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
Stucture :
Protein : human-MGLL
References (3)
| Title : Potent dual MAGL\/FAAH inhibitor AKU-005 engages endocannabinoids to diminish meningeal nociception implicated in migraine pain - Della Pietra_2023_J.Headache.Pain_24_38 |
| Author(s) : 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 |
| Abstract : Della Pietra_2023_J.Headache.Pain_24_38 |
| ESTHER : Della Pietra_2023_J.Headache.Pain_24_38 |
| PubMedSearch : Della Pietra_2023_J.Headache.Pain_24_38 |
| PubMedID: 37038131 |
| Gene_locus related to this paper: human-MGLL |
| Title : Inhibiting Endocannabinoid Hydrolysis as Emerging Analgesic Strategy Targeting a Spectrum of Ion Channels Implicated in Migraine Pain - Della Pietra_2022_Int.J.Mol.Sci_23_ |
| Author(s) : Della Pietra A , Savinainen J , Giniatullin R |
| Ref : Int J Mol Sci , 23 : , 2022 |
| Abstract : Della Pietra_2022_Int.J.Mol.Sci_23_ |
| ESTHER : Della Pietra_2022_Int.J.Mol.Sci_23_ |
| PubMedSearch : Della Pietra_2022_Int.J.Mol.Sci_23_ |
| PubMedID: 35457225 |
| Gene_locus related to this paper: human-MGLL |
| Title : Piperazine and piperidine triazole ureas as ultrapotent and highly selective inhibitors of monoacylglycerol lipase - Aaltonen_2013_Chem.Biol_20_379 |
| Author(s) : Aaltonen N , Savinainen JR , Ribas CR , Ronkko J , Kuusisto A , Korhonen J , Navia-Paldanius D , Hayrinen J , Takabe P , Kasnanen H , Pantsar T , Laitinen T , Lehtonen M , Pasonen-Seppanen S , Poso A , Nevalainen T , Laitinen JT |
| Ref : Chemical Biology , 20 :379 , 2013 |
| Abstract : Aaltonen_2013_Chem.Biol_20_379 |
| ESTHER : Aaltonen_2013_Chem.Biol_20_379 |
| PubMedSearch : Aaltonen_2013_Chem.Biol_20_379 |
| PubMedID: 23521796 |
| Gene_locus related to this paper: human-MGLL |