[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 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]
