D-serine [Ligand Id: 4171] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL285123 ((d)-serine, D-Serine) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Asc-type amino acid transporter 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105976] [GtoPdb: 901] [UniProtKB: P63116] | ||||||||
| ChEMBL | Inhibition of asc-1 mediated [3H]-D-serine uptake in P2 fraction of rat forebrain synaptosomes after 4 mins by beta scintillation counting | B | 5.03 | pIC50 | 9400 | nM | IC50 | US-8741955-B2. D-serine transporter inhibitors as pharmaceutical compositions for the treatment of central nervous system disorders (null) |
| 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 | Displacement of [3H]glycine from strychnine-insensitive glycine recognition site of NMDA receptor in rat brain cortex membrane | B | 6.5 | pKi | 316.23 | nM | Ki | J Med Chem (2009) 52: 5093-5107 [PMID:19642674] |
| ChEMBL | In vitro inhibition of [3H]glycine at NMDA receptor | B | 6.52 | pIC50 | 300 | nM | IC50 | J Med Chem (1994) 37: 4053-4067 [PMID:7990104] |
| 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 | 6.8 | pEC50 | 160 | 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 | 1000 | 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 | 6.21 | pEC50 | 620 | 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 | 6.72 | pEC50 | 190 | 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 | In vitro inhibitory activity to inhibit [3H]glycine binding to NMDA receptor | B | 6.17 | pIC50 | 670 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 1409-1414 [PMID:10360746] |
| 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 | 6.82 | pEC50 | 150 | nM | EC50 | J Med Chem (2022) 65: 734-746 [PMID:34918931] |
| 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 | 1.34 | pKi | -1.34 | mM | pKi | Bioorg Med Chem (2011) 19: 6409-6418 [PMID:21955456] |
ChEMBL data shown on this page come from version 33:
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]
