Reaction Details Report a problem with these data
Target
TGF-beta receptor type-1
Ligand
BDBM280368
Substrate
n/a
Meas. Tech.
In Vitro Kinase Assay Inhibition of ALK1/2/3/4/5/6 Kinases
IC50
77.3±n/a nM
Citation
 Rai, R; Chakravarty, S; Pujala, B; Shinde, BU; Nayak, AK; Chaklan, N; Agarwal, AK; Ramachandran, SA; Pham, SM Compounds and methods of use US Patent  US10030004 Publication Date 7/24/2018 
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:
BDBM280368
Synonyms:
2-(5-chloro-2-fluorophenyl)-5-(prop-1-en-2-yl)-N-[3-(pyrrolidine-1-carbonyl)pyridin-4-yl]pyridin-4-amine | US10030004, Compound 34 | US10501436, Compound 34 | US11053216, Compound 34 | US11702401, Compound 34
Type:
Small organic molecule
Emp. Form.:
C24H22ClFN4O
Mol. Mass.:
436.909
SMILES:
CC(=C)c1cnc(cc1Nc1ccncc1C(=O)N1CCCC1)-c1cc(Cl)ccc1F
Structure:
Search PDB for entries with ligand similarity: