Target
TGF-beta receptor type-1
Ligand
BDBM387330
Substrate
n/a
Meas. Tech.
Biological Assays
IC50
6.60±n/a nM
Citation
 Borzilleri, RMFink, BEHarikrishnan, LSSankara Warrier, J TGF beta receptor antagonists US Patent  US10292985 Publication Date 5/21/2019 
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:
BDBM387330
Synonyms:
6-fluoro-N-[2-(6-methylpyridin-2-yl)pyrrolo[2,1-f][1,2,4]triazin-4-yl]quinolin-4-amine | US10292985, Example 14
Type:
Small organic molecule
Emp. Form.:
C21H15FN6
Mol. Mass.:
370.3824
SMILES:
Cc1cccc(n1)-c1nc(Nc2ccnc3ccc(F)cc23)c2cccn2n1
Structure:
Search PDB for entries with ligand similarity: