Target
Gamma-secretase-activating protein
Ligand
BDBM50458159
Substrate
n/a
Meas. Tech.
ChEMBL_2267394
IC50
6.2±n/a nM
Citation
 Liao, MZhang, JWang, GWang, LLiu, JOuyang, LLiu, B Small-Molecule Drug Discovery in Triple Negative Breast Cancer: Current Situation and Future Directions. J Med Chem 64:2382-2418 (2021) [PubMed] 
Target
Name:
Gamma-secretase-activating protein
Synonyms:
GSAP | GSAP_HUMAN | Gamma-secretase | PION
Type:
Protein
Mol. Mass.:
97808.44
Organism:
Homo sapiens (Human)
Description:
A4D1B5
Residue:
854
Sequence:
MALRLVADFDLGKDVLPWLRAQRAVSEASGAGSGGADVLENDYESLHVLNVERNGNIIYTYKDDKGNVVFGLYDCQTRQNELLYTFEKDLQVFSCSVNSERTLLAASLVQSTKEGKRNELQPGSKCLTLLVEIHPVNNVKVLKAVDSYIWVQFLYPHIESHPLPENHLLLISEEKYIEQFRIHVAQEDGNRVVIKNSGHLPRDRIAEDFVWAQWDMSEQRLYYIDLKKSRSILKCIQFYADESYNLMFEVPLDISLSNSGFKLVNFGCDYHQYRDKFSKHLTLCVFTNHTGSLCVCYSPKCASWGQITYSVFYIHKGHSKTFTTSLENVGSHMTKGITFLNLDYYVAVYLPGHFFHLLNVQHPDLICHNLFLTGNNEMIDMLPHCPLQSLSGSLVLDCCSGKLYRALLSQSSLLQLLQNTCLDCEKMAALHCALYCGQGAQFLEAQIIQWISENVSACHSFDLIQEFIIASSYWSVYSETSNMDKLLPHSSVLTWNTEIPGITLVTEDIALPLMKVLSFKGYWEKLNSNLEYVKYAKPHFHYNNSVVRREWHNLISEEKTGKRRSAAYVRNILDNAVKVISNLEARNLGPRLTPLLQEEDSHQRLLMGLMVSELKDHFLRHLQGVEKKKIEQMVLDYISKLLDLICHIVETNWRKHNLHSWVLHFNSRGSAAEFAVFHIMTRILEATNSLFLPLPPGFHTLHTILGVQCLPLHNLLHCIDSGVLLLTETAVIRLMKDLDNTEKNEKLKFSIIVRLPPLIGQKICRLWDHPMSSNIISRNHVTRLLQNYKKQPRNSMINKSSFSVEFLPLNYFIEILTDIESSNQALYPFEGHDNVDAEFVEEAALKHTAMLLGL
  
Inhibitor
Name:
BDBM50458159
Synonyms:
Nirogacestat | PF 03084014 | PF 3084014 | PF-03084014 | PF-3084014
Type:
Small organic molecule
Emp. Form.:
C27H41F2N5O
Mol. Mass.:
489.6441
SMILES:
CCC[C@H](N[C@H]1CCc2cc(F)cc(F)c2C1)C(=O)Nc1cn(cn1)C(C)(C)CNCC(C)(C)C |r|
Structure:
Search PDB for entries with ligand similarity: