Ki Summary new BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
TargetTGF-beta receptor type I
LigandBDBM50428286
Substrate/Competitorn/a
Meas. Tech.ChEMBL_946470
IC50 3700±n/a nM
Citation Rheault TRStellwagen JCAdjabeng GMHornberger KRPetrov KGWaterson AGDickerson SHMook RALaquerre SGKing AJRossanese OWArnone MRSmitheman KNKane-Carson LSHan CMoorthy GSMoss KGUehling DE Discovery of Dabrafenib: A Selective Inhibitor of Raf Kinases with Antitumor Activity against B-Raf-Driven Tumors. ACS Med Chem Lett 4:358-62 (2013) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
TGF-beta receptor type I
Name:TGF-beta receptor type I
Synonyms:2.7.11.30 | ALK-5 | ALK5 | ALK5 | ALK5/TGFBR1 | Activin A receptor type II-like protein kinase of 53kD | Activin receptor-like kinase 5 | Activin receptor-like kinase 5 (ALK-5) | Activin receptor-like kinase 5 (ALK5/TGFbeta) | P36897 | SKR4 | TGF-beta receptor type-1 | TGF-beta receptor type-1 (TGFR1) | TGFBR1 | Transforming Growth Factor
Type:n/a
Mol. Mass.:55968.24
Organism:Homo sapiens (Human)
Description:n/a
Residue:503
Sequence:
MEAAVAAPRPRLLLLVLAAAAAAAAALLPGATALQCFCHLCTKDNFTCVTDGLCFVSVTE
TTDKVIHNSMCIAEIDLIPRDRPFVCAPSSKTGSVTTTYCCNQDHCNKIELPTTVKSSPG
LGPVELAAVIAGPVCFVCISLMLMVYICHNRTVIHHRVPNEEDPSLDRPFISEGTTLKDL
IYDMTTSGSGSGLPLLVQRTIARTIVLQESIGKGRFGEVWRGKWRGEEVAVKIFSSREER
SWFREAEIYQTVMLRHENILGFIAADNKDNGTWTQLWLVSDYHEHGSLFDYLNRYTVTVE
GMIKLALSTASGLAHLHMEIVGTQGKPAIAHRDLKSKNILVKKNGTCCIADLGLAVRHDS
ATDTIDIAPNHRVGTKRYMAPEVLDDSINMKHFESFKRADIYAMGLVFWEIARRCSIGGI
HEDYQLPYYDLVPSDPSVEEMRKVVCEQKLRPNIPNRWQSCEALRVMAKIMRECWYANGA
ARLTALRIKKTLSQLSQQEGIKM
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50428286
n/a
NameBDBM50428286
Synonyms:DABRAFENIB | GSK2118436A
TypeSmall organic molecule
Emp. Form.C23H20F3N5O2S2
Mol. Mass.519.562
SMILESCC(C)(C)c1nc(c(s1)-c1ccnc(N)n1)-c1cccc(NS(=O)(=O)c2c(F)cccc2F)c1F
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: