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Inhibitor Report for: AKU-005

Dual inhibitor of MAGL and FAAH: IC50 0.2-1.1 nM MAGL 63 nM FAAH


General
Type Piperazine, Triazol
Chemical_Nomenclature (4-benzhydrylpiperazin-1-yl)-(1,2,4-triazol-1-yl)methanone
Canonical SMILES C1CN(CCN1C(C2=CC=CC=C2)C3=CC=CC=C3)C(=O)N4C=NC=N4
InChI InChI=1S/C20H21N5O/c26-20(25-16-21-15-22-25)24-13-11-23(12-14-24)19(17-7-3-1-4-8-17)18-9-5-2-6-10-18/h1-10,15-16,19H,11-14H2
InChIKey DAHGNJMKRWHRFF-UHFFFAOYSA-N
Other name(s) CHEMBL3356956 ; BDBM50102829
________________________________________________________________________________________________
MW|347.4
Formula|C20H21N5O
CAS_number|
PubChem|118721876
UniChem|DAHGNJMKRWHRFF-UHFFFAOYSA-N
IUPHAR|
Wikipedia|

Target
Families | AKU-005 ligand of proteins in family: Monoglyceridelipase_lysophospholip
Protein | human-MGLL

References:
Search PubMed for references concerning: AKU-005
    Title: Potent dual MAGL/FAAH inhibitor AKU-005 engages endocannabinoids to diminish meningeal nociception implicated in migraine pain
    Della Pietra A, Krivoshein G, Ivanov K, Giniatullina R, Jyrkkanen HK, Leinonen V, Lehtonen M, van den Maagdenberg A, Savinainen J, Giniatullin R
    Ref: J Headache Pain, 24:38, 2023 : PubMed

            

    Title: Inhibiting Endocannabinoid Hydrolysis as Emerging Analgesic Strategy Targeting a Spectrum of Ion Channels Implicated in Migraine Pain
    Della Pietra A, Savinainen J, Giniatullin R
    Ref: Int J Mol Sci, 23:, 2022 : PubMed

            

    Title: Piperazine and piperidine triazole ureas as ultrapotent and highly selective inhibitors of monoacylglycerol lipase
    Aaltonen N, Savinainen JR, Ribas CR, Ronkko J, Kuusisto A, Korhonen J, Navia-Paldanius D, Hayrinen J, Takabe P and Laitinen JT <7 more author(s)>
    Ref: Chemical Biology, 20:379, 2013 : PubMed