| 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_1838956 (CHEMBL4339089) |
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| Ki | 1.4±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: | 2.7.11.30 | ALK5 | AU017197 | ESK2 | TGF-beta receptor type I | TGF-beta receptor type-1 | TGFR-1 | TGFR1_MOUSE | TbetaR-I | Tgfbr1 | Transforming growth factor-beta receptor type I |
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| Type: | n/a |
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| Mol. Mass.: | 56186.39 |
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| Organism: | Mus musculus |
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| Description: | n/a |
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| Residue: | 503 |
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| Sequence: | MEAAAAAPRRPQLLIVLVAAATLLPGAKALQCFCHLCTKDNFTCETDGLCFVSVTETTDK
VIHNSMCIAEIDLIPRDRPFVCAPSSKTGAVTTTYCCNQDHCNKIELPTTGPFSEKQSAG
LGPVELAAVIAGPVCFVCIALMLMVYICHNRTVIHHRVPNEEDPSLDRPFISEGTTLKDL
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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