Target
TGF-beta receptor type-1
Ligand
BDBM50329801
Substrate
n/a
Meas. Tech.
ChEMBL_674821 (CHEMBL1272394)
EC50
382±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:
BDBM50329801
Synonyms:
(Z)-3-((4-(2-(dimethylamino)-N-methylacetamido)phenylamino)(phenyl)methylene)-N-ethyl-N-methyl-2-oxoindoline-6-carboxamide | CHEMBL1271470
Type:
Small organic molecule
Emp. Form.:
C30H33N5O3
Mol. Mass.:
511.6147
SMILES:
CCN(C)C(=O)c1ccc2C(C(=Nc3ccc(cc3)N(C)C(=O)CN(C)C)c3ccccc3)C(=O)Nc2c1 |w:12.12|
Structure:
Search PDB for entries with ligand similarity: