Reaction Details Report a problem with these data
Target
Tafazzin/Transcriptional enhancer factor TEF-3 [217-434]/Transcriptional coactivator YAP1 [60-100]
Ligand
BDBM695397
Substrate
n/a
Meas. Tech.
In-Vitro Biochemical Assays
IC50
1.000±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:
BDBM695397
Synonyms:
US12083101, Example 118
Type:
Small organic molecule
Emp. Form.:
n/a
Mol. Mass.:
n/a
SMILES:
C[C@H]1c2c(O[C@]1(CNC1CCC1)c1ccccc1)cc(F)c(Cl)c2-c1c(F)c(OCCO)ccc1C(N)=O |r,wU:5.13,wD:1.0,(3.09,1.4,;2,.31,;.54,-.17,;.54,-1.71,;2,-2.18,;2.91,-.94,;4.24,-1.71,;4.24,-3.25,;5.58,-4.02,;5.98,-5.51,;7.46,-5.11,;7.06,-3.62,;4.24,-.17,;5.58,-.94,;6.91,-.17,;6.91,1.37,;5.58,2.14,;4.24,1.37,;-.79,-2.48,;-2.13,-1.71,;-3.46,-2.48,;-2.13,-.17,;-3.46,.6,;-.79,.6,;-.79,2.43,;-2.13,3.2,;-3.46,2.43,;-2.13,4.74,;-3.46,5.51,;-4.8,4.74,;-6.13,5.51,;-7.46,4.74,;-.79,5.51,;.54,4.74,;.54,3.2,;1.87,2.43,;3.21,3.2,;1.87,.89,)|
Structure:
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