Reaction Details Report a problem with these data
Target
TGF-beta receptor type-1
Ligand
BDBM406967
Substrate
n/a
Meas. Tech.
Biological Assays
IC50
0.590±n/a nM
Citation
Harikrishnan, LS; Fink, BE; Borzilleri, RM; Tonukunuru, G; Rahaman, H; Warrier, JS; Seshadri, B TGFβ receptor antagonist US Patent US10336761 Publication Date 7/2/2019
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:
BDBM406967
Synonyms:
(3S)-1-({2-[6-(difluoromethyl)pyridin-2-yl]-4-[(3-fluoropyridin-4-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-5-yl}methyl)pyrrolidin-3-ol | US10336761, Example 251
Type:
Small organic molecule
Emp. Form.:
C22H20F3N7O
Mol. Mass.:
455.4357
SMILES:
O[C@H]1CCN(Cc2ccn3nc(nc(Nc4ccncc4F)c23)-c2cccc(n2)C(F)F)C1 |r|