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Target
TGF-beta receptor type-1 [162-503]
Ligand
BDBM522135
Substrate
n/a
Meas. Tech.
In Vitro Enzyme Inhibition Using a Biochemical Peptide Phosphorylation Assay- Caliper Assay
IC50
1000±n/a nM
Citation
 Arista, L; Chamoin, S; D''Alessandro, PL; Lindvall, M; Lizos, D; Stiefl, NJ; Teixeira-Fouchard, S; Ullrich, T; Weiler, S Pyridinone derivatives and their use as selective ALK-2 inhibitors US Patent  US11160797 Publication Date 11/2/2021 
Target
Name:
TGF-beta receptor type-1 [162-503]
Synonyms:
ALK5 | Activin receptor-like kinase 5 (ALK-5)(aa 162-503) | Activin receptor-like kinase 5 (ALK5)(162-503) | SKR4 | TGFBR1 | TGFR1_HUMAN
Type:
Enzyme Catalytic Domain
Mol. Mass.:
38872.23
Organism:
Homo sapiens (Human)
Description:
aa 162-503
Residue:
342
Sequence:
EDPSLDRPFISEGTTLKDLIYDMTTSGSGSGLPLLVQRTIARTIVLQESIGKGRFGEVWRGKWRGEEVAVKIFSSREERSWFREAEIYQTVMLRHENILGFIAADNKDNGTWTQLWLVSDYHEHGSLFDYLNRYTVTVEGMIKLALSTASGLAHLHMEIVGTQGKPAIAHRDLKSKNILVKKNGTCCIADLGLAVRHDSATDTIDIAPNHRVGTKRYMAPEVLDDSINMKHFESFKRADIYAMGLVFWEIARRCSIGGIHEDYQLPYYDLVPSDPSVEEMRKVVCEQKLRPNIPNRWQSCEALRVMAKIMRECWYANGAARLTALRIKKTLSQLSQQEGIKM
  
Inhibitor
Name:
BDBM522135
Synonyms:
US11160797, Example 43
Type:
Small organic molecule
Emp. Form.:
C21H21N5O2
Mol. Mass.:
375.4237
SMILES:
CC(C)n1cc(ccc1=O)-c1nc(cnc1N)-c1ccc2N(C)C(=O)Cc2c1
Structure:
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