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Target
TGF-beta receptor type-1 [4-503,T204D]
Ligand
BDBM412745
Substrate
n/a
Meas. Tech.
Biological Assays
IC50
0.560±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:
BDBM412745
Synonyms:
N-(3-fluoropyridin-4-yl)-2-(6-(trifluoromethyl)pyridin-2-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine | US10399987, Example 10
Type:
Small organic molecule
Emp. Form.:
C17H10F4N6
Mol. Mass.:
374.2951
SMILES:
Fc1cnccc1Nc1nc(nc2[nH]ccc12)-c1cccc(n1)C(F)(F)F
Structure:
Search PDB for entries with ligand similarity: