d-AP5 [Ligand Id: 4168] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL84612
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GluN2D/GluN3B/GluN1/GluN2A/GluN2B/GluN2C/GluN3A/Glutamate [NMDA] receptor in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094124] [GtoPdb: 459, 461, 455, 456, 457, 458, 460] [UniProtKB: O15399, O60391, Q05586, Q12879, Q13224, Q14957, Q8TCU5]
ChEMBL Tested in vitro for the affinity against NMDA receptor in a cortical wedge assay B 5.43 pIC50 3700 nM IC50 Bioorg Med Chem Lett (1993) 3: 43-48
ChEMBL Tested in vitro for the affinity against NMDA receptor by examining its ability to inhibit [3H]-CGS-19,755 binding B 6.75 pIC50 177 nM IC50 Bioorg Med Chem Lett (1993) 3: 43-48
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 L-[3H]glutamate from N-methyl-D-aspartate glutamate receptor in rat brain synaptic membranes B 5.42 pKi 3830 nM Ki Bioorg Med Chem Lett (2005) 15: 2279-2283 [PMID:15837309]
ChEMBL In vitro binding affinity for rat cortical membrane N-methyl-D-aspartate glutamate receptor determined using [3H]CPP as radioligand B 6.06 pIC50 880 nM IC50 J Med Chem (2003) 46: 3102-3108 [PMID:12825948]
GluN1/GluN2A/Glutamate NMDA receptor; Grin1/Grin2a in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096680] [GtoPdb: 455, 456] [UniProtKB: P35439, Q00959]
ChEMBL Antagonist activity at recombinant rat GluN1a/GluN2A expressed in Xenopus laevis oocytes assessed as inhibition of glycine/glutamate-mediated current responses by two-electrode voltage clamp method B 6.41 pKi 390 nM Ki J Med Chem (2017) 60: 9885-9904 [PMID:29205034]
ChEMBL Inhibitory constant against (S)-glutamate and glycine evoked currents mediated by N-methyl-D-aspartate glutamate receptor NR1a/NR2A expressed in Xenopus oocytes B 6.55 pKi 280 nM Ki J Med Chem (2005) 48: 2627-2637 [PMID:15801853]
GluN1/GluN2B/Glutamate NMDA receptor; Grin1/Grin2b in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096666] [GtoPdb: 455, 457] [UniProtKB: P35439, Q00960]
ChEMBL Antagonist activity at recombinant rat GluN1a/GluN2B expressed in Xenopus laevis oocytes assessed as inhibition of glycine/glutamate-mediated current responses by two-electrode voltage clamp method B 5.55 pKi 2800 nM Ki J Med Chem (2017) 60: 9885-9904 [PMID:29205034]
ChEMBL Inhibitory constant against (S)-glutamate and glycine evoked currents mediated by N-methyl-D-aspartate glutamate receptor NR1a/NR2B expressed in Xenopus oocytes B 6.34 pKi 460 nM Ki J Med Chem (2005) 48: 2627-2637 [PMID:15801853]
GluN1/GluN2C/Glutamate NMDA receptor; Grin1/Grin2c in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096911] [GtoPdb: 455, 458] [UniProtKB: P35439, Q00961]
ChEMBL Antagonist activity at recombinant rat GluN1a/GluN2C expressed in Xenopus laevis oocytes assessed as inhibition of glycine/glutamate-mediated current responses by two-electrode voltage clamp method B 5.23 pKi 5900 nM Ki J Med Chem (2017) 60: 9885-9904 [PMID:29205034]
ChEMBL Inhibitory constant against (S)-glutamate and glycine evoked currents mediated by N-methyl-D-aspartate glutamate receptor NR1a/NR2C expressed in Xenopus oocytes B 5.79 pKi 1640 nM Ki J Med Chem (2005) 48: 2627-2637 [PMID:15801853]
GluN1/GluN2D/Ionotropic glutamate receptor NMDA 1/2D in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038506] [GtoPdb: 455, 459] [UniProtKB: P35439, Q62645]
ChEMBL Antagonist activity at recombinant rat GluN1a/GluN2D expressed in Xenopus laevis oocytes assessed as inhibition of glycine/glutamate-mediated current responses by two-electrode voltage clamp method B 4.68 pKi 21000 nM Ki J Med Chem (2017) 60: 9885-9904 [PMID:29205034]

ChEMBL data shown on this page come from version 32:

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]