L701324 [Ligand Id: 4240] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL31741 (L-701324)
  • Beta-lactamase AmpC in Escherichia coli [ChEMBL: CHEMBL2026] [UniProtKB: P00811]
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  • GluN1/Glutamate (NMDA) receptor subunit zeta 1 in Rat [ChEMBL: CHEMBL330] [GtoPdb: 455] [UniProtKB: P35439]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 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]