[3H]CPP [Ligand Id: 4082] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL22304 |
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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 | 6.22 | pIC50 | 600 | 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 | 6.66 | pIC50 | 220 | 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 | Inhibition against NMDA receptor by displacement of [3H]TCP binding from rat cortical membranes | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1994) 37: 3008-3015 [PMID:7932522] |
| ChEMBL | Tested for binding affinity against NMDA receptor, from rat synaptic membrane, using [3H]glycine as the radioligand. | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1993) 36: 331-342 [PMID:8093907] |
| ChEMBL | Tested for binding affinity against NMDA receptor, from rat synaptic membrane, using [3H]TCP as the radioligand. | B | 4.35 | pIC50 | 45000 | nM | IC50 | J Med Chem (1993) 36: 331-342 [PMID:8093907] |
| ChEMBL | Affinity for the NMDA receptor site was assessed by its ability to displace [3H]TCP from its binding site in rat brain | B | 4.35 | pIC50 | 45000 | nM | IC50 | J Med Chem (2001) 44: 1516-1529 [PMID:11334562] |
| ChEMBL | Compound tested for affinity towards N-methyl-D-aspartate glutamate receptor by measuring their ability to displace [3H]TCP from rat brain | B | 4.35 | pIC50 | 45000 | nM | IC50 | J Med Chem (1992) 35: 4720-4726 [PMID:1361582] |
| ChEMBL | Inhibition of NMDA receptor binding affinity in rat brain synaptosomal membrane using [3H]glutamate as radioligand | B | 6.08 | pIC50 | 837 | nM | IC50 | J Med Chem (1995) 38: 1955-1965 [PMID:7783127] |
| ChEMBL | Inhibition of [3H]-CGS- 19755 binding to N-methyl-D-aspartic acid receptors in rat crude synaptic membranes | B | 6.66 | pIC50 | 220 | nM | IC50 | J Med Chem (1989) 32: 2171-2178 [PMID:2549246] |
| ChEMBL | Tested for the ability to inhibit the specific binding of [3H]-CGS- 19755 to NMDA recognition sites on rat brain membranes | B | 6.72 | pIC50 | 190 | nM | IC50 | Bioorg Med Chem Lett (1993) 3: 33-38 |
| ChEMBL | Inhibition of NMDA receptor binding affinity in rat brain synaptosomal membrane was determined by [3H]-CGP- 39653 as radioligand | B | 6.83 | pIC50 | 148 | nM | IC50 | J Med Chem (1995) 38: 1955-1965 [PMID:7783127] |
| ChEMBL | Displacement of [3H]CPP from rat synaptic membrane glutamate NMDA receptor | B | 6.95 | pIC50 | 112.6 | nM | IC50 | J Med Chem (2001) 44: 1516-1529 [PMID:11334562] |
| ChEMBL | Tested for binding affinity against NMDA receptor, from rat synaptic membrane, using [3H]-CPP as the radioligand. | B | 6.95 | pIC50 | 112.6 | nM | IC50 | J Med Chem (1993) 36: 331-342 [PMID:8093907] |
| ChEMBL | Ability to displace [3H]CPP from NMDA receptor in rat brain membrane | B | 7.09 | pIC50 | 82 | nM | IC50 | J Med Chem (1992) 35: 1345-1370 [PMID:1533422] |
| ChEMBL | N-methyl-D-aspartate glutamate receptor antagonistic activity was assessed from the ability to displace [3H]CPP29,30 from rat cortical membranes. | F | 7.1 | pIC50 | 80 | nM | IC50 | J Med Chem (1989) 32: 1580-1590 [PMID:2544728] |
| ChEMBL | Inhibition of N-methyl-D-aspartate glutamate receptor by using [3H]CPP as a radioligand from the rat cortical membranes. | B | 7.1 | pIC50 | 79 | nM | IC50 | J Med Chem (1990) 33: 2916-2924 [PMID:2145436] |
| ChEMBL | Inhibitory activity evaluated by its ability to displace [3H]CPP from rat cortical membrane receptor at 10E-5 concentration of the compound | B | 7.1 | pIC50 | 79 | nM | IC50 | J Med Chem (1992) 35: 1371-1384 [PMID:1533423] |
| ChEMBL | Tested for the inhibitory activity against NMDA receptor site as measured in a [3H]CPP binding assay of rat brain neuronal membranes | B | 7.1 | pIC50 | 79 | nM | IC50 | Bioorg Med Chem Lett (1993) 3: 39-42 |
| ChEMBL | Compound was evaluated for its ability to displace [3H]CCP binding for NMDA receptor | B | 7.55 | pIC50 | 28 | nM | IC50 | Bioorg Med Chem Lett (1992) 2: 207-212 |
| GluA1/Glutamate receptor ionotropic, AMPA 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3753] [GtoPdb: 444] [UniProtKB: P19490] | ||||||||
| ChEMBL | Binding affinity towards AMPA receptor using [3H]AMPA as radioligand; Inactive | B | 4 | pKi | >100000 | nM | Ki | J Med Chem (1990) 33: 2961-2963 [PMID:1977908] |
| GluK3/Glutamate receptor ionotropic kainate 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3744] [GtoPdb: 452] [UniProtKB: P42264] | ||||||||
| ChEMBL | Binding affinity towards Ionotropic glutamate receptor kainate using [3H]-kainic acid as radioligand; Inactive | B | 4 | pKi | >100000 | nM | Ki | J Med Chem (1990) 33: 2961-2963 [PMID:1977908] |
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]
