AMPA [Ligand Id: 4131] 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]kainic acid from rat recombinant iGluR6(V,C,R) receptor expressed in Sf9 cells | B | 3 | pKi | >1000000 | nM | Ki | J Med Chem (2008) 51: 6614-6618 [PMID:18811139] |
| 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 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]
