glycine [Ligand Id: 727] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL773 (Aminoacetic acid, FEMA NO. 3287, Glycine, Glycocoll, Glycolixir, 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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  • GPRC6 receptor in Human [GtoPdb: 55] [UniProtKB: Q5T6X5]
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  • Glycine Receptor (All subtypes) in Human [GtoPdb: 428]
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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: 455, 456, 457, 458, 459, 461, 460] [UniProtKB: P35439, Q00959, Q00960, Q00961, Q62645, Q8VHN2, Q9R1M7]
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: 455, 456] [UniProtKB: P35439, Q00959]
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: 455, 457] [UniProtKB: P35439, Q00960]
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: 455, 458] [UniProtKB: P35439, Q00961]
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: 455, 459] [UniProtKB: P35439, Q62645]
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 (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]
GPRC6 receptor in Human [GtoPdb: 55] [UniProtKB: Q5T6X5]
GtoPdb - - 3.6 pEC50 - - - Mol Pharmacol (2005) 67: 589-97 [PMID:15576628]
Glycine Receptor (All subtypes) in Human [GtoPdb: 428]
GtoPdb - - 4.6 pEC50 - - - EMBO J (1993) 12: 3729-37 [PMID:8404844];
EMBO J (1997) 16: 110-20 [PMID:9009272]

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]