N-arachidonoylglycine [Ligand Id: 3635] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL161343 (Arachidonoyl Glycine, N-Arachidonoylglycine, N-Arachidonylglycine, N-Arachidonyl Glycine)
  • Fatty acid amide hydrolase/Anandamide amidohydrolase in Human [ChEMBL: CHEMBL2243] [GtoPdb: 1400] [UniProtKB: O00519]
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  • CB1 receptor/Cannabinoid CB1 receptor in Human [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
  • CB1 receptor/Cannabinoid CB1 receptor in Rat [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272]
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  • CB2 receptor/Cannabinoid CB2 receptor in Human [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
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  • LPA5 receptor in Human [GtoPdb: 124] [UniProtKB: Q9H1C0]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Fatty acid amide hydrolase/Anandamide amidohydrolase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2243] [GtoPdb: 1400] [UniProtKB: O00519]
ChEMBL Inhibition of fatty acid amide hydrolase; range = 4.1-7 uM B 5.15 pIC50 7000 nM IC50 J Med Chem (2005) 48: 5059-5087 [PMID:16078824]
CB1 receptor/Cannabinoid CB1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
ChEMBL Displacement of [3H]CP55,940 from human recombinant CB1 receptor expressed in CHO-K1 cells B 5 pKi >10000 nM Ki Medchemcomm (2014) 5: 632-649
CB1 receptor/Cannabinoid CB1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272]
ChEMBL In vitro binding affinity was determined against rat brain Cannabinoid receptor 1 B 5 pKi >10000 nM Ki J Med Chem (1997) 40: 659-667 [PMID:9057852]
CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
ChEMBL Displacement of [3H]CP55,940 from human recombinant CB2 receptor expressed in HEK293 cells B 5 pKi >10000 nM Ki Medchemcomm (2014) 5: 632-649
GlyT2/Glycine transporter 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3060] [GtoPdb: 936] [UniProtKB: Q9Y345]
ChEMBL Reversible non-competitive inhibition of human GlyT2a expressed in Xenopus laevis oocytes by two-electrode voltage clamp electrophysiology B 5.05 pIC50 9000 nM IC50 J Med Chem (2019) 62: 2466-2484 [PMID:30714733]
ChEMBL Inhibition of GlyT-2 (unknown origin) B 5.52 pIC50 3000 nM IC50 J Med Chem (2018) 61: 2652-2679 [PMID:28876062]
GPR55/G-protein coupled receptor 55 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075322] [GtoPdb: 109] [UniProtKB: Q9Y2T6]
ChEMBL Antagonist activity against human GPR55 expressed in CHO cells assessed as reduction in LPI-induced beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method B 5 pIC50 >10000 nM IC50 Medchemcomm (2014) 5: 632-649
GPR18/N-arachidonyl glycine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2384898] [GtoPdb: 89] [UniProtKB: Q14330]
ChEMBL Antagonist activity against human GPR18 expressed in CHO cells assessed as reduction in delta9-THC-induced beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method B 5 pIC50 >10000 nM IC50 Medchemcomm (2014) 5: 632-649
ChEMBL Antagonist activity at Prolink1-tagged human GPR18 receptor expressed in CHO cells assessed as inhibition of THC-induced beta arrestin recruitment after 90 mins by beta-galactosidase based topcount luminescence analysis F 5 pIC50 >10000 nM IC50 ACS Med Chem Lett (2020) 11: 2024-2031 [PMID:33062188]
ChEMBL Agonist activity at Prolink1-tagged human GPR18 receptor expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase based topcount luminescence analysis B 5 pEC50 >10000 nM EC50 ACS Med Chem Lett (2020) 11: 2024-2031 [PMID:33062188]
ChEMBL Agonist activity at recombinant human GPR18 expressed in HEK293 cells assessed as induction of p44/42 MAPK phosphorylation after 5 mins by Western blot analysis F 7.36 pEC50 44 nM EC50 Eur J Med Chem (2018) 155: 381-397 [PMID:29902723]
ChEMBL Agonist activity at recombinant full length human GPR18 expressed in CHO cells assessed as forskolin-stimulated cAMP accumulation after 10 mins by enzyme immunoassay F 7.7 pEC50 20 nM EC50 Eur J Med Chem (2018) 155: 381-397 [PMID:29902723]
GtoPdb - - 7.7 pEC50 20 nM EC50 Br J Pharmacol (2012) 165: 2414-24 [PMID:21595653]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay F 4.8 pIC50 15848.93 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay F 4.8 pIC50 15848.93 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay F 4.8 pIC50 15848.93 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
LPA5 receptor in Human [GtoPdb: 124] [UniProtKB: Q9H1C0]
GtoPdb - - 4.3 pEC50 >50000 nM EC50 J Biol Chem (2009) 284: 17304-19 [PMID:19366702];
J Biol Chem (2008) 283: 21054-64 [PMID:18499677]

ChEMBL data shown on this page come from version 32:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]