Reaction Details |
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Target | TGF-beta receptor type-1 |
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Ligand | BDBM50544399 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1992445 (CHEMBL4626180) |
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IC50 | 731±n/a nM |
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Citation | Smil, D; Wong, JF; Williams, EP; Adamson, RJ; Howarth, A; McLeod, DA; Mamai, A; Kim, S; Wilson, BJ; Kiyota, T; Aman, A; Owen, J; Poda, G; Horiuchi, KY; Kuznetsova, E; Ma, H; Hamblin, JN; Cramp, S; Roberts, OG; Edwards, AM; Uehling, D; Al-Awar, R; Bullock, AN; O'Meara, JA; Isaac, MB Leveraging an Open Science Drug Discovery Model to Develop CNS-Penetrant ALK2 Inhibitors for the Treatment of Diffuse Intrinsic Pontine Glioma. J Med Chem63:10061-10085 (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 |
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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BDBM50544399 |
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n/a |
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Name | BDBM50544399 |
Synonyms: | CHEMBL4638273 |
Type | Small organic molecule |
Emp. Form. | C25H26N4O3 |
Mol. Mass. | 430.4989 |
SMILES | COc1cc(cc(OC)c1OC)-c1cncc(-c2ccc(cc2)N2CCNCC2)c1C#N |
Structure |
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