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ChEMBL ligand: CHEMBL31741 (L-701324) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Beta-lactamase AmpC in Escherichia coli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2026] [UniProtKB: P00811] | ||||||||
ChEMBL | Inhibition of Escherichia coli AmpC beta lactamase using relaxed assay conditions in presence of 0.00001% Triton X-100 detergent | B | 4.66 | pIC50 | 22000 | nM | IC50 | J Med Chem (2007) 50: 2385-2390 [PMID:17447748] |
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 | Inhibition of [3H]glycine binding to NMDA receptor in rat brain membranes | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (2006) 49: 864-871 [PMID:16451052] |
ChEMBL | In vitro inhibitory concentration against binding of the [3H]glycine to strychnine-insensitive glycine binding sites of rat N-methyl-D-aspartate glutamate receptor | B | 7.88 | pIC50 | 13.2 | nM | IC50 | J Med Chem (2005) 48: 995-1018 [PMID:15715469] |
ChEMBL | Affinity for the glycine binding site on rat N-methyl-D-aspartate glutamate receptor 1, determined by displacement of the glycine site antagonist [3H]L-689,560 from rat cortical membranes | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (1997) 40: 4053-4068 [PMID:9406596] |
ChEMBL | In vitro inhibition of [3H]glycine at NMDA receptor | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (1994) 37: 4053-4067 [PMID:7990104] |
GtoPdb | Measuring inhibition of [3H]L-689,560 binding to the strychnine-insensitive glycine site on rat brain membranes. | - | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (1994) 37: 1402-5 [PMID:8182696] |
GluN1/GluN2B/Glutamate NMDA receptor; Grin1/Grin2b in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096666] [GtoPdb: 455, 457] [UniProtKB: P35439, Q00960] | ||||||||
ChEMBL | Antagonistic activity for suppression of membrane current response elicited by fixed concentration of glycine and glutamate in Xenopus oocyte expressing N-methyl-D-aspartate glutamate receptor 1/2B | F | 7.74 | pIC50 | 18 | nM | IC50 | J Med Chem (1999) 42: 4394-4404 [PMID:10543883] |
GtoPdb | Measuring inhibition of [3H]L-689,560 binding to the strychnine-insensitive glycine site on rat brain membranes. | - | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (1994) 37: 1402-5 [PMID:8182696] |
GluN1/Glutamate (NMDA) receptor subunit zeta 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL330] [GtoPdb: 455] [UniProtKB: P35439] | ||||||||
ChEMBL | Displacement of [3H]-5-7 dichlorokynurenic acid ([3H]- DCKA) from N-methyl-D-aspartate glutamate receptor glycine site of rat brain membrane homogenate | B | 7.85 | pKi | 14 | nM | Ki | J Med Chem (1999) 42: 4394-4404 [PMID:10543883] |
ChEMBL | Inhibition of [3H]glycine to glycine binding site, associated with the N-methyl-D-aspartate glutamate receptor 1 in crude synaptic membranes prepared from adult rat cerebral cortex. | B | 9 | pKi | 1 | nM | Ki | J Med Chem (1997) 40: 841-850 [PMID:9083472] |
ChEMBL | In vitro ability to displace [3H]L-689,560 binding to glycine site on the N-methyl-D-aspartate (NMDA) glutamate receptor 1 from rat cortical membranes | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (1997) 40: 754-765 [PMID:9057862] |
ChEMBL | Inhibition of the binding of [3H]L-689,560 ([3H]-4) to the strychnine-insensitive glycine site on rat brain membranes | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (1994) 37: 1402-1405 [PMID:8182696] |
ChEMBL | Inhibition of binding of [3H]glycine to N-methyl-D-aspartate glutamate receptor 1 from crude synaptic membranes prepared from adult rat cerebral cortex. | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (1998) 41: 808-820 [PMID:9526557] |
ChEMBL | Compound was evaluated for its ability to displace [3H]-L-689,560 from rat cortical membrane | B | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2089-2092 |
GtoPdb | Measuring inhibition of [3H]L-689,560 binding to the strychnine-insensitive glycine site on rat brain membranes. | - | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (1994) 37: 1402-5 [PMID:8182696] |
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]