Target
TGF-beta receptor type-1
Ligand
BDBM50557745
Substrate
n/a
Meas. Tech.
ChEMBL_2059985 (CHEMBL4714986)
IC50
1400±n/a nM
Citation
 Miwa, SYokota, MUeyama, YMaeda, KOgoshi, YSeki, NOgawa, NNishihata, JNomura, AAdachi, TKitao, YNozawa, KIshikawa, TUkaji, YShiozaki, M Discovery of Selective Transforming Growth Factor ? Type II Receptor Inhibitors as Antifibrosis Agents. ACS Med Chem Lett 12:745-751 (2021) [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:
BDBM50557745
Synonyms:
CHEMBL4741913
Type:
Small organic molecule
Emp. Form.:
C15H15N5O
Mol. Mass.:
281.3125
SMILES:
CNc1nc2c(cnn2cc1C=C)-c1ccnc(OC)c1
Structure:
Search PDB for entries with ligand similarity: