(S)-4-AHCP [Ligand Id: 4069] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL28472 |
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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: 455, 456, 457, 458, 459, 461, 460] [UniProtKB: P35439, Q00959, Q00960, Q00961, Q62645, Q8VHN2, Q9R1M7] | ||||||||
| 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: 444, 445, 446, 447] [UniProtKB: P19490, P19491, P19492, P19493] | ||||||||
| 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: 450, 451, 452, 453, 454] [UniProtKB: P22756, P42260, P42264, Q01812, Q63273] | ||||||||
| 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 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]
