Target
TGF-beta receptor type-1
Ligand
BDBM50304844
Substrate
n/a
Meas. Tech.
ChEMBL_606316 (CHEMBL1070008)
Ki
952000±n/a nM
Citation
 Guckian, KCarter, MBLin, EYChoi, MSun, LBoriack-Sjodin, PAChuaqui, CLane, BCheung, KLing, LLee, WC Pyrazolone based TGFbetaR1 kinase inhibitors. Bioorg Med Chem Lett 20:326-9 (2010) [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:
BDBM50304844
Synonyms:
4-(2-aminophenyl)-1,2-dimethyl-5-(quinoxalin-6-yl)-1H-pyrazol-3(2H)-one | CHEMBL606695
Type:
Small organic molecule
Emp. Form.:
C19H17N5O
Mol. Mass.:
331.3712
SMILES:
Cn1c(c(-c2ccccc2N)c(=O)n1C)-c1ccc2nccnc2c1 |(-.29,-47.9,;-.91,-46.49,;-2.42,-46.17,;-2.58,-44.64,;-3.92,-43.87,;-5.26,-44.64,;-6.59,-43.87,;-6.59,-42.33,;-5.26,-41.56,;-3.93,-42.32,;-2.6,-41.54,;-1.18,-44.01,;-.86,-42.51,;-.15,-45.16,;1.39,-44.99,;-3.74,-46.97,;-5.09,-46.22,;-6.41,-47.01,;-6.37,-48.55,;-7.69,-49.34,;-7.66,-50.88,;-6.31,-51.63,;-4.99,-50.83,;-5.02,-49.3,;-3.71,-48.5,)|
Structure:
Search PDB for entries with ligand similarity: