(S)-4-AHCP [Ligand Id: 4069] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL28472
1 CHEMBL28472_lig_chart_1 Glutamate NMDA receptor Rat
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2 CHEMBL28472_lig_chart_2 Glutamate receptor ionotropic, AMPA Rat
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  • 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]
  • 4.5
3 CHEMBL28472_lig_chart_3 Glutamate receptor ionotropic, AMPA 1 HumanRat
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  • GluA2/Glutamate receptor ionotropic, AMPA 2 in Rat [ChEMBL: CHEMBL3503] [GtoPdb: 445] [UniProtKB: P19491]
  • 4.5
4 CHEMBL28472_lig_chart_4 Glutamate receptor ionotropic, AMPA 2 Rat
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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]
  • 4.5
5 CHEMBL28472_lig_chart_5 Glutamate receptor ionotropic, AMPA 3 HumanRat
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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]
  • 4.49
6 CHEMBL28472_lig_chart_6 Glutamate receptor ionotropic, AMPA 4 HumanRat
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7 CHEMBL28472_lig_chart_7 Glutamate receptor ionotropic, kainate Rat
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  • GluK1/Glutamate receptor ionotropic kainate 1 in Rat [ChEMBL: CHEMBL2919] [GtoPdb: 450] [UniProtKB: P22756]
  • 4.49
8 CHEMBL28472_lig_chart_8 Glutamate receptor ionotropic kainate 1 Rat
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  • Glutamate receptor ionotropic kainate 2 in Xenopus laevis [ChEMBL: CHEMBL3395] [UniProtKB: B9V8S1]
  • GluK2/Glutamate receptor ionotropic kainate 2 in Rat [ChEMBL: CHEMBL3607] [GtoPdb: 451] [UniProtKB: P42260]
  • This target only has 1 pki data point
  • 4
9 CHEMBL28472_lig_chart_9 Glutamate receptor ionotropic kainate 2 Xenopus laevisRat
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  • GluK3/Glutamate receptor ionotropic kainate 3 in Rat [ChEMBL: CHEMBL3744] [GtoPdb: 452] [UniProtKB: P42264]
  • 4.47
10 CHEMBL28472_lig_chart_10 Glutamate receptor ionotropic kainate 3 Rat
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  • GluK5/Glutamate receptor ionotropic kainate 5 in Human [ChEMBL: CHEMBL2675] [GtoPdb: 454] [UniProtKB: Q16478]
  • This target only has 0 pki data point
  • 0
11 CHEMBL28472_lig_chart_11 Glutamate receptor ionotropic kainate 5 Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A/Glutamate NMDA receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907608] [GtoPdb: 455456457458459461460] [UniProtKB: P35439Q00959Q00960Q00961Q62645Q8VHN2Q9R1M7]
ChEMBL Displacement of [3H]CGP from NMDA receptor in rat cortical synaptosomes B 4 pKi >100000 nM Ki J. Med. Chem. (2009) 52: 4911-4922 [PMID:19588945]
GluA1/GluA2/GluA3/GluA4/Glutamate receptor ionotropic, AMPA in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2093871] [GtoPdb: 444445446447] [UniProtKB: P19490P19491P19492P19493]
ChEMBL Ability to displace [3H]AMPA radioligand at Ionotropic glutamate receptor AMPA in rat cortical membranes B 6.55 pIC50 280 nM IC50 J. Med. Chem. (2003) 46: 1350-1358 [PMID:12672235]
GluA1/Glutamate receptor ionotropic, AMPA 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2009] [GtoPdb: 444] [UniProtKB: P42261]
ChEMBL Electrophysiological data on Xenopus oocytes, expressing homomeric Ionotropic glutamate receptor AMPA 1 (GluR1o) B 5.35 pEC50 4500 nM EC50 J. Med. Chem. (2003) 46: 1350-1358 [PMID:12672235]
GluA1/Glutamate receptor ionotropic, AMPA 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3753] [GtoPdb: 444] [UniProtKB: P19490]
ChEMBL Displacement of [3H]AMPA from rat recombinant GluR1 flop isoform expressed in baculovirus infected Sf9 cells B 2.36 pKi 2.36 nM pKi J. Med. Chem. (2009) 52: 4911-4922 [PMID:19588945]
ChEMBL Displacement of [3H]AMPA from rat recombinant GluR1 flop isoform expressed in baculovirus infected Sf9 cells B 6.63 pKi 232 nM Ki J. Med. Chem. (2009) 52: 4911-4922 [PMID:19588945]
ChEMBL Agonist activity at rat recombinant GluR1 flip isoform expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo-4/AM assay F 4.49 pEC50 32000 nM EC50 J. Med. Chem. (2009) 52: 4911-4922 [PMID:19588945]
ChEMBL Agonist activity at ConA-treated rat GluR1 flip isoform expressed in Xenopus laevis oocytes assessed as glutamic acid-induced maximal current by two-electrode voltage clamp method F 5.35 pEC50 4500 nM EC50 J. Med. Chem. (2009) 52: 4911-4922 [PMID:19588945]
GluA2/Glutamate receptor ionotropic, AMPA 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3503] [GtoPdb: 445] [UniProtKB: P19491]
ChEMBL Displacement of [3H]AMPA from rat recombinant GluR2(R) RNA-edited flop isoform expressed in baculovirus infected Sf9 cells B 2.24 pKi 2.24 nM pKi J. Med. Chem. (2009) 52: 4911-4922 [PMID:19588945]
ChEMBL Displacement of [3H]AMPA from rat recombinant GluR2(R) RNA-edited flop isoform expressed in baculovirus infected Sf9 cells B 6.76 pKi 175 nM Ki J. Med. Chem. (2009) 52: 4911-4922 [PMID:19588945]
ChEMBL Agonist activity at rat recombinant GluR2(Q) RNA-edited isoform expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo-4/AM assay F 4.04 pEC50 92000 nM EC50 J. Med. Chem. (2009) 52: 4911-4922 [PMID:19588945]
GluA3/Glutamate receptor ionotropic, AMPA 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3595] [GtoPdb: 446] [UniProtKB: P42263]
ChEMBL Electrophysiological data on Xenopus oocytes, expressing homomeric Ionotropic glutamate receptor AMPA 3 (GluR3o) B 5.14 pEC50 7200 nM EC50 J. Med. Chem. (2003) 46: 1350-1358 [PMID:12672235]
GluA3/Glutamate receptor ionotropic, AMPA 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3504] [GtoPdb: 446] [UniProtKB: P19492]
ChEMBL Displacement of [3H]AMPA from rat recombinant GluR3 flop isoform expressed in baculovirus infected Sf9 cells B 2.23 pKi 2.23 nM pKi J. Med. Chem. (2009) 52: 4911-4922 [PMID:19588945]
ChEMBL Displacement of [3H]AMPA from rat recombinant GluR3 flop isoform expressed in baculovirus infected Sf9 cells B 6.76 pKi 173 nM Ki J. Med. Chem. (2009) 52: 4911-4922 [PMID:19588945]
ChEMBL Agonist activity at rat recombinant GluR3 flip isomer expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo-4/AM assay F 4.89 pEC50 13000 nM EC50 J. Med. Chem. (2009) 52: 4911-4922 [PMID:19588945]
GluA4/Glutamate receptor ionotropic, AMPA 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3190] [GtoPdb: 447] [UniProtKB: P48058]
ChEMBL Electrophysiological data on Xenopus oocytes, expressing homomeric Ionotropic glutamate receptor AMPA 4 (GluR4o) B 4.82 pEC50 15000 nM EC50 J. Med. Chem. (2003) 46: 1350-1358 [PMID:12672235]
GluA4/Glutamate receptor ionotropic, AMPA 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3505] [GtoPdb: 447] [UniProtKB: P19493]
ChEMBL Displacement of [3H]AMPA from rat recombinant GluR4 flop isoform expressed in baculovirus infected Sf9 cells B 2.29 pKi 2.29 nM pKi J. Med. Chem. (2009) 52: 4911-4922 [PMID:19588945]
ChEMBL Displacement of [3H]AMPA from rat recombinant GluR4 flop isoform expressed in baculovirus infected Sf9 cells B 6.69 pKi 202 nM Ki J. Med. Chem. (2009) 52: 4911-4922 [PMID:19588945]
ChEMBL Agonist activity at rat recombinant GluR4 flip isomer expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo-4/AM assay F 5.17 pEC50 6700 nM EC50 J. Med. Chem. (2009) 52: 4911-4922 [PMID:19588945]
GluK1/GluK2/GluK3/GluK4/GluK5/Glutamate receptor ionotropic, kainate in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094119] [GtoPdb: 450451452453454] [UniProtKB: P22756P42260P42264Q01812Q63273]
ChEMBL Ability to displace [3H]-kainic acid radioligand at kainate receptor in rat cortical membranes B 5.8 pIC50 1600 nM IC50 J. Med. Chem. (2003) 46: 1350-1358 [PMID:12672235]
GluK1/Glutamate receptor ionotropic kainate 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2919] [GtoPdb: 450] [UniProtKB: P22756]
ChEMBL Displacement of [3H]SYM from rat recombinant GluR5(Q) RNA-edited isoform expressed in baculovirus infected Sf9 cells B 0.4 pKi 0.4 nM pKi J. Med. Chem. (2009) 52: 4911-4922 [PMID:19588945]
ChEMBL Displacement of [3H]SYM from rat recombinant GluR5(Q) RNA-edited isoform expressed in baculovirus infected Sf9 cells B 8.59 pKi 2.57 nM Ki J. Med. Chem. (2009) 52: 4911-4922 [PMID:19588945]
ChEMBL Agonist activity at rat recombinant GluR5(Q) RNA-edited isoform expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo-4/AM assay F 6.24 pEC50 580 nM EC50 J. Med. Chem. (2009) 52: 4911-4922 [PMID:19588945]
ChEMBL Agonist activity at ConA-treated rat GluR5(Q) RNA-edited isoform expressed in Xenopus laevis oocytes assessed as glutamic acid-induced maximal current by two-electrode voltage clamp method F 6.89 pEC50 130 nM EC50 J. Med. Chem. (2009) 52: 4911-4922 [PMID:19588945]
Glutamate receptor ionotropic kainate 2 in Xenopus laevis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3395] [UniProtKB: B9V8S1]
ChEMBL Electrophysiological data on Xenopus oocytes, expressing heteromeric Ionotropic glutamate receptor ionotropic kainate 2 B 5.19 pEC50 6400 nM EC50 J. Med. Chem. (2003) 46: 1350-1358 [PMID:12672235]
GluK2/Glutamate receptor ionotropic kainate 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3607] [GtoPdb: 451] [UniProtKB: P42260]
ChEMBL Displacement of [3H]KA from rat recombinant GluR6(VCR) RNA-edited isoform expressed in baculovirus infected Sf9 cells B 4 pKi >100000 nM Ki J. Med. Chem. (2009) 52: 4911-4922 [PMID:19588945]
GluK3/Glutamate receptor ionotropic kainate 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3744] [GtoPdb: 452] [UniProtKB: P42264]
ChEMBL Displacement of [3H]SYM from rat recombinant GluR7A expressed in baculovirus infected Sf9 cells B 2.25 pKi 2.25 nM pKi J. Med. Chem. (2009) 52: 4911-4922 [PMID:19588945]
ChEMBL Displacement of [3H]SYM from rat recombinant GluR7A expressed in baculovirus infected Sf9 cells B 6.7 pKi 199 nM Ki J. Med. Chem. (2009) 52: 4911-4922 [PMID:19588945]
GluK5/Glutamate receptor ionotropic kainate 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2675] [GtoPdb: 454] [UniProtKB: Q16478]
ChEMBL Electrophysiological data on Xenopus oocytes, expressing homomeric Ionotropic glutamate receptor ionotropic kainate 1 (GluR5) B 6.89 pEC50 130 nM EC50 J. Med. Chem. (2003) 46: 1350-1358 [PMID:12672235]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]