Target
TGF-beta receptor type-1
Ligand
BDBM280367
Substrate
n/a
IC50
78.8±n/a nM
Citation
 Rai, RChakravarty, SPujala, BShinde, BUNayak, AKAgarwal, AKRamachandran, SAPham, SM Compounds and methods of use US Patent  US11053216 Publication Date 7/6/2021 
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:
BDBM280367
Synonyms:
4-{[2-(5-chloro-2-fluorophenyl)-5-(pyrrolidin-1-yl)pyridin-4-yl]amino}-N-(1,3-dihydroxypropan-2-yl)pyridine-3-carboxamide | US10030004, Compound 33 | US10501436, Compound 33 | US11053216, Compound 33 | US11702401, Compound 33
Type:
Small organic molecule
Emp. Form.:
C24H25ClFN5O3
Mol. Mass.:
485.938
SMILES:
OCC(CO)NC(=O)c1cnccc1Nc1cc(ncc1N1CCCC1)-c1cc(Cl)ccc1F
Structure:
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