GYKI53784 [Ligand Id: 4210] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL275006 (GYKI-52466) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 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 | Antagonist potency against functional AMPA receptor by kainate-induced Ca+2 in rat cerebellar granule neurons in primary culture | F | 4.66 | pIC50 | 22000 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 1203-1205 [PMID:10866381] |
| ChEMBL | Ability to inhibit kainate-induced increase of calcium in rat cerebellar granule cells expressing AMPA receptor | F | 4.66 | pIC50 | 22000 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 167-170 [PMID:16216501] |
| ChEMBL | Displacement of [3H]CP-526427 from AMPA receptor in rat forebrain membranes | B | 4.9 | pIC50 | 12600 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 167-170 [PMID:16216501] |
| ChEMBL | Ability to displace [3H]CP-526427 from the AMPA receptor binding site in rat forebrain membranes | B | 4.9 | pIC50 | 12600 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 443-446 [PMID:12565947] |
| ChEMBL | Ability to displace [3H]CP-526427 (3 nM) from binding site of the Ionotropic glutamate receptor AMPA in rat forebrain membrane | B | 4.9 | pIC50 | 12600 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 4427-4430 [PMID:14643339] |
| ChEMBL | Inhibitory activity against AMPA receptor currents in rat cortical cells stimulated with 50 uM kainic acid | F | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (1996) 39: 343-346 [PMID:8558499] |
| ChEMBL | In vitro inhibition of AMPA receptor mediated currents in primary cultured rat fetal hippocampal neurons | B | 5.05 | pIC50 | 9000 | nM | IC50 | J Med Chem (2005) 48: 4618-4627 [PMID:15999999] |
| GluA2/Glutamate receptor ionotropic, AMPA 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4016] [GtoPdb: 445] [UniProtKB: P42262] | ||||||||
| ChEMBL | Antagonist activity at open state of GFP-tagged GluA2Qflip isoform (unknown origin) expressed in HEK293S cells assessed as reduction in glutamate-induced current response in presence of 3 mM glutamate by whole cell assay relative to control | B | 5.3 | pKi | 5000 | nM | Ki | Bioorg Med Chem (2017) 25: 3631-3637 [PMID:28571973] |
| ChEMBL | Antagonist activity at closed state of GFP-tagged GluA2Qflip isoform (unknown origin) expressed in HEK293S cells assessed as reduction in glutamate-induced current response in presence of 0.1 mM glutamate by whole cell assay | B | 5.4 | pKi | 4000 | nM | Ki | Bioorg Med Chem (2017) 25: 3631-3637 [PMID:28571973] |
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]
