Reaction Details Report a problem with these data
Target
TGF-beta receptor type-1
Ligand
BDBM50579183
Substrate
n/a
Meas. Tech.
ChEMBL_2134690 (CHEMBL4844300)
IC50
13±n/a nM
Citation
 Kharbanda, A; Tran, P; Zhang, L; Leung, YK; Li, HY; Frett, B Discovery of 4-aminoquinolines as highly selective TGF?R1 inhibitors with an attenuated MAP4K4 profile for potential applications in immuno-oncology. Eur J Med Chem 225:0 (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:
BDBM50579183
Synonyms:
CHEMBL4854949
Type:
Small organic molecule
Emp. Form.:
C25H21F2N3O2S
Mol. Mass.:
465.515
SMILES:
CS(=O)(=O)c1ccc(\C=C\C2CC(Nc3ccnc(c3)-c3cc(F)ccc3F)=CC=N2)cc1 |c:29,31|
Structure:
Search PDB for entries with ligand similarity: