Target
TGF-beta receptor type-1
Ligand
BDBM35953
Substrate
BDBM35940
Meas. Tech.
Enzyme Compound Activity (IC50) and Cell Compound Activity (IC50/EC50)
pH
7.4±n/a
Temperature
296.15±n/a K
IC50
12±n/a nM
EC50
31±n/a nM
Citation
 Goldberg, FWWard, RAPowell, SJDebreczeni, JENorman, RARoberts, NJDishington, APGingell, HJWickson, KFRoberts, AL Rapid generation of a high quality lead for transforming growth factor-beta (TGF-beta) type I receptor (ALK5). J Med Chem 52:7901-5 (2009) [PubMed]  Article 
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:
BDBM35953
Synonyms:
4-pyridinoxy-2-anilinopyridine-based compound, 17
Type:
Small organic molecule
Emp. Form.:
C26H25N5O2
Mol. Mass.:
439.509
SMILES:
CN(C)C(=O)c1ccc(Nc2cc(Oc3cc(C)c(C)nc3-c3ccccn3)ccn2)cc1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM35940
Synonyms:
((2Z)-3-(6-{4-[2-({4-[(6-chloro[1,3]dioxolo[4,5-b]pyridin-7-yl)amino]-5-(1-methylethoxy)quinazolin-7-yl}oxy)ethyl]piperazin-1-yl}-6-oxohexyl)-2-[(2E,4E)-5-(3-ethyl-1,1-dimethyl-6,8-disulfo-1H-benzo[e] | ALK5 FP probe
Type:
Small organic molecule
Emp. Form.:
n/a
Mol. Mass.:
n/a
SMILES:
n/a
Structure: