D-cycloserine [Ligand Id: 9489] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL771 (Cycloserinum, NSC-154851, Orientomycin, Seromycin, D-cycloserine, Cicloserina, NSC-76029, Cycloserine) |
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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 | In vitro inhibition of [3H]glycine at NMDA receptor | B | 5.64 | pIC50 | 2300 | nM | IC50 | 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 | 5.53 | pEC50 | 2950 | nM | EC50 | Bioorg Med Chem Lett (1999) 9: 1409-1414 [PMID:10360746] |
| GluN1/GluN2A/Glutamate NMDA receptor; GRIN1/GRIN2A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907604] [GtoPdb: 455, 456] [UniProtKB: Q05586, Q12879] | ||||||||
| ChEMBL | Agonist activity at recombinant human GluN1/2A expressed in Xenopus laevis oocytes by TEVC recording method | B | 4.68 | pEC50 | 21000 | nM | EC50 | J Med Chem (2024) 67: 20135-20155 [PMID:39560374] |
| GluN1/GluN2A/Glutamate NMDA receptor; Grin1/Grin2a in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096680] [GtoPdb: 455, 456] [UniProtKB: P35439, Q00959] | ||||||||
| ChEMBL | Partial agonist activity at wild-type rat GluN1/2A expressed in Xenopus laevis oocytes by TEVC recording method | B | 4.72 | pEC50 | 19000 | nM | EC50 | J Med Chem (2024) 67: 20135-20155 [PMID:39560374] |
| ChEMBL | Agonist activity at recombinant rat GluN1/GluN2A NMDA receptor expressed in xenopus laevis oocytes in presence of glutamate by two-electrode voltage-clamp method | B | 4.74 | pEC50 | 18000 | nM | EC50 | J Med Chem (2025) 68: 3572-3590 [PMID:39847708] |
| GluN1/GluN2B/Glutamate NMDA receptor; GRIN1/GRIN2B in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907603] [GtoPdb: 455, 457] [UniProtKB: Q05586, Q13224] | ||||||||
| ChEMBL | Agonist activity at recombinant human GluN1/2B expressed in Xenopus laevis oocytes by TEVC recording method | B | 5.13 | pEC50 | 7400 | nM | EC50 | J Med Chem (2024) 67: 20135-20155 [PMID:39560374] |
| 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 recombinant rat GluN1/GluN2B NMDA receptor expressed in xenopus laevis oocytes in presence of glutamate by two-electrode voltage-clamp method | B | 5.08 | pEC50 | 8300 | nM | EC50 | J Med Chem (2025) 68: 3572-3590 [PMID:39847708] |
| ChEMBL | Partial agonist activity at wild-type rat GluN1/2B expressed in Xenopus laevis oocytes by TEVC recording method | B | 5.09 | pEC50 | 8200 | nM | EC50 | J Med Chem (2024) 67: 20135-20155 [PMID:39560374] |
| GluN1/GluN2C/Glutamate NMDA receptor; Grin1/Grin2c in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096911] [GtoPdb: 455, 458] [UniProtKB: P35439, Q00961] | ||||||||
| ChEMBL | Partial agonist activity at wild-type rat GluN1/2C expressed in Xenopus laevis oocytes by TEVC recording method | B | 5.48 | pEC50 | 3300 | nM | EC50 | J Med Chem (2024) 67: 20135-20155 [PMID:39560374] |
| ChEMBL | Agonist activity at recombinant rat GluN1/GluN2C NMDA receptor expressed in xenopus laevis oocytes in presence of glutamate by two-electrode voltage-clamp method | B | 5.55 | pEC50 | 2800 | nM | EC50 | J Med Chem (2025) 68: 3572-3590 [PMID:39847708] |
| GluN1/Glutamate receptor ionotropic, NMDA 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 | 5.13 | pIC50 | 7370 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 1409-1414 [PMID:10360746] |
| GluN2C/Glutamate receptor ionotropic, NMDA 2C in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL401] [GtoPdb: 458] [UniProtKB: Q00961] | ||||||||
| ChEMBL | Compound was evaluated for in vitro inhibition of [3H]TCP at NMDA receptor. | B | 4.74 | pEC50 | 18100 | nM | EC50 | J Med Chem (1994) 37: 4053-4067 [PMID:7990104] |
| GluN1/GluN2C/Ionotropic glutamate receptor NMDA 1/2C in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038504] [GtoPdb: 455, 458] [UniProtKB: Q05586, Q14957] | ||||||||
| ChEMBL | Agonist activity at recombinant human GluN1/2C expressed in Xenopus laevis oocytes by TEVC recording method | B | 5.35 | pEC50 | 4500 | nM | EC50 | J Med Chem (2024) 67: 20135-20155 [PMID:39560374] |
| GluN2D/GluN1/Ionotropic glutamate receptor NMDA 1/2D in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038505] [GtoPdb: 459, 455] [UniProtKB: O15399, Q05586] | ||||||||
| ChEMBL | Agonist activity at recombinant human GluN1/2D expressed in Xenopus laevis oocytes by TEVC recording method | B | 5.82 | pEC50 | 1500 | nM | EC50 | J Med Chem (2024) 67: 20135-20155 [PMID:39560374] |
| GluN1/GluN2D/Ionotropic glutamate receptor NMDA 1/2D in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038506] [GtoPdb: 455, 459] [UniProtKB: P35439, Q62645] | ||||||||
| ChEMBL | Partial agonist activity at wild-type rat GluN1/2D expressed in Xenopus laevis oocytes by TEVC recording method | B | 5.54 | pEC50 | 2900 | nM | EC50 | J Med Chem (2024) 67: 20135-20155 [PMID:39560374] |
| ChEMBL | Agonist activity at recombinant rat GluN1/GluN2D NMDA receptor expressed in xenopus laevis oocytes in presence of glutamate by two-electrode voltage-clamp method | B | 5.55 | pEC50 | 2800 | nM | EC50 | J Med Chem (2025) 68: 3572-3590 [PMID:39847708] |
| 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 | 0.64 | pKi | -0.64 | mM | pKi | Bioorg Med Chem (2011) 19: 6409-6418 [PMID:21955456] |
ChEMBL data shown on this page come from version 37:
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]
