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Target
Tafazzin/Transcriptional enhancer factor TEF-3 [217-434]/Transcriptional coactivator YAP1 [60-100]
Ligand
BDBM695400
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:
BDBM695400
Synonyms:
US12083101, Example 121
Type:
Small organic molecule
Emp. Form.:
n/a
Mol. Mass.:
n/a
SMILES:
CNC(=O)c1ccc(OCCO)c(F)c1-c1c2[C@H](C)[C@](CN[C@H]3CC[C@](C)(O)CC3)(Oc2cc(F)c1Cl)c1ccccc1 |r,wU:19.40,22.22,25.26,wD:17.18,25.27,(4.82,4.26,;3.48,5.03,;2.15,4.26,;1.38,2.93,;.82,5.03,;.82,6.57,;-.52,7.34,;-1.85,6.57,;-3.19,7.34,;-4.52,6.57,;
Structure:
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