Reaction Details Report a problem with these data
Target
TGF-beta receptor type-1
Ligand
BDBM518473
Substrate
n/a
Meas. Tech.
LanthaScreen Eu Kinase Binding Assay TGFBR1 (ALK5)
IC50
<100.0±n/a nM
Citation
 Sawyer, JS Tri-substituted imidazoles for the inhibition of TGF beta and methods of treatment US Patent  US11124509 Publication Date 9/21/2021 
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:
BDBM518473
Synonyms:
US11124509, Compound 45
Type:
Small organic molecule
Emp. Form.:
C24H21F2N7
Mol. Mass.:
445.4672
SMILES:
CC(C)n1ccc(n1)-c1nc(CNc2cc(F)ccc2F)[nH]c1-c1ccc2nccnc2c1
Structure:
Search PDB for entries with ligand similarity: