| Reaction Details |
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 | Report a problem with these data |
| Target | TGF-beta receptor type-1 |
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| Ligand | BDBM280340 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_2265106 |
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| IC50 | 20±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 |
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| 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 |
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| Type: | enzyme |
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| Mol. Mass.: | 55968.24 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P36897 |
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| Residue: | 503 |
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| Sequence: | MEAAVAAPRPRLLLLVLAAAAAAAAALLPGATALQCFCHLCTKDNFTCVTDGLCFVSVTE
TTDKVIHNSMCIAEIDLIPRDRPFVCAPSSKTGSVTTTYCCNQDHCNKIELPTTVKSSPG
LGPVELAAVIAGPVCFVCISLMLMVYICHNRTVIHHRVPNEEDPSLDRPFISEGTTLKDL
IYDMTTSGSGSGLPLLVQRTIARTIVLQESIGKGRFGEVWRGKWRGEEVAVKIFSSREER
SWFREAEIYQTVMLRHENILGFIAADNKDNGTWTQLWLVSDYHEHGSLFDYLNRYTVTVE
GMIKLALSTASGLAHLHMEIVGTQGKPAIAHRDLKSKNILVKKNGTCCIADLGLAVRHDS
ATDTIDIAPNHRVGTKRYMAPEVLDDSINMKHFESFKRADIYAMGLVFWEIARRCSIGGI
HEDYQLPYYDLVPSDPSVEEMRKVVCEQKLRPNIPNRWQSCEALRVMAKIMRECWYANGA
ARLTALRIKKTLSQLSQQEGIKM
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| BDBM280340 |
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| n/a |
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| Name | BDBM280340 |
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| Synonyms: | (S)-4-(2-(5-chloro-2-fluorophenyl)-5-isopropylpyridin-4-ylamino)-N-(1-hydroxypropan-2-yl)nicotinamide | US10030004, Compound 6a | US10501436, Compound 6a | US11053216, Compound 6a | US11702401, Compound 6a |
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| Type | Small organic molecule |
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| Emp. Form. | C23H24ClFN4O2 |
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| Mol. Mass. | 442.914 |
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| SMILES | CC(C)c1cnc(cc1Nc1ccncc1C(=O)N[C@@H](C)CO)-c1cc(Cl)ccc1F |r| |
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| Structure | 
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