tezampanel [Ligand Id: 4245] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL14935 (LY-293,558, LY-293558, NGX-424, NGX424, Tezampanel anhydrous) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| 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 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]
