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Target
TGF-beta receptor type-1
Ligand
BDBM50468181
Substrate
n/a
Meas. Tech.
ChEMBL_1798297 (CHEMBL4270414)
IC50
22±n/a nM
Citation
 Zhang, Y; Zhao, Y; Tebben, AJ; Sheriff, S; Ruzanov, M; Fereshteh, MP; Fan, Y; Lippy, J; Swanson, J; Ho, CP; Wautlet, BS; Rose, A; Parrish, K; Yang, Z; Donnell, AF; Zhang, L; Fink, BE; Vite, GD; Augustine-Rauch, K; Fargnoli, J; Borzilleri, RM Discovery of 4-Azaindole Inhibitors of TGF?RI as Immuno-oncology Agents. ACS Med Chem Lett 9:1117-1122 (2018) [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:
BDBM50468181
Synonyms:
CHEMBL4289841
Type:
Small organic molecule
Emp. Form.:
C19H14FN5O
Mol. Mass.:
347.3458
SMILES:
CC(=O)Nc1cc(ccn1)-c1[nH]c2cccnc2c1-c1ccc(F)nc1
Structure:
Search PDB for entries with ligand similarity: