tezampanel [Ligand Id: 4245] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL14935 (LY-293558, LY-293,558, NGX-424) |
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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 | Inhibitory activity against NMDA receptor using [3H]-CGS- 19755 as radioligand | B | 4.92 | pIC50 | 12100 | nM | IC50 | J Med Chem (1993) 36: 2046-2048 [PMID:8393116] |
| 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 | Compound was tested for NMDA receptor antagonistic activity by measuring its ability to inhibit depolarizations induced by 40 uM NMDA in rat cortical slice preparation. | F | 4.21 | pIC50 | 61300 | nM | IC50 | J Med Chem (1996) 39: 2219-2231 [PMID:8667365] |
| ChEMBL | Antagonism at NMDA receptor by inhibition of depolarizations induced by 40 uM NMDA in rat cortical slice preparation. | F | 4.21 | pIC50 | 61000 | nM | IC50 | J Med Chem (1996) 39: 2232-2244 [PMID:8667366] |
| ChEMBL | Affinity of [3H]-CGS- 19755 radioligand to rat N-methyl-D-aspartate (NMDA) receptor | B | 4.58 | pIC50 | 26400 | nM | IC50 | J Med Chem (1996) 39: 2232-2244 [PMID:8667366] |
| ChEMBL | Binding affinity against NMDA receptor using [3H]-CGS- 19755 as a radioligand in rat | B | 4.58 | pIC50 | 26400 | nM | IC50 | J Med Chem (1995) 38: 4885-4890 [PMID:8523401] |
| ChEMBL | Binding affinity at N-methyl-D-aspartate glutamate receptor in rat cortical tissue by [3H]-CGS- 19755 displacement. | B | 4.58 | pIC50 | 26400 | nM | IC50 | J Med Chem (1996) 39: 2219-2231 [PMID:8667365] |
| ChEMBL | Inhibition of NMDA receptor glutamate site from rat cortical membrane | B | 4.92 | pIC50 | 12100 | nM | IC50 | J Med Chem (2010) 53: 5367-5382 [PMID:20356304] |
| ChEMBL | Affinity of [3H]-CGS- 19755 radioligand to rat N-methyl-D-aspartate (NMDA) receptor | B | 4.92 | pIC50 | 12100 | nM | IC50 | J Med Chem (1996) 39: 2232-2244 [PMID:8667366] |
| ChEMBL | In vitro binding affinity towards glycine modulatory site on the NMDA receptors using [3H]DCKA as radioligand in rat cortical membrane preparations | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 2921-2926 [PMID:10571148] |
| ChEMBL | Displacement of [3H]DCKA from glycine NMDA receptor of rat cortical membranes | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 1205-1210 [PMID:11354378] |
| ChEMBL | Binding affinity for N-methyl-D-aspartate glutamate receptor | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2749-2754 [PMID:11133083] |
| ChEMBL | Displacement of [3H]DCKA from N-methyl-D-aspartate glutamate receptor of rat cortical membrane | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 1133-1137 [PMID:10843235] |
| ChEMBL | In vitro binding affinity towards NMDA glutamate receptor using [3H]5,7-dichlorokynurenate as ligand on rat cortical membrane preparations | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 127-132 [PMID:11206442] |
| 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 | Binding affinity against Ionotropic glutamate receptor AMPA using [3H]AMPA as a radioligand | B | 5.32 | pIC50 | 4800 | nM | IC50 | J Med Chem (1995) 38: 4885-4890 [PMID:8523401] |
| ChEMBL | Inhibitory activity against AMPA receptor using [3H]AMPA as radioligand | B | 5.87 | pIC50 | 1350 | nM | IC50 | J Med Chem (1993) 36: 2046-2048 [PMID:8393116] |
| 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 | Binding affinity against Ionotropic glutamate receptor AMPA using [3H]AMPA 19755 radioligand | B | 4.85 | pIC50 | 14000 | nM | IC50 | J Med Chem (1996) 39: 2232-2244 [PMID:8667366] |
| ChEMBL | Antagonism at AMPA receptor by inhibition of depolarizations induced by 40 uM AMPA in rat cortical slice preparation. | F | 5.22 | pIC50 | 6000 | nM | IC50 | J Med Chem (1996) 39: 2232-2244 [PMID:8667366] |
| ChEMBL | AMPA receptor antagonistic activity as inhibition of depolarizations induced by 40 uM AMPA in rat cortical slice preparation | F | 5.22 | pIC50 | 6000 | nM | IC50 | J Med Chem (1996) 39: 2219-2231 [PMID:8667365] |
| ChEMBL | Binding affinity at Ionotropic glutamate receptor AMPA in rat cortical tissue by [3H]AMPA displacement. | B | 5.32 | pIC50 | 4800 | nM | IC50 | J Med Chem (1996) 39: 2219-2231 [PMID:8667365] |
| ChEMBL | Binding affinity against Ionotropic glutamate receptor AMPA using [3H]AMPA 19755 radioligand | B | 5.32 | pIC50 | 4800 | nM | IC50 | J Med Chem (1996) 39: 2232-2244 [PMID:8667366] |
| ChEMBL | Antagonism at AMPA receptor by inhibition of depolarizations induced by 40 uM AMPA in rat cortical slice preparation. | F | 5.74 | pIC50 | 1800 | nM | IC50 | J Med Chem (1996) 39: 2232-2244 [PMID:8667366] |
| ChEMBL | Displacement of [3H]AMPA from Ionotropic glutamate receptor AMPA of rat cortical membranes | B | 6.22 | pIC50 | 600 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 1133-1137 [PMID:10843235] |
| ChEMBL | Affinity towards Ionotropic glutamate receptor AMPA using [3H]AMPA as ligand on rat cortical membrane preparations | B | 6.22 | pIC50 | 600 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 127-132 [PMID:11206442] |
| ChEMBL | In vitro binding affinity towards ionotropic glutamate receptor AMPA using [3H]AMPA as radioligand in rat cortical membrane preparations | B | 6.22 | pIC50 | 600 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 2921-2926 [PMID:10571148] |
| ChEMBL | Displacement of [3H]AMPA from Ionotropic glutamate receptor AMPA of rat cortical membranes | B | 6.22 | pIC50 | 600 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 1205-1210 [PMID:11354378] |
| ChEMBL | Binding affinity for Ionotropic glutamate receptor AMPA | B | 6.22 | pIC50 | 600 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2749-2754 [PMID:11133083] |
| ChEMBL | Antagonistic activity against Ionotropic glutamate receptor AMPA using kainate-evoked current in Xenopus oocytes injected with rat brain mRNA | F | 6.64 | pIC50 | 230 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2749-2754 [PMID:11133083] |
| GluA1/Glutamate receptor ionotropic, AMPA 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2009] [GtoPdb: 444] [UniProtKB: P42261] | ||||||||
| ChEMBL | Ability to displace binding of [3H]AMPA to recombinant human Ionotropic glutamate receptor AMPA 1 | B | 5.04 | pKi | 9200 | nM | Ki | J Med Chem (2002) 45: 4383-4386 [PMID:12238915] |
| ChEMBL | Binding affinity to GluR1 | B | 5.04 | pKi | 9200 | nM | Ki | J Med Chem (2010) 53: 5367-5382 [PMID:20356304] |
| GluA2/Glutamate receptor ionotropic, AMPA 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4016] [GtoPdb: 445] [UniProtKB: P42262] | ||||||||
| ChEMBL | Ability to displace binding of [3H]AMPA to recombinant human Ionotropic glutamate receptor AMPA 2 | B | 5.49 | pKi | 3200 | nM | Ki | J Med Chem (2002) 45: 4383-4386 [PMID:12238915] |
| ChEMBL | Binding affinity to GluR2 | B | 5.49 | pKi | 3200 | nM | Ki | J Med Chem (2010) 53: 5367-5382 [PMID:20356304] |
| ChEMBL | Displacement of [3H]AMPA from homomeric recombinant GluA2 receptor (unknown origin) | B | 5.52 | pKi | 3000 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 6463-6466 [PMID:24140446] |
| ChEMBL | Inhibition of [3H]AMPA binding to human Ionotropic glutamate receptor 2 | B | 5.66 | pKi | 2210 | nM | Ki | J Med Chem (2005) 48: 4200-4203 [PMID:15974569] |
| GluA3/Glutamate receptor ionotropic, AMPA 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3595] [GtoPdb: 446] [UniProtKB: P42263] | ||||||||
| ChEMBL | Ability to displace binding of [3H]AMPA to recombinant human Ionotropic glutamate receptor AMPA 3 | B | 4.49 | pKi | 32000 | nM | Ki | J Med Chem (2002) 45: 4383-4386 [PMID:12238915] |
| ChEMBL | Binding affinity to GluR3 | B | 4.49 | pKi | 32000 | nM | Ki | J Med Chem (2010) 53: 5367-5382 [PMID:20356304] |
| GluA4/Glutamate receptor ionotropic, AMPA 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3190] [GtoPdb: 447] [UniProtKB: P48058] | ||||||||
| ChEMBL | Binding affinity to GluR4 | B | 4.3 | pKi | 50500 | nM | Ki | J Med Chem (2010) 53: 5367-5382 [PMID:20356304] |
| ChEMBL | Ability to displace binding of [3H]AMPA to recombinant human Ionotropic glutamate receptor AMPA 4 | B | 4.3 | pKi | 50000 | nM | Ki | J Med Chem (2002) 45: 4383-4386 [PMID:12238915] |
| 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 | Antagonism at Ionotropic glutamate receptor kainate by inhibition of depolarizations induced by 10 uM kainic acid in rat cortical slice preparation. | F | 4.5 | pIC50 | 31700 | nM | IC50 | J Med Chem (1996) 39: 2232-2244 [PMID:8667366] |
| ChEMBL | Ionotropic glutamate receptor kainate antagonism by measuring inhibition of 10 uM kainic acid induced depolarizations in rat cortical slice preparation. | F | 4.5 | pIC50 | 31700 | nM | IC50 | J Med Chem (1996) 39: 2219-2231 [PMID:8667365] |
| ChEMBL | Binding affinity against Ionotropic glutamate receptor kainate using [3H]-Kainic acid 19755 radioligand | B | 4.55 | pIC50 | 28100 | nM | IC50 | J Med Chem (1996) 39: 2232-2244 [PMID:8667366] |
| ChEMBL | Inhibitory activity against generation of currents by 50 uM kainate in Xenopus oocytes injected with rat brain mRNA | F | 6.64 | pIC50 | 230 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 1133-1137 [PMID:10843235] |
| GluK1/Glutamate receptor ionotropic kainate 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1918] [GtoPdb: 450] [UniProtKB: P39086] | ||||||||
| ChEMBL | Binding affinity to GluR5 | B | 5.38 | pKi | 4200 | nM | Ki | J Med Chem (2010) 53: 5367-5382 [PMID:20356304] |
| ChEMBL | Displacement of [3H]ATPA from human Gluk1 receptor | B | 5.38 | pKi | 4200 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 6463-6466 [PMID:24140446] |
| ChEMBL | Inhibition of [3H]-KA binding to iontropic glutamate receptor 5 | B | 5.38 | pKi | 4160 | nM | Ki | J Med Chem (2005) 48: 4200-4203 [PMID:15974569] |
| ChEMBL | Inhibition of GluK1 receptor (unknown origin) | B | 6.3 | pIC50 | 500 | nM | IC50 | J Med Chem (2013) 56: 593-624 [PMID:23121096] |
| GluK2/Glutamate receptor ionotropic kainate 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3683] [GtoPdb: 451] [UniProtKB: Q13002] | ||||||||
| ChEMBL | Ability to displace binding of [3H]AMPA to recombinant human AMPA receptor Ionotropic glutamate receptor ionotropic kainate 2 | B | 4 | pKi | >100000 | nM | Ki | J Med Chem (2002) 45: 4383-4386 [PMID:12238915] |
| ChEMBL | Ability to displace binding of [3H]KA to recombinant human KA receptor Ionotropic glutamate receptor ionotropic kainate 2 expressed in EK 293 cell membranes | B | 4 | pKi | >100000 | nM | Ki | J Med Chem (2002) 45: 4383-4386 [PMID:12238915] |
| ChEMBL | Inhibition of [3H]KA binding to iontropic glutamate receptor 6 | B | 4 | pKi | >100000 | nM | Ki | J Med Chem (2005) 48: 4200-4203 [PMID:15974569] |
| ChEMBL | Binding affinity to GluR6 | B | 4 | pKi | >100000 | nM | Ki | J Med Chem (2010) 53: 5367-5382 [PMID:20356304] |
| GluK3/Glutamate receptor ionotropic kainate 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3684] [GtoPdb: 452] [UniProtKB: Q13003] | ||||||||
| ChEMBL | Binding affinity to GluR7 | B | 4 | pKi | >100000 | nM | Ki | J Med Chem (2010) 53: 5367-5382 [PMID:20356304] |
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]
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