Reaction Details Report a problem with these data
Target
TGF-beta receptor type-1
Ligand
BDBM282822
Substrate
n/a
Meas. Tech.
Biological Assay
pH
7.4±n/a
Temperature
298.15±n/a K
IC50
6.40±n/a nM
Comments
extracted
Citation
Kinsella, T; Gelman, M; Hong, H; Darwish, IS; Singh, R; Yu, J; Borzilleri, RM; Velaparthi, U; Liu, P; Darne, C; Rahaman, H; Warrier, JS TGF-beta inhibitors US Patent US9884868 Publication Date 2/6/2018
More Info.:
Target
Name:
TGF-beta receptor type-1
Synonyms:
ALK-5 | ALK5 | Activin A receptor type II-like protein kinase of 53kD | Activin receptor-like kinase 5 | SKR4 | Serine/threonine-protein kinase receptor R4 | TGF-beta receptor type I | TGF-beta type I receptor | TGFBR1 | TGFR-1 | TGFR1_HUMAN | TbetaR-I | Transforming growth factor-beta receptor type I
Type:
enzyme
Mol. Mass.:
55968.24
Organism:
Homo sapiens (Human)
Description:
P36897
Residue:
503
Sequence:
MEAAVAAPRPRLLLLVLAAAAAAAAALLPGATALQCFCHLCTKDNFTCVTDGLCFVSVTETTDKVIHNSMCIAEIDLIPRDRPFVCAPSSKTGSVTTTYCCNQDHCNKIELPTTVKSSPGLGPVELAAVIAGPVCFVCISLMLMVYICHNRTVIHHRVPNEEDPSLDRPFISEGTTLKDLIYDMTTSGSGSGLPLLVQRTIARTIVLQESIGKGRFGEVWRGKWRGEEVAVKIFSSREERSWFREAEIYQTVMLRHENILGFIAADNKDNGTWTQLWLVSDYHEHGSLFDYLNRYTVTVEGMIKLALSTASGLAHLHMEIVGTQGKPAIAHRDLKSKNILVKKNGTCCIADLGLAVRHDSATDTIDIAPNHRVGTKRYMAPEVLDDSINMKHFESFKRADIYAMGLVFWEIARRCSIGGIHEDYQLPYYDLVPSDPSVEEMRKVVCEQKLRPNIPNRWQSCEALRVMAKIMRECWYANGAARLTALRIKKTLSQLSQQEGIKM
Inhibitor
Name:
BDBM282822
Synonyms:
(S)-6-(4-(4-fluorophenyl)-1-(4,4,4-trifluoro-1- hydroxybutan-2-yl)-1H-imidazol-5-yl)imidazo[1,2- b]pyridazine-3-carbonitrile | US10287295, Example 29' | US11352360, Example 29' | US9884868, Example 29'
Type:
Small organic molecule
Emp. Form.:
C20H14F4N6O
Mol. Mass.:
430.3584
SMILES:
OC[C@H](CC(F)(F)F)n1cnc(c1-c1ccc2ncc(C#N)n2n1)-c1ccc(F)cc1 |r|