(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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
