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Target
TGF-beta receptor type-1
Ligand
BDBM50564603
Substrate
n/a
Meas. Tech.
ChEMBL_2088442 (CHEMBL4769705)
IC50
13±n/a nM
Citation
 Xu, G; Zhang, Y; Wang, H; Guo, Z; Wang, X; Li, X; Chang, S; Sun, T; Yu, Z; Xu, T; Zhao, L; Wang, Y; Yu, W Synthesis and biological evaluation of 4-(pyridin-4-oxy)-3-(3,3-difluorocyclobutyl)-pyrazole derivatives as novel potent transforming growth factor-? type 1 receptor inhibitors. Eur J Med Chem 198:0 (2020) [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:
BDBM50564603
Synonyms:
CHEMBL4777294 | US11691981, Compound 77
Type:
Small organic molecule
Emp. Form.:
C25H29F2N5O2
Mol. Mass.:
469.5269
SMILES:
CC(C)(O)c1cc(Nc2cc(Oc3cn(nc3C3CCC(F)(F)CC3)C3CC3)ccn2)ccn1
Structure:
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