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Target
Tafazzin/Transcriptional enhancer factor TEF-3 [217-434]/Transcriptional coactivator YAP1 [60-100]
Ligand
BDBM695382
Substrate
n/a
Meas. Tech.
In-Vitro Biochemical Assays
IC50
2.00±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:
BDBM695382
Synonyms:
US12083101, Example 107
Type:
Small organic molecule
Emp. Form.:
n/a
Mol. Mass.:
n/a
SMILES:
C[C@H]1c2c(O[C@]1(CN)c1ccccc1)cc(F)c(Cl)c2-c1c(F)c(OCCO)ccc1C(N)=O |r,wU:5.8,wD:1.0,(3.37,.27,;2.28,-.82,;.82,-1.3,;.82,-2.84,;2.28,-3.31,;3.19,-2.07,;4.52,-2.84,;4.52,-4.38,;4.52,-1.3,;5.85,-2.07,;7.19,-1.3,;7.19,.24,;5.85,1.01,;4.52,.24,;-.52,-3.61,;-1.85,-2.84,;-3.19,-3.61,;-1.85,-1.3,;-3.19,-.53,;-.52,-.53,;-.52,1.3,;-1.85,2.07,;-3.19,1.3,;-1.85,3.61,;-3.19,4.38,;-4.52,3.61,;-5.85,4.38,;-7.19,3.61,;-.52,4.38,;.82,3.61,;.82,2.07,;2.15,1.3,;3.48,2.07,;2.15,-.24,)|
Structure:
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