Target
TGF-beta receptor type-1
Ligand
BDBM50329795
Substrate
n/a
Meas. Tech.
ChEMBL_674822 (CHEMBL1272395)
IC50
3±n/a nM
Citation
 Roth, GJHeckel, ABrandl, TGrauert, MHoerer, SKley, JTSchnapp, GBaum, PMennerich, DSchnapp, APark, JE Design, synthesis, and evaluation of indolinones as inhibitors of the transforming growth factorß receptor I (TGFßRI). J Med Chem 53:7287-95 (2010) [PubMed]  Article 
Target
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:
MEAAVAAPRPRLLLLVLAAAAAAAAALLPGATALQCFCHLCTKDNFTCVTDGLCFVSVTETTDKVIHNSMCIAEIDLIPRDRPFVCAPSSKTGSVTTTYCCNQDHCNKIELPTTVKSSPGLGPVELAAVIAGPVCFVCISLMLMVYICHNRTVIHHRVPNEEDPSLDRPFISEGTTLKDLIYDMTTSGSGSGLPLLVQRTIARTIVLQESIGKGRFGEVWRGKWRGEEVAVKIFSSREERSWFREAEIYQTVMLRHENILGFIAADNKDNGTWTQLWLVSDYHEHGSLFDYLNRYTVTVEGMIKLALSTASGLAHLHMEIVGTQGKPAIAHRDLKSKNILVKKNGTCCIADLGLAVRHDSATDTIDIAPNHRVGTKRYMAPEVLDDSINMKHFESFKRADIYAMGLVFWEIARRCSIGGIHEDYQLPYYDLVPSDPSVEEMRKVVCEQKLRPNIPNRWQSCEALRVMAKIMRECWYANGAARLTALRIKKTLSQLSQQEGIKM
  
Inhibitor
Name:
BDBM50329795
Synonyms:
(Z)-3-((4-(N-(3-(dimethylamino)propyl)acetamido)phenylamino)(phenyl)methylene)-N-ethyl-2-oxoindoline-6-carboxamide | CHEMBL1271736
Type:
Small organic molecule
Emp. Form.:
C31H35N5O3
Mol. Mass.:
525.6413
SMILES:
CCNC(=O)c1ccc2C(C(=Nc3ccc(cc3)N(CCCN(C)C)C(C)=O)c3ccccc3)C(=O)Nc2c1 |w:11.11|
Structure:
Search PDB for entries with ligand similarity: