Target
TGF-beta receptor type-1 [162-503]
Ligand
BDBM451803
Substrate
n/a
Meas. Tech.
Caliper Assay
IC50
5725±n/a nM
Citation
 Arista, LBabu, SBian, JCui, KDillon, MPLattmann, RLi, JLiao, LLizos, DRamos, RStiefl, NJUllrich, TUsselmann, PWang, XWaykole, LMWeiler, SZhang, YZhou, YZhu, T Aminopyridine derivatives and their use as selective ALK-2 inhibitors US Patent  US10710980 Publication Date 7/14/2020 
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:
BDBM451803
Synonyms:
US10710980, Example 35 | US10947218, Example 35
Type:
Small organic molecule
Emp. Form.:
C31H38F2N4O2
Mol. Mass.:
536.6558
SMILES:
Nc1ncc(cc1C(=O)NC12CCC(O)(CC1)CC2)-c1ccc(cc1)[C@]12C[C@H]1CN(C2)C1CCC(F)(F)CC1 |r|
Structure:
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