[14C]glycine [Ligand Id: 4635] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL773 (Aminoacetic acid, FEMA NO. 3287, Glycolixir, Glycocoll, Glycine, NSC-25936)
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  • GluN1/Glutamate (NMDA) receptor subunit zeta 1 in Rat [ChEMBL: CHEMBL330] [GtoPdb: 455] [UniProtKB: P35439]
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  • glycine receptor α1 subunit/Glycine receptor subunit alpha-1 in Human [ChEMBL: CHEMBL5845] [GtoPdb: 423] [UniProtKB: P23415]
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  • Proton-coupled Amino acid Transporter 1/Proton-coupled amino acid transporter 1 in Human [ChEMBL: CHEMBL1914279] [GtoPdb: 1161] [UniProtKB: Q7Z2H8]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A/Glutamate NMDA receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907608] [GtoPdb: 455456457458459461460] [UniProtKB: P35439Q00959Q00960Q00961Q62645Q8VHN2Q9R1M7]
ChEMBL Affinity for the glycine binding site of NMDA receptor by inhibition of [3H]5,7-dichlorokynurenic acid ([3H]DCKA) binding to rat brain synaptic membrane B 6.77 pKi 170 nM Ki J. Med. Chem. (1994) 37: 3956-3968 [PMID:7966156]
ChEMBL Displacement of [3H]glycine from strychnine-insensitive glycine recognition site of NMDA receptor in rat brain cortex membrane B 6.9 pKi 125.89 nM Ki J. Med. Chem. (2009) 52: 5093-5107 [PMID:19642674]
ChEMBL Binding affinity against glycine binding site associated with N-methyl-D-aspartate glutamate receptor of rat synaptic plasma membrane(SPM) determined using [3H]glycine as radioligand. B 6.16 pIC50 690 nM IC50 J. Med. Chem. (1992) 35: 4135-4142 [PMID:1433216]
ChEMBL In vitro inhibition of [3H]glycine at NMDA receptor B 6.7 pIC50 200 nM IC50 J. Med. Chem. (1994) 37: 4053-4067 [PMID:7990104]
ChEMBL Tested for binding affinity against NMDA receptor, from rat synaptic membrane, using [3H]glycine as the radioligand. B 7.07 pIC50 86 nM IC50 J. Med. Chem. (1993) 36: 331-342 [PMID:8093907]
ChEMBL Compound was evaluated for in vitro inhibition of [3H]TCP at NMDA receptor B 6.7 pEC50 200 nM EC50 J. Med. Chem. (1994) 37: 4053-4067 [PMID:7990104]
ChEMBL In vitro concentration eliciting half-maximal effect on [3H]-MK 801 radioligand binding to NMDA receptor B 7.17 pEC50 68 nM EC50 Bioorg. Med. Chem. Lett. (1999) 9: 1409-1414 [PMID:10360746]
GluN1/Glutamate (NMDA) receptor subunit zeta 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL330] [GtoPdb: 455] [UniProtKB: P35439]
ChEMBL Inhibitory concentration required to inhibit [3H]strychnine binding to N-methyl-D-aspartate glutamate receptor 1 B 5.21 pIC50 6200 nM IC50 J. Med. Chem. (1992) 35: 233-241 [PMID:1310117]
ChEMBL In vitro inhibitory activity to inhibit [3H]glycine binding to NMDA receptor B 6.6 pIC50 250 nM IC50 Bioorg. Med. Chem. Lett. (1999) 9: 1409-1414 [PMID:10360746]
glycine receptor α1 subunit/Glycine receptor subunit alpha-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5845] [GtoPdb: 423] [UniProtKB: P23415]
ChEMBL Antagonist activity at human glycine alpha-1 receptor in HEK293 cells by FMP assay F 4.02 pEC50 95499.26 nM EC50 J. Med. Chem. (2007) 50: 4616-4629 [PMID:17722904]
ChEMBL Antagonist activity at human glycine alpha-1 receptor in HEK293 cells by FMP assay F 4.03 pEC50 94000 nM EC50 J. Med. Chem. (2007) 50: 4616-4629 [PMID:17722904]
GlyT1/Glycine transporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2337] [GtoPdb: 935] [UniProtKB: P48067]
ChEMBL Inhibition of GlyT1 (unknown origin) assessed as inhibition of [14C]glycine uptake B 4.5 pIC50 31600 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 1067-1070 [PMID:24461352]
Olfactory receptor 51E2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523454] [UniProtKB: Q9H255]
ChEMBL Agonist activity at PSGR/OR51E2 (unknown origin) expressed in human Hana3A cells co-transfected with CRE-Luc by luciferase reporter gene assay B 7.24 pEC50 58 nM EC50 US-20180116992-A1. Modulators of Prostate-Specific G-Protein Receptor (PSGR/OR51E2) and Methods of Using Same (null)
Proton-coupled Amino acid Transporter 1/Proton-coupled amino acid transporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1914279] [GtoPdb: 1161] [UniProtKB: Q7Z2H8]
ChEMBL Inhibition of human PAT1-mediated L-[3H]proline uptake in human Caco2 cells after 10 mins by liquid scintillation counting B 0.71 pKi -0.71 mM pKi Bioorg. Med. Chem. (2011) 19: 6409-6418 [PMID:21955456]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]