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Target
Tafazzin/Transcriptional enhancer factor TEF-3 [217-434]/Transcriptional coactivator YAP1 [60-100]
Ligand
BDBM695280
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:
BDBM695280
Synonyms:
US12083101, Example 28a
Type:
Small organic molecule
Emp. Form.:
n/a
Mol. Mass.:
n/a
SMILES:
COc1ccc(C(N)=O)c(c1F)-c1c2C[C@](CN[C@H]3CC[C@@H](CC3)C(O)=O)(Oc2ccc1Cl)c1ccccc1 |r,wU:15.36,18.18,wD:21.25,(-7.85,15.21,;-6.52,15.98,;-5.19,15.21,;-3.85,15.98,;-2.52,15.21,;-2.52,13.67,;-1.18,12.9,;.15,13.67,;-1.18,11.36,;-3.85,12.9,;-5.19,13.67,;-6.52,12.9,;-3.85,10.96,;-2.52,10.19,;-1.05,10.66,;-.15,9.42,;1.18,8.65,;1.18,7.11,;2.52,6.34,;3.85,7.11,;5.19,6.34,;5.19,4.8,;3.85,4.03,;2.52,4.8,;6.52,4.03,;7.85,4.8,;6.52,2.49,;-1.05,8.17,;-2.52,8.65,;-3.85,7.88,;-5.19,8.65,;-5.19,10.19,;-6.52,10.96,;1.18,10.19,;2.52,9.42,;3.85,10.19,;3.85,11.73,;2.52,12.5,;1.18,11.73,)|
Structure:
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