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Target
TGF-beta receptor type-1
Ligand
BDBM50382322
Substrate
n/a
Meas. Tech.
ChEMBL_815898 (CHEMBL2026333)
IC50
274±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:
2.7.11.30 | ALK5 | AU017197 | ESK2 | TGF-beta receptor type I | TGF-beta receptor type-1 | TGFR-1 | TGFR1_MOUSE | TbetaR-I | Tgfbr1 | Transforming growth factor-beta receptor type I
Type:
n/a
Mol. Mass.:
56186.39
Organism:
Mus musculus
Description:
n/a
Residue:
503
Sequence:
MEAAAAAPRRPQLLIVLVAAATLLPGAKALQCFCHLCTKDNFTCETDGLCFVSVTETTDKVIHNSMCIAEIDLIPRDRPFVCAPSSKTGAVTTTYCCNQDHCNKIELPTTGPFSEKQSAGLGPVELAAVIAGPVCFVCIALMLMVYICHNRTVIHHRVPNEEDPSLDRPFISEGTTLKDLIYDMTTSGSGSGLPLLVQRTIARTIVLQESIGKGRFGEVWRGKWRGEEVAVKIFSSREERSWFREAEIYQTVMLRHENILGFIAADNKDNGTWTQLWLVSDYHEHGSLFDYLNRYTVTVEGMIKLALSTASGLAHLHMEIVGTQGKPAIAHRDLKSKNILVKKNGTCCIADLGLAVRHDSATDTIDIAPNHRVGTKRYMAPEVLDDSINMKHFESFKRADIYAMGLVFWEIARRCSIGGIHEDYQLPYYDLVPSDPSVEEMRKVVCEQKLRPNIPNRWQSCEALRVMAKIMRECWYANGAARLTALRIKKTLSQLSQQEGIKM
  
Inhibitor
Name:
BDBM50382322
Synonyms:
CHEMBL2024689
Type:
Small organic molecule
Emp. Form.:
C20H19N5O
Mol. Mass.:
345.3978
SMILES:
CCc1cc(-c2ccc3ncn(C)c(=O)c3c2)n(n1)-c1cccc(C)n1
Structure:
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