Target
TGF-beta receptor type-1
Ligand
BDBM50304874
Substrate
n/a
Meas. Tech.
ChEMBL_606316 (CHEMBL1070008)
Ki
1870±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:
BDBM50304874
Synonyms:
4-(benzo[b]thiophen-3-yl)-1,2-dimethyl-5-(quinoxalin-6-yl)-1H-pyrazol-3(2H)-one | CHEMBL603642
Type:
Small organic molecule
Emp. Form.:
C21H16N4OS
Mol. Mass.:
372.443
SMILES:
Cn1c(c(-c2csc3ccccc23)c(=O)n1C)-c1ccc2nccnc2c1 |(1.19,-27.99,;-.28,-28.46,;-.76,-29.93,;-2.31,-29.93,;-3.09,-31.25,;-2.47,-32.65,;-3.62,-33.67,;-4.95,-32.89,;-6.41,-33.35,;-7.54,-32.32,;-7.21,-30.81,;-5.74,-30.35,;-4.61,-31.39,;-2.78,-28.46,;-4.25,-27.98,;-1.54,-27.55,;-1.54,-26.01,;.14,-31.17,;-.49,-32.58,;.41,-33.83,;1.95,-33.67,;2.85,-34.91,;4.39,-34.75,;5.01,-33.33,;4.1,-32.09,;2.58,-32.26,;1.67,-31.01,)|
Structure:
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