Target
TGF-beta receptor type-1 [T204D]
Ligand
BDBM282953
Substrate
n/a
Meas. Tech.
Biological Assay
IC50
0.800±n/a nM
Citation
 Kinsella, TGelman, MHong, HDarwish, ISSingh, RYu, JBorzilleri, RMVelaparthi, ULiu, PDarne, CPRahaman, HWarrier, 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:
BDBM282953
Synonyms:
6-(1-(cylcobutylmethyl)-4-(4-fluorophenyl)-1H- imidazol-5-yl)imidazo[1,2-a]pyridine-3-carboxamide | US10287295, Example 157' | US11352360, Example 157' | US9884868, Example 157'
Type:
Small organic molecule
Emp. Form.:
C22H20FN5O
Mol. Mass.:
389.4255
SMILES:
NC(=O)c1cnc2ccc(cn12)-c1c(ncn1CC1CCC1)-c1ccc(F)cc1
Structure:
Search PDB for entries with ligand similarity: