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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]