BPAM344 [Ligand Id: 13392] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2441067 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| GluA1/GluA2/GluA3/GluA4/Glutamate receptor ionotropic AMPA in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2096670] [GtoPdb: 444, 445, 446, 447] [UniProtKB: P42261, P42262, P42263, P48058] | ||||||||
| ChEMBL | Positive allosteric modulation at AMPAR in HEK293 cells expressing GluA2Q assessed as glutamate induced calcium influx | B | 6.56 | pEC50 | 275.42 | nM | EC50 | Eur J Med Chem (2023) 250: 115221-115221 [PMID:36863228] |
| GluA2/Glutamate receptor ionotropic, AMPA 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4016] [GtoPdb: 445] [UniProtKB: P42262] | ||||||||
| ChEMBL | Binding affinity to GluA2-LBD-L483Y-N754S complex (unknown origin) by isothermal titration calorimetry | B | 6.46 | pKd | 350 | nM | Kd | J Med Chem (2014) 57: 9539-9553 [PMID:25375781] |
| ChEMBL | Positive allosteric modulation of GluA2 (Q) flop isoform (unknown origin) expressed in HEK293 cells assessed as potentiation of glutamate-evoked calcium flux by fluo-4/AM dye-based fluorescence assay | B | 6.09 | pEC50 | 812.83 | nM | EC50 | J Med Chem (2018) 61: 251-264 [PMID:29256599] |
| ChEMBL | Positive allosteric modulation of GluA2 (Q) flop isoform (unknown origin) expressed in HEK293 cells assessed as potentiation of glutamate-evoked calcium flux by fluo-4/AM dye-based fluorescence assay | B | 6.09 | pEC50 | 810 | nM | EC50 | J Med Chem (2018) 61: 251-264 [PMID:29256599] |
| GluA2/Glutamate receptor ionotropic, AMPA 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3503] [GtoPdb: 445] [UniProtKB: P19491] | ||||||||
| ChEMBL | Positive allosteric modulation of GluA2 receptor in rat embryonic cortex neuron assessed as increase of AMPA-induced membrane depolarization by fluorescence assay | B | 6.05 | pEC50 | 900 | nM | EC50 | J Med Chem (2013) 56: 8736-8745 [PMID:24131202] |
| GluK2 in Human [GtoPdb: 451] [UniProtKB: Q13002] | ||||||||
| GtoPdb | - | - | 4.1 | pEC50 | 79000 | nM | EC50 | Mol Pharmacol (2017) 91: 576-585 [PMID:28360094] |
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]
