Reaction Details Report a problem with these data
Target
TGF-beta receptor type-1 [T204D]
Ligand
BDBM282936
Substrate
n/a
Meas. Tech.
Biological Assay
IC50
0.800±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:
BDBM282936
Synonyms:
6-(4-(3-chloro-4-fluorophenyl)-1-(3-fluorocyclobutyl)- 1H-imidazol-5-yl)imidazo[1,2-b]pyridazine-3- carboxamide | US10287295, Example 141' | US11352360, Example 141' | US9884868, Example 141'
Type:
Small organic molecule
Emp. Form.:
C20H15ClF2N6O
Mol. Mass.:
428.823
SMILES:
NC(=O)c1cnc2ccc(nn12)-c1c(ncn1C1CC(F)C1)-c1ccc(F)c(Cl)c1 |(-6.29,-2.18,;-4.81,-1.78,;-3.72,-2.87,;-4.41,-.29,;-5.31,.96,;-4.41,2.2,;-2.94,1.73,;-1.61,2.5,;-.28,1.73,;-.28,.19,;-1.61,-.58,;-2.94,.19,;1.06,-.58,;2.52,-.11,;3.43,-1.35,;2.52,-2.6,;1.06,-2.12,;-.03,-3.21,;-1.57,-3.21,;-1.57,-4.75,;-2.66,-5.84,;-.03,-4.75,;2.92,1.38,;1.83,2.47,;2.23,3.96,;3.72,4.35,;4.12,5.84,;4.81,3.27,;6.29,3.66,;4.41,1.78,)|
Structure:
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