Agarwal, AK; Guerrero, J; Herrera, FJ; Bernales, S; Guha, M; Chakravarty, S; Pham, SM; Rai, R Discovery of MDV6058 (PF-06952229), a selective and potent TGF?R1 inhibitor: Design, synthesis and optimization. Bioorg Med Chem Lett75:0 (2022) [PubMed] |
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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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BDBM50405406 |
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n/a |
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Name | BDBM50405406 |
Synonyms: | CHEMBL5285227 |
Type | Small organic molecule |
Emp. Form. | C24H26ClFN4O2 |
Mol. Mass. | 456.94 |
SMILES | CC[C@@H](CO)NC(=O)c1cnccc1Nc1cc(ncc1C(C)C)-c1cc(Cl)ccc1F |r| |
Structure |
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