[3H]AMPA [Ligand Id: 4077] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL13378 |
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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 | In vitro binding affinity against N-methyl-D-aspartate glutamate receptor using [3H]-CPG 39653 as radioligand | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1997) 40: 2831-2842 [PMID:9288165] |
| 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 [3H]CGP 39653 from NMDA receptor in rat synaptosomes | B | 4 | pKi | >100000 | nM | Ki | J Med Chem (2007) 50: 2408-2414 [PMID:17455929] |
| ChEMBL | Displacement of [3H]CGP39653 from NMDA receptor in Sprague-Dawley rat brain membranes | B | 4 | pKi | >100000 | nM | Ki | J Med Chem (2010) 53: 4110-4118 [PMID:20408529] |
| ChEMBL | Binding affinity for N-methyl-D-aspartate glutamate receptor (NMDA) using [3H]- CPP | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2002) 45: 19-31 [PMID:11754576] |
| ChEMBL | Compound was evaluated for the inhibition of binding of [3H]- CPP to NMDA receptor | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1994) 37: 878-884 [PMID:7512140] |
| ChEMBL | Compound was evaluated for the inhibition of binding of [3H]- MK-801 to NMDA receptor | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1994) 37: 878-884 [PMID:7512140] |
| ChEMBL | Binding affinity by measuring displacement of [3H]CPP from NMDA receptor in rat cortical slice preparation | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (1993) 3: 1649-1654 |
| ChEMBL | Concentration required for 50% inhibition of [3H]-CPP binding to N-methyl-D-aspartate glutamate receptor in rat cortical slice preparation | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1992) 35: 3512-3519 [PMID:1383544] |
| ChEMBL | Concentration required for 50% inhibition of [3H]-MK-801 binding to N-methyl-D-aspartate glutamate receptor in rat cortical slice preparation | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1992) 35: 3512-3519 [PMID:1383544] |
| GluN2C/Glutamate [NMDA] receptor subunit epsilon 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL401] [GtoPdb: 458] [UniProtKB: Q00961] | ||||||||
| ChEMBL | Binding affinity of compound was determined against N-methyl-D-aspartate glutamate receptor, using radioligand [3H]- CGP-39653 | B | 4 | pKi | >100000 | nM | Ki | J Med Chem (2003) 46: 2246-2249 [PMID:12747796] |
| GluN1/Glutamate (NMDA) receptor subunit zeta 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL330] [GtoPdb: 455] [UniProtKB: P35439] | ||||||||
| ChEMBL | Compound was evaluated for the inhibition of binding of [3H]glycine to NMDA receptor | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1994) 37: 878-884 [PMID:7512140] |
| GluA1/GluA2/Glutamate receptor AMPA 1/2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3883294] [GtoPdb: 444, 445] [UniProtKB: P42261, P42262] | ||||||||
| ChEMBL | Agonist activity at recombinant GluA1A2 receptor flip isoform expressed in Xenopus oocytes | F | 5.48 | pEC50 | 3310 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
| GluA1/GluA2/GluA3/GluA4/Glutamate receptor ionotropic AMPA in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2096670] [GtoPdb: 444, 445, 446, 447] [UniProtKB: P42261, P42262, P42263, P48058] | ||||||||
| ChEMBL | Inhibition of the binding of radioligand [3H]AMPA in the presence at low-affinity AMPA receptor sites. | B | 6.44 | pIC50 | 364 | nM | IC50 | J Med Chem (1991) 34: 123-130 [PMID:1825114] |
| ChEMBL | In vitro binding affinity against Ionotropic glutamate receptor AMPA using [3H]AMPA as radioligand | B | 7.64 | pIC50 | 23 | nM | IC50 | J Med Chem (1997) 40: 2831-2842 [PMID:9288165] |
| ChEMBL | Inhibition of the binding of radioligand [3H]AMPA in the presence at high-affinity AMPA receptor sites. | B | 7.72 | pIC50 | 19 | nM | IC50 | J Med Chem (1991) 34: 123-130 [PMID:1825114] |
| GluA1/GluA2/GluA4/GluA3/Glutamate receptor ionotropic, AMPA in Mouse (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2096617] [GtoPdb: 444, 445, 447, 446] [UniProtKB: P23818, P23819, Q9Z2W8, Q9Z2W9] | ||||||||
| ChEMBL | Compound was tested for in vitro binding affinity against Ionotropic glutamate receptor AMPA using [3H]AMPA ligand | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (1998) 41: 930-939 [PMID:9526567] |
| GluA1/GluA2/GluA3/GluA4/Glutamate receptor ionotropic, AMPA in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2093871] [GtoPdb: 444, 445, 446, 447] [UniProtKB: P19490, P19491, P19492, P19493] | ||||||||
| ChEMBL | Concentration required for 50% inhibition of [3H]Glu binding to AMPA receptor in rat cortical slice preparation in the presence of 2.5 mM CaCl2 | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1992) 35: 3512-3519 [PMID:1383544] |
| ChEMBL | Tested for inhibition of Specific DL-[H]Ionotropic glutamate receptor AMPA binding to rat brain membranes | B | 6.1 | pIC50 | 800 | nM | IC50 | J Med Chem (1983) 26: 901-903 [PMID:6133955] |
| ChEMBL | Binding affinity at Ionotropic glutamate receptor AMPA, using [3H]AMPA receptor binding assay. | B | 7.1 | pIC50 | 79 | nM | IC50 | J Med Chem (1992) 35: 107-111 [PMID:1370693] |
| ChEMBL | Concentration required for 50% inhibition of [3H]AMPA binding to AMPA receptor in rat cortical slice preparation | B | 7.22 | pIC50 | 60 | nM | IC50 | J Med Chem (1992) 35: 3512-3519 [PMID:1383544] |
| ChEMBL | Binding affinity by measuring displacement of [3H]AMPA from Ionotropic glutamate receptor AMPA in rat cortical slice preparation | B | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem Lett (1993) 3: 1649-1654 |
| ChEMBL | Binding affinity for Ionotropic glutamate receptor AMPA using [3H]- AMPA | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (2002) 45: 19-31 [PMID:11754576] |
| ChEMBL | Compound was evaluated for the inhibition of binding of [3H]AMPA to the AMPA receptor | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (1994) 37: 878-884 [PMID:7512140] |
| ChEMBL | In vitro binding affinity for Ionotropic glutamate receptor AMPA site was determined using [3H]AMPA as radioligand in rat cortex | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (1997) 40: 520-527 [PMID:9046343] |
| ChEMBL | Compound was evaluated for the agonist activity on AMPA receptor in rat cortical wedge preparation | F | 5.46 | pEC50 | 3500 | nM | EC50 | J Med Chem (1994) 37: 878-884 [PMID:7512140] |
| GluA1/Glutamate receptor ionotropic, AMPA 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2009] [GtoPdb: 444] [UniProtKB: P42261] | ||||||||
| ChEMBL | Binding affinity of compound was determined towards cloned Ionotropic glutamate receptor AMPA 1 (GluR1) expressed in Sf 9 insect cells | B | 7.66 | pKi | 22 | nM | Ki | J Med Chem (2003) 46: 2246-2249 [PMID:12747796] |
| GluA1/Glutamate receptor ionotropic, AMPA 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3502] [GtoPdb: 444] [UniProtKB: P23818] | ||||||||
| ChEMBL | Effective concentration of compound was determined for electrophysiological properties on Ionotropic glutamate receptor AMPA 1 using rat cortical slice model in Xenopus laevis oocytes | F | 5.06 | pEC50 | 8700 | nM | EC50 | J Med Chem (2003) 46: 2246-2249 [PMID:12747796] |
| GluA1/Glutamate receptor ionotropic, AMPA 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3753] [GtoPdb: 444] [UniProtKB: P19490] | ||||||||
| ChEMBL | Displacement of (R,S)-[5-methyl-3H]AMPA from rat recombinant flop iGluR1 expressed in Sf9 cells | B | 7.66 | pKi | 21.9 | nM | Ki | J Med Chem (2008) 51: 6614-6618 [PMID:18811139] |
| ChEMBL | Displacement of [3H]AMPA from rat recombinant GluR1 expressed in Sf9 cells | B | 10.66 | pKi | 0.02 | nM | Ki | J Med Chem (2007) 50: 2408-2414 [PMID:17455929] |
| ChEMBL | Binding affinity of compound was determined against Ionotropic glutamate receptor AMPA receptor, using radioligand [3H]- AMPA | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (2003) 46: 2246-2249 [PMID:12747796] |
| ChEMBL | Agonist activity at rat recombinant GluA1 receptor flip isoform expressed in HEK293 cells assessed as effect on cyclothiazide-induced calcium flux by Fluo-4/AM staining-based fluorescence assay | F | 4.28 | pEC50 | 53000 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
| ChEMBL | Agonist activity at rat recombinant GluA1 receptor flop isoform expressed in Xenopus oocytes | F | 5.06 | pEC50 | 8700 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
| GluA2/Glutamate receptor ionotropic, AMPA 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4016] [GtoPdb: 445] [UniProtKB: P42262] | ||||||||
| ChEMBL | Binding affinity of compound was determined towards cloned Ionotropic glutamate receptor AMPA 2 (GluR2) expressed in Sf 9 insect cells | B | 7.77 | pKi | 17 | nM | Ki | J Med Chem (2003) 46: 2246-2249 [PMID:12747796] |
| GluA2/Glutamate receptor ionotropic, AMPA 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3503] [GtoPdb: 445] [UniProtKB: P19491] | ||||||||
| ChEMBL | Displacement of (R,S)-[5-methyl-3H]AMPA from rat recombinant flop iGluR2(R) expressed in Sf9 cells | B | 7.77 | pKi | 16.8 | nM | Ki | J Med Chem (2008) 51: 6614-6618 [PMID:18811139] |
| ChEMBL | Displacement of [3H]AMPA from rat recombinant GluR2 expressed in Sf9 cells | B | 10.77 | pKi | 0.02 | nM | Ki | J Med Chem (2007) 50: 2408-2414 [PMID:17455929] |
| ChEMBL | Agonist activity at rat recombinant GluA2 receptor flip isoform expressed in HEK293 cells assessed as effect on cyclothiazide-induced calcium flux by Fluo-4/AM staining-based fluorescence assay | F | 4.17 | pEC50 | 67000 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
| GluA3/Glutamate receptor ionotropic, AMPA 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3595] [GtoPdb: 446] [UniProtKB: P42263] | ||||||||
| ChEMBL | Binding affinity of compound was determined towards cloned Ionotropic glutamate receptor AMPA 3 (GluR3) expressed in Sf 9 insect cells | B | 7.68 | pKi | 21 | nM | Ki | J Med Chem (2003) 46: 2246-2249 [PMID:12747796] |
| GluA3/Glutamate receptor ionotropic, AMPA 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3504] [GtoPdb: 446] [UniProtKB: P19492] | ||||||||
| ChEMBL | Displacement of (R,S)-[5-methyl-3H]AMPA from rat recombinant flop iGluR3 expressed in Sf9 cells | B | 7.69 | pKi | 20.6 | nM | Ki | J Med Chem (2008) 51: 6614-6618 [PMID:18811139] |
| ChEMBL | Displacement of [3H]AMPA from rat recombinant GluR3 expressed in Sf9 cells | B | 10.68 | pKi | 0.02 | nM | Ki | J Med Chem (2007) 50: 2408-2414 [PMID:17455929] |
| ChEMBL | Agonist activity at rat recombinant GluA3 receptor flip isoform expressed in HEK293 cells assessed as effect on cyclothiazide-induced calcium flux by Fluo-4/AM staining-based fluorescence assay | F | 4.43 | pEC50 | 37000 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
| ChEMBL | Effective concentration of compound was determined for electrophysiological properties on Ionotropic glutamate receptor AMPA 3 (GluR3) using rat cortical slice model in Xenopus laevis oocytes | F | 5.85 | pEC50 | 1400 | nM | EC50 | J Med Chem (2003) 46: 2246-2249 [PMID:12747796] |
| ChEMBL | Agonist activity at rat recombinant GluA3 receptor flop isoform expressed in Xenopus oocytes | F | 5.85 | pEC50 | 1400 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
| GluA4/Glutamate receptor ionotropic, AMPA 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3190] [GtoPdb: 447] [UniProtKB: P48058] | ||||||||
| ChEMBL | Binding affinity of compound was determined towards cloned Ionotropic glutamate receptor AMPA 4 (GluR4) expressed in Sf 9 insect cells | B | 7.4 | pKi | 40 | nM | Ki | J Med Chem (2003) 46: 2246-2249 [PMID:12747796] |
| GluA4/Glutamate receptor ionotropic, AMPA 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3505] [GtoPdb: 447] [UniProtKB: P19493] | ||||||||
| ChEMBL | Displacement of (R,S)-[5-methyl-3H]AMPA from rat recombinant flop iGluR4 expressed in Sf9 cells | B | 7.4 | pKi | 40 | nM | Ki | J Med Chem (2008) 51: 6614-6618 [PMID:18811139] |
| ChEMBL | Displacement of [3H]AMPA from rat recombinant GluR4 expressed in Sf9 cells | B | 10.4 | pKi | 0.04 | nM | Ki | J Med Chem (2007) 50: 2408-2414 [PMID:17455929] |
| ChEMBL | Agonist activity at rat recombinant GluA4 receptor flip isoform expressed in HEK293 cells assessed as effect on cyclothiazide-induced calcium flux by Fluo-4/AM staining-based fluorescence assay | F | 4.8 | pEC50 | 16000 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
| GluK1/GluK2/GluK3/GluK4/GluK5/Glutamate receptor ionotropic kainate in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2109241] [GtoPdb: 450, 451, 452, 453, 454] [UniProtKB: P39086, Q13002, Q13003, Q16099, Q16478] | ||||||||
| ChEMBL | In vitro binding affinity against Ionotropic glutamate receptor kainate (kainic acid) using [3H]KAIN as radioligand | B | 4.17 | pIC50 | 68000 | nM | IC50 | J Med Chem (1997) 40: 2831-2842 [PMID:9288165] |
| GluK1/GluK2/GluK3/GluK4/GluK5/Glutamate receptor ionotropic, kainate in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094119] [GtoPdb: 450, 451, 452, 453, 454] [UniProtKB: P22756, P42260, P42264, Q01812, Q63273] | ||||||||
| ChEMBL | Binding affinity for Ionotropic glutamate receptor using [3H]- kainic acid | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2002) 45: 19-31 [PMID:11754576] |
| ChEMBL | Compound was evaluated for the inhibition of binding of [3H]-Kainic acid to kianic acid receptor | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1994) 37: 878-884 [PMID:7512140] |
| ChEMBL | Binding affinity by measuring displacement of [3H]KAIN from Ionotropic glutamate receptor kainate in rat cortical slice preparation | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (1993) 3: 1649-1654 |
| ChEMBL | Concentration required for 50% inhibition of [3H]-kainic acid binding to ionotropic glutamate receptor ionotropic kainate in rat cortical slice preparation | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1992) 35: 3512-3519 [PMID:1383544] |
| ChEMBL | Binding affinity was measured by [3H]- Ionotropic glutamate receptor ionotropic kainate binding assay. | B | 4.3 | pIC50 | 50100 | nM | IC50 | J Med Chem (1992) 35: 107-111 [PMID:1370693] |
| ChEMBL | Inhibition of [3H]- Kainate binding to Ionotropic glutamate receptor kainate in brain homogenates. | B | 7.92 | pIC50 | 12 | nM | IC50 | J Med Chem (1996) 39: 4430-4438 [PMID:8893837] |
| GluK1/Glutamate receptor ionotropic kainate 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1918] [GtoPdb: 450] [UniProtKB: P39086] | ||||||||
| ChEMBL | Binding affinity of compound was determined towards cloned Ionotropic glutamate receptor ionotropic kainate 1 (GluR5) expressed in Sf 9 insect cells | B | 6.13 | pKi | 740 | nM | Ki | J Med Chem (2003) 46: 2246-2249 [PMID:12747796] |
| GluK1/Glutamate receptor ionotropic kainate 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2919] [GtoPdb: 450] [UniProtKB: P22756] | ||||||||
| ChEMBL | Displacement of [3H]SYM2081 from rat recombinant iGluR5(Q)1b expressed in Sf9 cells | B | 5.94 | pKi | 1150 | nM | Ki | J Med Chem (2008) 51: 6614-6618 [PMID:18811139] |
| ChEMBL | Displacement of [3H]SYM 2081 from rat recombinant GluR5 expressed in Sf9 cells | B | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (2007) 50: 2408-2414 [PMID:17455929] |
| GluK2/Glutamate receptor ionotropic kainate 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3683] [GtoPdb: 451] [UniProtKB: Q13002] | ||||||||
| ChEMBL | Binding affinity of compound was determined towards cloned Ionotropic glutamate receptor ionotropic kainate 6 (GluR6) expressed in Sf 9 insect cells | B | 4 | pKi | >100000 | nM | Ki | J Med Chem (2003) 46: 2246-2249 [PMID:12747796] |
| GluK2/Glutamate receptor ionotropic kainate 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3607] [GtoPdb: 451] [UniProtKB: P42260] | ||||||||
| ChEMBL | Displacement of [3H]KA from rat recombinant GluR6 expressed in Sf9 cells | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2007) 50: 2408-2414 [PMID:17455929] |
| GluK3/Glutamate receptor ionotropic kainate 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3744] [GtoPdb: 452] [UniProtKB: P42264] | ||||||||
| ChEMBL | Binding affinity of compound was determined against Ionotropic glutamate receptor ionotropic kainate, using radioligand [3H]- KA | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2003) 46: 2246-2249 [PMID:12747796] |
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]
