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

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ChEMBL ligand: CHEMBL773 (Aminoacetic acid, FEMA NO. 3287, Glycine, Glycocoll, 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/GluN2A/Glutamate NMDA receptor; Grin1/Grin2a in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096680] [GtoPdb: 455456] [UniProtKB: P35439Q00959]
ChEMBL Agonist activity at rat GluN1/GluN2A NMDA receptor expressed in Xenopus oocytes measured after 4 days in presence of L-glutamte by two-electrode voltage-clamp recording assay B 6 pEC50 990 nM EC50 J Med Chem (2022) 65: 734-746 [PMID:34918931]
GluN1/GluN2B/Glutamate NMDA receptor; Grin1/Grin2b in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096666] [GtoPdb: 455457] [UniProtKB: P35439Q00960]
ChEMBL Agonist activity at rat GluN1/GluN2B NMDA receptor expressed in Xenopus oocytes measured after 4 days in presence of L-glutamte by two-electrode voltage-clamp recording assay B 6.62 pEC50 240 nM EC50 J Med Chem (2022) 65: 734-746 [PMID:34918931]
GluN1/GluN2C/Glutamate NMDA receptor; Grin1/Grin2c in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096911] [GtoPdb: 455458] [UniProtKB: P35439Q00961]
ChEMBL Agonist activity at rat GluN1/GluN2C NMDA receptor expressed in Xenopus oocytes measured after 4 days in presence of L-glutamte by two-electrode voltage-clamp recording assay B 6.68 pEC50 210 nM EC50 J Med Chem (2022) 65: 734-746 [PMID:34918931]
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]
GluN1/GluN2D/Ionotropic glutamate receptor NMDA 1/2D in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038506] [GtoPdb: 455459] [UniProtKB: P35439Q62645]
ChEMBL Agonist activity at rat GluN1/GluN2D NMDA receptor expressed in Xenopus oocytes measured after 4 days in presence of L-glutamte by two-electrode voltage-clamp recording assay B 7.04 pEC50 91 nM EC50 J Med Chem (2022) 65: 734-746 [PMID:34918931]
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 F 7.24 pEC50 58 nM EC50 US-20180116992-A1. Modulators of Prostate-Specific G-Protein Receptor (PSGR/OR51E2) and Methods of Using Same (2018)
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 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]