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TargetTGF-beta receptor type-1
LigandBDBM50015639
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1349479 (CHEMBL3270798)
IC50 17±n/a nM
Citation Jin, CHKrishnaiah, MSreenu, DSubrahmanyam, VBRao, KSLee, HJPark, SJPark, HJLee, KSheen, YYKim, DK Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-ß type I receptor kinase as cancer immunotherapeutic/antifibrotic agent. J Med Chem57:4213-38 (2014) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
TGF-beta receptor type-1
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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50015639
n/a
NameBDBM50015639
Synonyms:CHEMBL3260567 | USRE47141, Example 2
TypeSmall organic molecule
Emp. Form.C22H18FN7
Mol. Mass.399.4236
SMILESCc1cccc(n1)-c1[nH]c(CNc2ccccc2F)nc1-c1ccc2ncnn2c1
Structure
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