Reaction Details Report a problem with these data
Target
TGF-beta receptor type-1
Ligand
BDBM50298220
Substrate
n/a
Meas. Tech.
ChEMBL_1349480 (CHEMBL3270799)
IC50
77±n/a nM
Citation
 Jin, CH; Krishnaiah, M; Sreenu, D; Subrahmanyam, VB; Rao, KS; Lee, HJ; Park, SJ; Park, HJ; Lee, K; Sheen, YY; Kim, DK Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-ß type I receptor kinase as cancer immunotherapeutic/antifibrotic agent. J Med Chem 57:4213-38 (2014) [PubMed]  Article 
Target
Name:
TGF-beta receptor type-1
Synonyms:
2.7.11.30 | ALK5 | AU017197 | ESK2 | TGF-beta receptor type I | TGF-beta receptor type-1 | TGFR-1 | TGFR1_MOUSE | TbetaR-I | Tgfbr1 | Transforming growth factor-beta receptor type I
Type:
n/a
Mol. Mass.:
56186.39
Organism:
Mus musculus
Description:
n/a
Residue:
503
Sequence:
MEAAAAAPRRPQLLIVLVAAATLLPGAKALQCFCHLCTKDNFTCETDGLCFVSVTETTDKVIHNSMCIAEIDLIPRDRPFVCAPSSKTGAVTTTYCCNQDHCNKIELPTTGPFSEKQSAGLGPVELAAVIAGPVCFVCIALMLMVYICHNRTVIHHRVPNEEDPSLDRPFISEGTTLKDLIYDMTTSGSGSGLPLLVQRTIARTIVLQESIGKGRFGEVWRGKWRGEEVAVKIFSSREERSWFREAEIYQTVMLRHENILGFIAADNKDNGTWTQLWLVSDYHEHGSLFDYLNRYTVTVEGMIKLALSTASGLAHLHMEIVGTQGKPAIAHRDLKSKNILVKKNGTCCIADLGLAVRHDSATDTIDIAPNHRVGTKRYMAPEVLDDSINMKHFESFKRADIYAMGLVFWEIARRCSIGGIHEDYQLPYYDLVPSDPSVEEMRKVVCEQKLRPNIPNRWQSCEALRVMAKIMRECWYANGAARLTALRIKKTLSQLSQQEGIKM
  
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: