Target
TGF-beta receptor type-1 [4-503,T204D]
Ligand
BDBM412742
Substrate
n/a
Meas. Tech.
Biological Assays
IC50
3.70±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:
BDBM412742
Synonyms:
2-(6-(difluoromethyl)pyridin-2-yl)-N-(3-fluoropyridin-4-yl)-5-((4-methylpiperazin-1-yl)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine | US10399987, Example 7
Type:
Small organic molecule
Emp. Form.:
C23H23F3N8
Mol. Mass.:
468.4775
SMILES:
CN1CCN(Cc2c[nH]c3nc(nc(Nc4ccncc4F)c23)-c2cccc(n2)C(F)F)CC1
Structure:
Search PDB for entries with ligand similarity: