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Target
TGF-beta receptor type-1 [4-503,T204D]
Ligand
BDBM412779
Substrate
n/a
Meas. Tech.
Biological Assays
IC50
2.60±n/a nM
Citation
 Harikrishnan, LS; Fink, BE; Borzilleri, RM; Tonukunuru, G; Sankara Warrier, J TGF beta receptor antagonists US Patent  US10399987 Publication Date 9/3/2019 
Target
Name:
TGF-beta receptor type-1 [4-503,T204D]
Synonyms:
ALK5 | SKR4 | TGF-beta receptor type-1 T204D | TGFBR1 | TGFR-1 T204D | TGFR1_HUMAN
Type:
Enzyme Catalytic Domain
Mol. Mass.:
55650.84
Organism:
Homo sapiens (Human)
Description:
P36897 T204D
Residue:
500
Sequence:
AVAAPRPRLLLLVLAAAAAAAAALLPGATALQCFCHLCTKDNFTCVTDGLCFVSVTETTDKVIHNSMCIAEIDLIPRDRPFVCAPSSKTGSVTTTYCCNQDHCNKIELPTTVKSSPGLGPVELAAVIAGPVCFVCISLMLMVYICHNRTVIHHRVPNEEDPSLDRPFISEGTTLKDLIYDMTTSGSGSGLPLLVQRTIARDIVLQESIGKGRFGEVWRGKWRGEEVAVKIFSSREERSWFREAEIYQTVMLRHENILGFIAADNKDNGTWTQLWLVSDYHEHGSLFDYLNRYTVTVEGMIKLALSTASGLAHLHMEIVGTQGKPAIAHRDLKSKNILVKKNGTCCIADLGLAVRHDSATDTIDIAPNHRVGTKRYMAPEVLDDSINMKHFESFKRADIYAMGLVFWEIARRCSIGGIHEDYQLPYYDLVPSDPSVEEMRKVVCEQKLRPNIPNRWQSCEALRVMAKIMRECWYANGAARLTALRIKKTLSQLSQQEGIKM
  
Inhibitor
Name:
BDBM412779
Synonyms:
N-[4-({2-[6-(difluoromethyl)pyridin-2-yl]-5-{[(2-hydroxy-2-methylpropyl)amino]methyl}-7H-pyrrolo[2,3-d]pyrimidin-4-yl}amino)-5-fluoropyridin-2-yl]acetamide | US10399987, Example 44
Type:
Small organic molecule
Emp. Form.:
C24H25F3N8O2
Mol. Mass.:
514.5029
SMILES:
CC(=O)Nc1cc(Nc2nc(nc3[nH]cc(CNCC(C)(C)O)c23)-c2cccc(n2)C(F)F)c(F)cn1
Structure:
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