Target
TGF-beta receptor type-1
Ligand
BDBM50298220
Substrate
n/a
Meas. Tech.
ChEMBL_1351655 (CHEMBL3269342)
IC50
590±n/a nM
Citation
 Jin, CHKrishnaiah, MSreenu, DSubrahmanyam, VBPark, HJPark, SJSheen, YYKim, DK 4-([1,2,4]Triazolo[1,5-a]pyridin-6-yl)-5(3)-(6-methylpyridin-2-yl)imidazole and -pyrazole derivatives as potent and selective inhibitors of transforming growth factor-ß type I receptor kinase. Bioorg Med Chem 22:2724-32 (2014) [PubMed]  Article 
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:
BDBM50298220
Synonyms:
2-(4-(benzo[d][1,3]dioxol-5-yl)-2-tert-butyl-1H-imidazol-5-yl)-6-methylpyridine | 2-(5-(benzo[d][1,3]dioxol-5-yl)-2-tert-butyl-1H-imidazol-4-yl)-6-methylpyridine | CHEMBL1824446 | CHEMBL226838 | SB-505124 | US11759530, Compound Table1.2
Type:
Small organic molecule
Emp. Form.:
C20H21N3O2
Mol. Mass.:
335.3996
SMILES:
Cc1cccc(n1)-c1nc([nH]c1-c1ccc2OCOc2c1)C(C)(C)C
Structure:
Search PDB for entries with ligand similarity: