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 (2014) |
| 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 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]
