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Target
TGF-beta receptor type-1 [T204D]
Ligand
BDBM282899
Substrate
n/a
Meas. Tech.
Biological Assay
IC50
0.500±n/a nM
Citation
 Kinsella, T; Gelman, M; Hong, H; Darwish, IS; Singh, R; Yu, J; Borzilleri, RM; Velaparthi, U; Liu, P; Darne, CP; Rahaman, H; Warrier, JS TGF-β inhibitors US Patent  US10287295 Publication Date 5/14/2019 
Target
Name:
TGF-beta receptor type-1 [T204D]
Synonyms:
ALK5 | SKR4 | TGF-beta receptor type-1 (T204D) | TGF-betaR1 T204D | TGFBR1 | TGFBR1T204D | TGFR-1 (T204D) | TGFR1_HUMAN
Type:
n/a
Mol. Mass.:
55981.22
Organism:
Homo sapiens (Human)
Description:
P36897[T204D]
Residue:
503
Sequence:
MEAAVAAPRPRLLLLVLAAAAAAAAALLPGATALQCFCHLCTKDNFTCVTDGLCFVSVTETTDKVIHNSMCIAEIDLIPRDRPFVCAPSSKTGSVTTTYCCNQDHCNKIELPTTVKSSPGLGPVELAAVIAGPVCFVCISLMLMVYICHNRTVIHHRVPNEEDPSLDRPFISEGTTLKDLIYDMTTSGSGSGLPLLVQRTIARDIVLQESIGKGRFGEVWRGKWRGEEVAVKIFSSREERSWFREAEIYQTVMLRHENILGFIAADNKDNGTWTQLWLVSDYHEHGSLFDYLNRYTVTVEGMIKLALSTASGLAHLHMEIVGTQGKPAIAHRDLKSKNILVKKNGTCCIADLGLAVRHDSATDTIDIAPNHRVGTKRYMAPEVLDDSINMKHFESFKRADIYAMGLVFWEIARRCSIGGIHEDYQLPYYDLVPSDPSVEEMRKVVCEQKLRPNIPNRWQSCEALRVMAKIMRECWYANGAARLTALRIKKTLSQLSQQEGIKM
  
Inhibitor
Name:
BDBM282899
Synonyms:
6-(4-(3-chloro-4-fluorophenyl)-1-(3-fluorocyclobutyl)- 1H-imidazol-5-yl)imidazo[1,2-b]pyridazine-3- carbonitrile | US10287295, Example 104' | US11352360, Example 104' | US9884868, Example 104'
Type:
Small organic molecule
Emp. Form.:
C20H13ClF2N6
Mol. Mass.:
410.807
SMILES:
FC1CC(C1)n1cnc(c1-c1ccc2ncc(C#N)n2n1)-c1ccc(F)c(Cl)c1 |(-2.83,-5.84,;-1.74,-4.75,;-1.74,-3.21,;-.2,-3.21,;-.2,-4.75,;.88,-2.12,;2.35,-2.6,;3.25,-1.35,;2.35,-.11,;.88,-.58,;-.45,.19,;-.45,1.73,;-1.78,2.5,;-3.12,1.73,;-4.58,2.2,;-5.49,.96,;-4.58,-.29,;-5.06,-1.75,;-5.53,-3.22,;-3.12,.19,;-1.78,-.58,;2.75,1.38,;1.66,2.47,;2.06,3.96,;3.54,4.35,;3.94,5.84,;4.63,3.27,;6.12,3.66,;4.24,1.78,)|
Structure:
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