Target
TGF-beta receptor type-1
Ligand
BDBM172452
Substrate
n/a
Meas. Tech.
ALK-5 Kinase Assay
pH
7.6±n/a
Temperature
277.15±n/a K
IC50
4.33±1.51 nM
Comments
extracted
Citation
 Barrett, SDKramer, JBBoys, MLChen, H Therapeutic pyrazolyl thienopyridines US Patent  US9260450 Publication Date 2/16/2016 
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:
BDBM172452
Synonyms:
US9090625, 4 | US9260450, 4 | US9938289, 4
Type:
Small organic molecule
Emp. Form.:
C18H16N4S
Mol. Mass.:
320.411
SMILES:
CCc1cnn(c1-c1cc2cnccc2s1)-c1cccc(C)n1
Structure:
Search PDB for entries with ligand similarity: