comp-43 [Ligand Id: 13995] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4782344
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  • GPR52/Probable G-protein coupled receptor 52 in Human [ChEMBL: CHEMBL3297639] [GtoPdb: 108] [UniProtKB: Q9Y2T5]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GPR52 in Human [GtoPdb: 108] [UniProtKB: Q9Y2T5]
GtoPdb - - 6.2 pIC50 630 nM IC50 J Med Chem (2021) 64: 941-957 [PMID:33185430]
GPR52/G-protein coupled receptor 52 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105791] [GtoPdb: 108] [UniProtKB: P0C5J4]
ChEMBL In-vivo antagonist activity at GPR52 in HdhQ140 mouse model with GPR52 knockdown assessed as decrease in mHTT levels F 6.2 pIC50 630 nM IC50 J Med Chem (2021) 64: 938-940 [PMID:33443413]
GPR52/Probable G-protein coupled receptor 52 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3297639] [GtoPdb: 108] [UniProtKB: Q9Y2T5]
ChEMBL Antagonist activity at GPR52 (unknown origin) expressed in HEK293 cells assessed as inhibition of WO459-induced cAMP accumulation preincubated for 15 mins followed by WO459 addition and measured after 30 mins by LANCE Ultra cAMP kit based microplate reader analysis F 6.06 pIC50 880 nM IC50 J Med Chem (2021) 64: 941-957 [PMID:33185430]
GtoPdb - - 6.2 pIC50 630 nM IC50 J Med Chem (2021) 64: 941-957 [PMID:33185430]
ChEMBL Inhibition of GPR52 (unknown origin) B 6.2 pIC50 630 nM IC50 J Med Chem (2022) 65: 15993-16032 [PMID:36490325]

ChEMBL data shown on this page come from version 35:

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]