Reaction Details Report a problem with these data
Target
TGF-beta receptor type-1
Ligand
BDBM280343
Substrate
n/a
IC50
99.2±n/a nM
Citation
Rai, R; Chakravarty, S; Pujala, B; Shinde, BU; Nayak, AK; Agarwal, AK; Ramachandran, SA; Pham, SM Compounds and methods of use US Patent US11053216 Publication Date 7/6/2021
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:
BDBM280343
Synonyms:
4-[[2-(5-chloro-2-fluoro-phenyl)-5-isopropenyl-4-pyridyl]amino]-N-(2-hydroxy-1,1-dimethyl-ethyl)pyridine-3-carboxamide | US10030004, Compound 8 | US10501436, Compound 8 | US11053216, Compound 8 | US11702401, Compound 8
Type:
Small organic molecule
Emp. Form.:
C24H24ClFN4O2
Mol. Mass.:
454.924
SMILES:
CC(=C)c1cnc(cc1Nc1ccncc1C(=O)NC(C)(C)CO)-c1cc(Cl)ccc1F