Reaction Details Report a problem with these data
Target
Tafazzin/Transcriptional enhancer factor TEF-3 [217-434]/Transcriptional coactivator YAP1 [60-100]
Ligand
BDBM695261
Substrate
n/a
Meas. Tech.
In-Vitro Biochemical Assays
IC50
3.00±n/a nM
Citation
 Bordas, V; Brocklehurst, C; Chene, P; Furet, P; Guagnano, V; Imbach-Weese, P; Kallen, J; Le Douget, M; Lorthiois, EL; McKenna, J; Salem, B; Schmelzle, T; Sellner, H; Soldermann, N; Voegtle, M; Wartmann, M Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors US Patent  US12083101 Publication Date 9/10/2024 
Target
Name:
Tafazzin/Transcriptional enhancer factor TEF-3 [217-434]/Transcriptional coactivator YAP1 [60-100]
Synonyms:
Transcriptional coactivator (YAP)/Tafazzin (TAZ)- Transcriptional enhancer factor TEF-3 (TEAD4)
Type:
Protein
Mol. Mass.:
n/a
Description:
n/a
Components:
This complex has 3 components.
Component 1
Name:
Transcriptional enhancer factor TEF-3 [217-434]
Synonyms:
Transcriptional enhancer factor TEF-3 (TEAD4)(217-434)
Type:
Enzyme Catalytic Domain
Mol. Mass.:
25409.87
Organism:
Human
Description:
Q15561[217-434]
Residue:
218
Sequence:
RSVASSKLWMLEFSAFLEQQQDPDTYNKHLFVHIGQSSPSYSDPYLEAVDIRQIYDKFPEKKGGLKDLFERGPSNAFFLVKFWADLNTNIEDEGSSFYGVSSQYESPENMIITCSTKVCSFGKQVVEKVETEYARYENGHYSYRIHRSPLCEYMINFIHKLKHLPEKYMMNSVLENFTILQVVTNRDTQETLLCIAYVFEVSASEHGAQHHIYRLVKE
  
Component 2
Name:
Transcriptional coactivator YAP1 [60-100]
Synonyms:
Transcriptional coactivator YAP1 (60-100)
Type:
Protein
Mol. Mass.:
4644.27
Organism:
Homo sapiens (Human)
Description:
P46937[60-100]
Residue:
41
Sequence:
DSETDLEALFNAVMNPKTANVPQTVPMRLRKLPDSFFKPPE
  
Component 3
Name:
Tafazzin
Synonyms:
Protein G4.5 | Taz
Type:
Protein
Mol. Mass.:
30216.65
Organism:
Human
Description:
Q16635
Residue:
262
Sequence:
MPLHVKWPFPAVPPLTWTLASSVVMGLVGTYSCFWTKYMNHLTVHNREVLYELIEKRGPATPLITVSNHQSCMDDPHLWGILKLRHIWNLKLMRWTPAAADICFTKELHSHFFSLGKCVPVCRGDGVYQKGMDFILEKLNHGDWVHIFPEGKVNMSSEFLRFKWGIGRLIAECHLNPIILPLWHVGMNDVLPNSPPYFPRFGQKITVLIGKPFSALPVLERLRAENKSAVEMRKALTDFIQEEFQHLKTQAEQLHNHLQPGR
  
Inhibitor
Name:
BDBM695261
Synonyms:
US12083101, Example 10
Type:
Small organic molecule
Emp. Form.:
n/a
Mol. Mass.:
n/a
SMILES:
NC[C@]1(Cc2c(O1)ccc(Cl)c2-c1c(F)c(OCCO)ccc1C(N)=O)c1ccccc1 |r,wU:2.28,(3.57,-4.37,;3.96,-2.88,;2.88,-1.79,;1.97,-.55,;.51,-1.02,;.51,-2.56,;1.97,-3.04,;-.83,-3.33,;-2.16,-2.56,;-2.16,-1.02,;-3.49,-.25,;-.83,-.25,;-.83,1.29,;-2.16,2.06,;-3.49,1.29,;-2.16,3.6,;-3.49,4.37,;-4.83,3.6,;-6.16,4.37,;-7.5,3.6,;-.83,4.37,;.51,3.6,;.51,2.06,;1.84,1.29,;3.17,2.06,;2.61,-.05,;4.42,-1.79,;5.19,-3.13,;6.73,-3.13,;7.5,-1.79,;6.73,-.46,;5.19,-.46,)|
Structure:
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