Target
TGF-beta receptor type-1 [4-503,T204D]
Ligand
BDBM412777
Substrate
n/a
Meas. Tech.
Biological Assays
IC50
1.70±n/a nM
Citation
 Harikrishnan, LSFink, BEBorzilleri, RMTonukunuru, GSankara Warrier, J TGF beta receptor antagonists US Patent  US10399987 Publication Date 9/3/2019 
Target
Name:
TGF-beta receptor type-1 [4-503,T204D]
Synonyms:
ALK5 | SKR4 | TGF-beta receptor type-1 T204D | TGFBR1 | TGFR-1 T204D | TGFR1_HUMAN
Type:
Enzyme Catalytic Domain
Mol. Mass.:
55650.84
Organism:
Homo sapiens (Human)
Description:
P36897 T204D
Residue:
500
Sequence:
AVAAPRPRLLLLVLAAAAAAAAALLPGATALQCFCHLCTKDNFTCVTDGLCFVSVTETTDKVIHNSMCIAEIDLIPRDRPFVCAPSSKTGSVTTTYCCNQDHCNKIELPTTVKSSPGLGPVELAAVIAGPVCFVCISLMLMVYICHNRTVIHHRVPNEEDPSLDRPFISEGTTLKDLIYDMTTSGSGSGLPLLVQRTIARDIVLQESIGKGRFGEVWRGKWRGEEVAVKIFSSREERSWFREAEIYQTVMLRHENILGFIAADNKDNGTWTQLWLVSDYHEHGSLFDYLNRYTVTVEGMIKLALSTASGLAHLHMEIVGTQGKPAIAHRDLKSKNILVKKNGTCCIADLGLAVRHDSATDTIDIAPNHRVGTKRYMAPEVLDDSINMKHFESFKRADIYAMGLVFWEIARRCSIGGIHEDYQLPYYDLVPSDPSVEEMRKVVCEQKLRPNIPNRWQSCEALRVMAKIMRECWYANGAARLTALRIKKTLSQLSQQEGIKM
  
Inhibitor
Name:
BDBM412777
Synonyms:
3-methoxy-N-{2-[6-(trifluoromethyl)pyridin-2-yl]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}pyridin-4-amine | US10399987, Example 42
Type:
Small organic molecule
Emp. Form.:
C18H13F3N6O
Mol. Mass.:
386.3306
SMILES:
COc1cnccc1Nc1nc(nc2[nH]ccc12)-c1cccc(n1)C(F)(F)F
Structure:
Search PDB for entries with ligand similarity: