Target
TGF-beta receptor type-1
Ligand
BDBM407051
Substrate
n/a
Meas. Tech.
Biological Assays
IC50
0.370±n/a nM
Citation
 Harikrishnan, LSFink, BEBorzilleri, RMTonukunuru, GRahaman, HWarrier, JSSeshadri, B TGFβ receptor antagonist US Patent  US10336761 Publication Date 7/2/2019 
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:
BDBM407051
Synonyms:
N-[4-({2-[6-(trifluoromethyl)pyridin-2-yl]pyrrolo[2,1-f][1,2,4]triazin-4-yl}amino)pyridin-2-yl]cyclopropanecarboxamide | US10336761, Example 335
Type:
Small organic molecule
Emp. Form.:
C21H16F3N7O
Mol. Mass.:
439.3932
SMILES:
FC(F)(F)c1cccc(n1)-c1nc(Nc2ccnc(NC(=O)C3CC3)c2)c2cccn2n1
Structure:
Search PDB for entries with ligand similarity: