LY233053 [Ligand Id: 4243] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL173031 (LY-233053, LY-235723)
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GluN2D/GluN3B/GluN1/GluN2A/GluN2B/GluN2C/GluN3A/Glutamate [NMDA] receptor in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094124] [GtoPdb: 459461455456457458460] [UniProtKB: O15399O60391Q05586Q12879Q13224Q14957Q8TCU5]
ChEMBL Tested in vitro for the affinity against NMDA receptor in a cortical wedge assay B 5.38 pIC50 4200 nM IC50 Bioorg. Med. Chem. Lett. (1993) 3: 43-48
ChEMBL Tested in vitro for the affinity against NMDA receptor by examining its ability to inhibit [3H]-CGS-19,755 binding B 6.97 pIC50 107 nM IC50 Bioorg. Med. Chem. Lett. (1993) 3: 43-48
GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A/Glutamate NMDA receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907608] [GtoPdb: 455456457458459461460] [UniProtKB: P35439Q00959Q00960Q00961Q62645Q8VHN2Q9R1M7]
ChEMBL Compound was tested for the antagonistic activity against depolarizations due to NMDA using rat cortical slice preparation F 4.38 pIC50 42000 nM IC50 J. Med. Chem. (1992) 35: 3111-3115 [PMID:1387167]
ChEMBL Compound was tested for the antagonistic activity against depolarizations due to NMDA using rat cortical slice preparation F 4.41 pIC50 39100 nM IC50 J. Med. Chem. (1992) 35: 3111-3115 [PMID:1387167]
ChEMBL Compound was evaluated in vitro in a cortical-wedge preparation for the antagonism of N-methyl-D-aspartate-induced responses F 5.38 pIC50 4200 nM IC50 J. Med. Chem. (1991) 34: 90-97 [PMID:1825117]
ChEMBL Compound was tested in vitro for its ability to inhibit depolarizations induced by 40 uM NMDA in a cortical slice (NMDA antagonist) F 5.38 pIC50 4200 nM IC50 Bioorg. Med. Chem. Lett. (1998) 8: 389-394 [PMID:9871691]
ChEMBL Ability to inhibit [3H]-CGS- 19755 binding to NMDA receptor B 5.62 pIC50 2393 nM IC50 J. Med. Chem. (1992) 35: 3111-3115 [PMID:1387167]
ChEMBL Compound was tested for the antagonistic activity against depolarizations due to NMDA using rat cortical slice preparation F 5.72 pIC50 1900 nM IC50 J. Med. Chem. (1992) 35: 3111-3115 [PMID:1387167]
ChEMBL Ability to inhibit [3H]-CGS- 19755 binding to NMDA receptor B 6.97 pIC50 107 nM IC50 J. Med. Chem. (1992) 35: 3111-3115 [PMID:1387167]
ChEMBL In vitro binding affinity against N-methyl-D-aspartate glutamate receptor using [3H]CGS-19,755 ligand B 6.97 pIC50 107 nM IC50 J. Med. Chem. (1991) 34: 90-97 [PMID:1825117]
ChEMBL In vitro compound's ability to displace [3H]-CGS-19,755 binding as a measure of its affinity for the glutamate recognition site on the NMDA receptor complex. B 6.97 pIC50 107 nM IC50 J. Med. Chem. (1992) 35: 3547-3560 [PMID:1404235]
ChEMBL Ability to inhibit [3H]-CGS- 19755 binding to NMDA receptor B 7.17 pIC50 67 nM IC50 J. Med. Chem. (1992) 35: 3111-3115 [PMID:1387167]
ChEMBL Compound was tested in vitro for inhibition of binding of [3H]-CGS- 19755 radioligand to NMDA receptor in rat brain membranes B 7.77 pIC50 17 nM IC50 Bioorg. Med. Chem. Lett. (1998) 8: 389-394 [PMID:9871691]

ChEMBL data shown on this page come from version 26:

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]