Target
TGF-beta receptor type-1
Ligand
BDBM50262079
Substrate
poly(Glu4, Tyr)
Meas. Tech.
in vitro Kinase Assay
IC50
565.0±0.0 nM
Citation
 Hao, JHo, JNLewis, JAKarim, KADaniels, RNGentry, PRHopkins, CRLindsley, CWHong, CC In vivo structure-activity relationship study of dorsomorphin analogues identifies selective VEGF and BMP inhibitors. ACS Chem Biol 5:245-53 (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:
BDBM50262079
Synonyms:
4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline | 4-[6-(4-piperazin-1-ylphenyl)pyrazolo[1,5-a]pyrimidin-3-yl]quinoline | CHEMBL513147 | LDN-193189
Type:
Small organic molecule
Emp. Form.:
C25H22N6
Mol. Mass.:
406.4824
SMILES:
C1CN(CCN1)c1ccc(cc1)-c1cnc2c(cnn2c1)-c1ccnc2ccccc12
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
poly(Glu4, Tyr)
Synonyms:
n/a
Type:
Random copolymer
Mol. Mass.:
358.43
Organism:
n/a
Description:
n/a
Residue:
3
Sequence:
NA