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ChEMBL ligand: CHEMBL435582 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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GluA1/Glutamate receptor ionotropic, AMPA 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2009] [GtoPdb: 444] [UniProtKB: P42261] | ||||||||
ChEMBL | Inhibition of GluR1 expressed in HEK cells | B | 5.25 | pEC50 | 5650 | nM | EC50 | J Med Chem (2010) 53: 7271-7279 [PMID:20839777] |
GtoPdb | - | - | 5.25 | pEC50 | 5650 | nM | EC50 | Neuropharmacology (2001) 40: 976-83 [PMID:11406188] |
GluA2/Glutamate receptor ionotropic, AMPA 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4016] [GtoPdb: 445] [UniProtKB: P42262] | ||||||||
ChEMBL | Activity against human GLUR2 flop expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay | F | 5.72 | pEC50 | 1905 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 5057-5061 [PMID:16879964] |
ChEMBL | Inhibition of GluR2 flop expressed in HEK cells | B | 5.84 | pEC50 | 1440 | nM | EC50 | J Med Chem (2010) 53: 7271-7279 [PMID:20839777] |
ChEMBL | Activity against human GLUR2 flip expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay | F | 6.25 | pEC50 | 559 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 5057-5061 [PMID:16879964] |
GtoPdb | - | - | 6.82 | pEC50 | 150 | nM | EC50 | Neuropharmacology (2001) 40: 976-83 [PMID:11406188] |
ChEMBL | Agonist activity at GluR2 receptor | F | 6.82 | pEC50 | 150 | nM | EC50 | J Med Chem (2010) 53: 7271-7279 [PMID:20839777] |
GluA3/Glutamate receptor ionotropic, AMPA 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3595] [GtoPdb: 446] [UniProtKB: P42263] | ||||||||
ChEMBL | Inhibition of GluR3 expressed in HEK cells | B | 5.78 | pEC50 | 1660 | nM | EC50 | J Med Chem (2010) 53: 7271-7279 [PMID:20839777] |
GtoPdb | - | - | 5.78 | pEC50 | 1660 | nM | EC50 | Neuropharmacology (2001) 40: 976-83 [PMID:11406188] |
GluA4/Glutamate receptor ionotropic, AMPA 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3190] [GtoPdb: 447] [UniProtKB: P48058] | ||||||||
ChEMBL | Activity against human GLUR4 flop expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay | F | 5.97 | pEC50 | 1061 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 5057-5061 [PMID:16879964] |
ChEMBL | Activity against human GLUR4 flip expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay | F | 6.38 | pEC50 | 420 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 5057-5061 [PMID:16879964] |
ChEMBL | Tested for potentiation towards human iGluR4 receptor expressed in HEK293 cells | F | 6.54 | pEC50 | 290 | nM | EC50 | J Med Chem (2000) 43: 4354-4358 [PMID:11087558] |
ChEMBL | Potentiation of responses mediated by 100 uM L-glutamate in transfected HEK293 cells expressing human homomeric iGluR4 flip receptors. | F | 6.54 | pEC50 | 290 | nM | EC50 | J Med Chem (2002) 45: 2101-2111 [PMID:11985477] |
ChEMBL | Inhibition of GluR4 expressed in HEK293 cells | B | 6.54 | pEC50 | 290 | nM | EC50 | J Med Chem (2010) 53: 7271-7279 [PMID:20839777] |
GtoPdb | - | - | 6.68 | pEC50 | 210 | nM | EC50 | Neuropharmacology (2001) 40: 976-83 [PMID:11406188] |
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]