Target
TGF-beta receptor type-1
Ligand
BDBM282852
Substrate
n/a
Meas. Tech.
Biological Assay
pH
7.4±n/a
Temperature
298.15±n/a K
IC50
0.800±n/a nM
Comments
extracted
Citation
 Kinsella, TGelman, MHong, HDarwish, ISSingh, RYu, JBorzilleri, RMVelaparthi, ULiu, PDarne, CRahaman, HWarrier, JS TGF-beta inhibitors US Patent  US9884868 Publication Date 2/6/2018 
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:
BDBM282852
Synonyms:
6-(4-(3-chloro-4-fluorophenyl)-1-cyclobutyl-1H- imidazol-5-yl)imidazo[1,2-b]pyridazine-3-carbonitrile | US10287295, Example 58' | US11352360, Example 58' | US9884868, Example 58'
Type:
Small organic molecule
Emp. Form.:
C20H14ClFN6
Mol. Mass.:
392.817
SMILES:
Fc1ccc(cc1Cl)-c1ncn(C2CCC2)c1-c1ccc2ncc(C#N)n2n1
Structure:
Search PDB for entries with ligand similarity: