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Target
TGF-beta receptor type-1
Ligand
BDBM50382325
Substrate
n/a
Meas. Tech.
ChEMBL_815895 (CHEMBL2026330)
IC50
5±n/a nM
Citation
 Boys, ML; Bian, F; Kramer, JB; Chio, CL; Ren, XD; Chen, H; Barrett, SD; Sexton, KE; Iula, DM; Filzen, GF; Nguyen, MN; Angell, P; Downs, VL; Wang, Z; Raheja, N; Ellsworth, EL; Fakhoury, S; Bratton, LD; Keller, PR; Gowan, R; Drummond, EM; Maiti, SN; Hena, MA; Lu, L; McConnell, P; Knafels, JD; Thanabal, V; Sun, F; Alessi, D; McCarthy, A; Zhang, E; Finzel, BC; Patel, S; Ciotti, SM; Eisma, R; Payne, NA; Gilbertsen, RB; Kostlan, CR; Pocalyko, DJ; Lala, DS Discovery of a series of 2-(1H-pyrazol-1-yl)pyridines as ALK5 inhibitors with potential utility in the prevention of dermal scarring. Bioorg Med Chem Lett 22:3392-7 (2012) [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:
BDBM50382325
Synonyms:
CHEMBL2024693
Type:
Small organic molecule
Emp. Form.:
C20H17N5O
Mol. Mass.:
343.3819
SMILES:
Cc1cccc(n1)-n1nc2CCCc2c1-c1ccc2nc[nH]c(=O)c2c1
Structure:
Search PDB for entries with ligand similarity: