(S)-5-fluorowillardiine [Ligand Id: 4070] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL123132 (5-Fluorowillardiine, (S)-5-Fluorowillardiine)
  • GluA1/Glutamate receptor ionotropic, AMPA 1 in Human [ChEMBL: CHEMBL2009] [GtoPdb: 444] [UniProtKB: P42261]
  • GluA1/Glutamate receptor ionotropic, AMPA 1 in Rat [ChEMBL: CHEMBL3753] [GtoPdb: 444] [UniProtKB: P19490]
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  • GluA2/Glutamate receptor ionotropic, AMPA 2 in Human [ChEMBL: CHEMBL4016] [GtoPdb: 445] [UniProtKB: P42262]
  • GluA2/Glutamate receptor ionotropic, AMPA 2 in Rat [ChEMBL: CHEMBL3503] [GtoPdb: 445] [UniProtKB: P19491]
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  • GluA3/Glutamate receptor ionotropic, AMPA 3 in Human [ChEMBL: CHEMBL3595] [GtoPdb: 446] [UniProtKB: P42263]
  • GluA3/Glutamate receptor ionotropic, AMPA 3 in Rat [ChEMBL: CHEMBL3504] [GtoPdb: 446] [UniProtKB: P19492]
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  • GluA4/Glutamate receptor ionotropic, AMPA 4 in Human [ChEMBL: CHEMBL3190] [GtoPdb: 447] [UniProtKB: P48058]
  • GluA4/Glutamate receptor ionotropic, AMPA 4 in Rat [ChEMBL: CHEMBL3505] [GtoPdb: 447] [UniProtKB: P19493]
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  • GluK1/Glutamate receptor ionotropic kainate 1 in Rat [ChEMBL: CHEMBL2919] [GtoPdb: 450] [UniProtKB: P22756]
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  • GluK2/Glutamate receptor ionotropic kainate 2 in Rat [ChEMBL: CHEMBL3607] [GtoPdb: 451] [UniProtKB: P42260]
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  • GluK5/Glutamate receptor ionotropic kainate 5 in Human [ChEMBL: CHEMBL2675] [GtoPdb: 454] [UniProtKB: Q16478]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 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]