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ChEMBL ligand: CHEMBL123132 (5-Fluorowillardiine, (S)-5-Fluorowillardiine) |
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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 | Displacement of [3H]AMPA from human Ionotropic glutamate receptor AMPA 1 expressed in HEK293 cells | B | 7.83 | pKi | 14.7 | nM | Ki | J Med Chem (1997) 40: 3645-3650 [PMID:9357531] |
ChEMBL | Agonist activity at recombinant GluA1 receptor flip isoform expressed in Xenopus oocytes | F | 6.42 | pEC50 | 382 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
ChEMBL | Agonist activity at recombinant GluA1 receptor expressed in Xenopus oocytes | F | 6.42 | pEC50 | 380 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
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 | 8.54 | pKi | 2.9 | nM | Ki | J Med Chem (2008) 51: 6614-6618 [PMID:18811139] |
ChEMBL | Agonist activity at cyclothiazide-desensitized rat recombinant flip iGluR1 expressed in Xenopus laevis oocytes by two electrode voltage-clamp electrophysiology method | F | 6.42 | pEC50 | 380 | nM | EC50 | J Med Chem (2008) 51: 6614-6618 [PMID:18811139] |
GluA2/Glutamate receptor ionotropic, AMPA 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4016] [GtoPdb: 445] [UniProtKB: P42262] | ||||||||
ChEMBL | Displacement of [3H]AMPA from human Ionotropic glutamate receptor AMPA 2 expressed in HEK293 cells | B | 7.6 | pKi | 25.1 | nM | Ki | J Med Chem (1997) 40: 3645-3650 [PMID:9357531] |
ChEMBL | Agonist activity at recombinant GluA2 receptor flip isoform expressed in Xenopus oocytes | F | 6.33 | pEC50 | 463 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
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 | 8.4 | pKi | 4 | nM | Ki | J Med Chem (2008) 51: 6614-6618 [PMID:18811139] |
ChEMBL | Agonist activity at cyclothiazide-desensitized rat recombinant flip iGluR2(Q) expressed in Xenopus laevis oocytes by two electrode voltage-clamp electrophysiology method | F | 6.34 | pEC50 | 460 | nM | EC50 | J Med Chem (2008) 51: 6614-6618 [PMID:18811139] |
GluA3/Glutamate receptor ionotropic, AMPA 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3595] [GtoPdb: 446] [UniProtKB: P42263] | ||||||||
ChEMBL | Agonist activity at recombinant GluA3 receptor expressed in Xenopus oocytes | F | 4.68 | pEC50 | 20900 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
ChEMBL | Agonist activity at recombinant GluA3 receptor flip isoform expressed in Xenopus oocytes | F | 4.68 | pEC50 | 20900 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
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 | 7.15 | pKi | 70 | nM | Ki | J Med Chem (2008) 51: 6614-6618 [PMID:18811139] |
ChEMBL | Agonist activity at cyclothiazide-desensitized rat recombinant flip iGluR3 expressed in Xenopus laevis oocytes by two electrode voltage-clamp electrophysiology method | F | 4.68 | pEC50 | 20900 | nM | EC50 | J Med Chem (2008) 51: 6614-6618 [PMID:18811139] |
GluA4/Glutamate receptor ionotropic, AMPA 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3190] [GtoPdb: 447] [UniProtKB: P48058] | ||||||||
ChEMBL | Displacement of [3H]AMPA from human Ionotropic glutamate receptor AMPA 4 expressed in HEK293 cells | B | 6.52 | pKi | 305 | nM | Ki | J Med Chem (1997) 40: 3645-3650 [PMID:9357531] |
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 | 6.91 | pKi | 123 | nM | Ki | J Med Chem (2008) 51: 6614-6618 [PMID:18811139] |
ChEMBL | Agonist activity at cyclothiazide-desensitized rat recombinant flip iGluR4 expressed in Xenopus laevis oocytes by two electrode voltage-clamp electrophysiology method | F | 4.92 | pEC50 | 11900 | nM | EC50 | J Med Chem (2008) 51: 6614-6618 [PMID:18811139] |
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 | 5.86 | pKi | 1380 | nM | Ki | J Med Chem (2008) 51: 6614-6618 [PMID:18811139] |
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 | 4 | pKi | >100000 | nM | Ki | J Med Chem (2008) 51: 6614-6618 [PMID:18811139] |
GluK5/Glutamate receptor ionotropic kainate 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2675] [GtoPdb: 454] [UniProtKB: Q16478] | ||||||||
ChEMBL | Displacement of [3H]kainate from human Ionotropic glutamate receptor ionotropic kainate 1 expressed in HEK293 cells | B | 5.74 | pKi | 1820 | nM | Ki | J Med Chem (1997) 40: 3645-3650 [PMID:9357531] |
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]