ChEMBL ligand: CHEMBL435582
GluA1/Glutamate receptor ionotropic, AMPA 1 in Human [ChEMBL: CHEMBL2009] [GtoPdb: 444] [UniProtKB: P42261] There should be some charts here, you may need to enable JavaScript!
GluA2/Glutamate receptor ionotropic, AMPA 2 in Human [ChEMBL: CHEMBL4016] [GtoPdb: 445] [UniProtKB: P42262] There should be some charts here, you may need to enable JavaScript!
GluA3/Glutamate receptor ionotropic, AMPA 3 in Human [ChEMBL: CHEMBL3595] [GtoPdb: 446] [UniProtKB: P42263] There should be some charts here, you may need to enable JavaScript!
GluA4/Glutamate receptor ionotropic, AMPA 4 in Human [ChEMBL: CHEMBL3190] [GtoPdb: 447] [UniProtKB: P48058] There should be some charts here, you may need to enable JavaScript!

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	Inhibition of GluR1 expressed in HEK cells	B	5.25	pEC50	5650	nM	EC50	J Med Chem (2010) 53: 7271-7279 [PMID:20839777]
GtoPdb	-	-	5.25	pEC50	5650	nM	EC50	Neuropharmacology (2001) 40: 976-83 [PMID:11406188]
GluA2/Glutamate receptor ionotropic, AMPA 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4016] [GtoPdb: 445] [UniProtKB: P42262]
ChEMBL	Activity against human GLUR2 flop expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay	F	5.72	pEC50	1905	nM	EC50	Bioorg Med Chem Lett (2006) 16: 5057-5061 [PMID:16879964]
ChEMBL	Inhibition of GluR2 flop expressed in HEK cells	B	5.84	pEC50	1440	nM	EC50	J Med Chem (2010) 53: 7271-7279 [PMID:20839777]
ChEMBL	Activity against human GLUR2 flip expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay	F	6.25	pEC50	559	nM	EC50	Bioorg Med Chem Lett (2006) 16: 5057-5061 [PMID:16879964]
GtoPdb	-	-	6.82	pEC50	150	nM	EC50	Neuropharmacology (2001) 40: 976-83 [PMID:11406188]
ChEMBL	Agonist activity at GluR2 receptor	F	6.82	pEC50	150	nM	EC50	J Med Chem (2010) 53: 7271-7279 [PMID:20839777]
GluA3/Glutamate receptor ionotropic, AMPA 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3595] [GtoPdb: 446] [UniProtKB: P42263]
ChEMBL	Inhibition of GluR3 expressed in HEK cells	B	5.78	pEC50	1660	nM	EC50	J Med Chem (2010) 53: 7271-7279 [PMID:20839777]
GtoPdb	-	-	5.78	pEC50	1660	nM	EC50	Neuropharmacology (2001) 40: 976-83 [PMID:11406188]
GluA4/Glutamate receptor ionotropic, AMPA 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3190] [GtoPdb: 447] [UniProtKB: P48058]
ChEMBL	Activity against human GLUR4 flop expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay	F	5.97	pEC50	1061	nM	EC50	Bioorg Med Chem Lett (2006) 16: 5057-5061 [PMID:16879964]
ChEMBL	Activity against human GLUR4 flip expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay	F	6.38	pEC50	420	nM	EC50	Bioorg Med Chem Lett (2006) 16: 5057-5061 [PMID:16879964]
ChEMBL	Tested for potentiation towards human iGluR4 receptor expressed in HEK293 cells	F	6.54	pEC50	290	nM	EC50	J Med Chem (2000) 43: 4354-4358 [PMID:11087558]
ChEMBL	Potentiation of responses mediated by 100 uM L-glutamate in transfected HEK293 cells expressing human homomeric iGluR4 flip receptors.	F	6.54	pEC50	290	nM	EC50	J Med Chem (2002) 45: 2101-2111 [PMID:11985477]
ChEMBL	Inhibition of GluR4 expressed in HEK293 cells	B	6.54	pEC50	290	nM	EC50	J Med Chem (2010) 53: 7271-7279 [PMID:20839777]
GtoPdb	-	-	6.68	pEC50	210	nM	EC50	Neuropharmacology (2001) 40: 976-83 [PMID:11406188]

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]