| Reaction Details |
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 | Report a problem with these data |
| Target | TGF-beta receptor type-1 |
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| Ligand | BDBM282825 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1838955 (CHEMBL4339088) |
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| Ki | 0.800000±n/a nM |
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| Citation |  Velaparthi, U; Darne, CP; Warrier, J; Liu, P; Rahaman, H; Augustine-Rauch, K; Parrish, K; Yang, Z; Swanson, J; Brown, J; Dhar, G; Anandam, A; Holenarsipur, VK; Palanisamy, K; Wautlet, BS; Fereshteh, MP; Lippy, J; Tebben, AJ; Sheriff, S; Ruzanov, M; Yan, C; Gupta, A; Gupta, AK; Vetrichelvan, M; Mathur, A; Gelman, M; Singh, R; Kinsella, T; Murtaza, A; Fargnoli, J; Vite, G; Borzilleri, RM Discovery of BMS-986260, a Potent, Selective, and Orally Bioavailable TGF?R1 Inhibitor as an Immuno-oncology Agent. ACS Med Chem Lett11:172-178 (2020) [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 |
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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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| BDBM282825 |
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| n/a |
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| Name | BDBM282825 |
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| Synonyms: | 6-(4-(3-chloro-4-fluorophenyl)-1-(2-hydroxyethyl)-1H- imidazol-5-yl)imidazo[1,2-b]pyridazine-3-carbonitrile | US10287295, Example 32' | US11352360, Example 32' | US9884868, Example 32' |
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| Type | Small organic molecule |
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| Emp. Form. | C18H12ClFN6O |
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| Mol. Mass. | 382.779 |
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| SMILES | OCCn1cnc(c1-c1ccc2ncc(C#N)n2n1)-c1ccc(F)c(Cl)c1 |
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| Structure | 
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