glycine [Ligand Id: 727] 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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| 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 (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] |
| 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 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]
