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Target
TGF-beta receptor type-1
Ligand
BDBM412755
Substrate
n/a
Meas. Tech.
ChEMBL_1753651 (CHEMBL4188411)
Ki
0.150000±n/a nM
Citation
 Harikrishnan, LS; Warrier, J; Tebben, AJ; Tonukunuru, G; Madduri, SR; Baligar, V; Mannoori, R; Seshadri, B; Rahaman, H; Arunachalam, PN; Dikundwar, AG; Fink, BE; Fargnoli, J; Fereshteh, M; Fan, Y; Lippy, J; Ho, CP; Wautlet, B; Sheriff, S; Ruzanov, M; Borzilleri, RM Heterobicyclic inhibitors of transforming growth factor beta receptor I (TGF?RI). Bioorg Med Chem 26:1026-1034 (2018) [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:
BDBM412755
Synonyms:
N-(4-((2-(6-(trifluoromethyl)pyridin-2-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)pyridin-2-yl)acetamide | US10399987, Example 20
Type:
Small organic molecule
Emp. Form.:
C19H14F3N7O
Mol. Mass.:
413.356
SMILES:
CC(=O)Nc1cc(Nc2nc(nc3[nH]ccc23)-c2cccc(n2)C(F)(F)F)ccn1
Structure:
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