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TargetTGF-beta receptor type-1
LigandBDBM50405402
Substrate/Competitorn/a
Meas. Tech.ChEMBL_2265106
IC50 3.0±n/a nM
Citation Pujala, BRamachandran, SASonawane, MKamble, MMPanpatil, DAdhikari, SSoni, SSubbareddy, VShinde, BUNayak, AKBansal, CGupta, AMukherjee, KAgarwal, AKGuerrero, JHerrera, FJBernales, SGuha, MChakravarty, SPham, SMRai, R Discovery of MDV6058 (PF-06952229), a selective and potent TGF?R1 inhibitor: Design, synthesis and optimization. Bioorg Med Chem Lett75:0 (2022) [PubMed]
More Info.:Get all data from this article,  Assay Method
 
TGF-beta receptor type-1
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:
MEAAVAAPRPRLLLLVLAAAAAAAAALLPGATALQCFCHLCTKDNFTCVTDGLCFVSVTE
TTDKVIHNSMCIAEIDLIPRDRPFVCAPSSKTGSVTTTYCCNQDHCNKIELPTTVKSSPG
LGPVELAAVIAGPVCFVCISLMLMVYICHNRTVIHHRVPNEEDPSLDRPFISEGTTLKDL
IYDMTTSGSGSGLPLLVQRTIARTIVLQESIGKGRFGEVWRGKWRGEEVAVKIFSSREER
SWFREAEIYQTVMLRHENILGFIAADNKDNGTWTQLWLVSDYHEHGSLFDYLNRYTVTVE
GMIKLALSTASGLAHLHMEIVGTQGKPAIAHRDLKSKNILVKKNGTCCIADLGLAVRHDS
ATDTIDIAPNHRVGTKRYMAPEVLDDSINMKHFESFKRADIYAMGLVFWEIARRCSIGGI
HEDYQLPYYDLVPSDPSVEEMRKVVCEQKLRPNIPNRWQSCEALRVMAKIMRECWYANGA
ARLTALRIKKTLSQLSQQEGIKM
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50405402
n/a
NameBDBM50405402
Synonyms:CHEMBL5267945
TypeSmall organic molecule
Emp. Form.C20H18ClFN4O
Mol. Mass.384.835
SMILESCC(C)c1cnc(cc1Nc1ccncc1C(N)=O)-c1cc(Cl)ccc1F
Structure
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