JNJ-42153605 [Ligand Id: 6317] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2179319 (JNJ-42153605)
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  • mGlu2 receptor/Metabotropic glutamate receptor 2 in Human [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416]
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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
ChEMBL PDSP Secondary Binding target: SLC6A3 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. B 5.37 pKi 4309.23 nM Ki EUbOPEN Chemogenomics Library - PDSP Secondary Binding
mGlu2 receptor/Metabotropic glutamate receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416]
GtoPdb - - 7.82 pKi 15 nM Ki J Med Chem (2012) 55: 8770-89 [PMID:23072213]
ChEMBL Displacement of [3H]8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-phenyl-1-piperidinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine from mGlu2 receptor (unknown origin) B 7.82 pKi 15 nM Ki J Med Chem (2016) 59: 8495-8507 [PMID:27579727]
ChEMBL Binding affinity to human mGlu2R expressed in CHO cells by radioligand binding assay B 7.82 pIC50 15 nM IC50 J Med Chem (2012) 55: 8770-8789 [PMID:23072213]
ChEMBL Positive allosteric modulation at human mGlu2 receptor W773A mutant expressed in CHO-K1 cells assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins by scintillation counting method B 5 pEC50 >10000 nM EC50 J Med Chem (2016) 59: 8495-8507 [PMID:27579727]
ChEMBL Positive allosteric modulation at human mGlu2 receptor F643A mutant expressed in CHO-K1 cells assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins by scintillation counting method B 6.41 pEC50 385 nM EC50 J Med Chem (2016) 59: 8495-8507 [PMID:27579727]
ChEMBL Agonist activity at human mGlu2R expressed in CHO cells F 6.57 pEC50 270 nM EC50 J Med Chem (2012) 55: 8770-8789 [PMID:23072213]
ChEMBL Positive allosteric modulation of mGlu2 receptor (unknown origin) B 6.83 pEC50 147 nM EC50 Bioorg Med Chem (2022) 56: 116614-116614 [PMID:35033884]
ChEMBL Positive allosteric modulation at wild type human mGlu2 receptor L732A mutant expressed in CHO-K1 cells assessed as potentiation of glutamate-induced effect preincubated for 30 mins prior to glutamate challenge measured after 30 mins by [35S]GTP-gammaS binding assay B 7.33 pEC50 46.4 nM EC50 J Med Chem (2016) 59: 8495-8507 [PMID:27579727]
ChEMBL Positive allosteric modulation at human mGlu2 receptor N735D mutant expressed in CHO-K1 cells assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins by scintillation counting method B 7.57 pEC50 27 nM EC50 J Med Chem (2016) 59: 8495-8507 [PMID:27579727]
ChEMBL Positive allosteric modulation at human mGlu2 receptor F776A mutant expressed in CHO-K1 cells assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins by scintillation counting method B 7.63 pEC50 23.6 nM EC50 J Med Chem (2016) 59: 8495-8507 [PMID:27579727]
ChEMBL Positive allosteric modulation of human mGlu2 receptor expressed in CHO cell membranes assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins by scintillation counting method B 7.77 pEC50 17 nM EC50 J Med Chem (2016) 59: 8495-8507 [PMID:27579727]
ChEMBL Positive allosteric modulator activity at human mGlu2R expressed in CHO cells incubated for 30 mins by [35S]GTPgammaS binding assay F 7.77 pEC50 17 nM EC50 J Med Chem (2012) 55: 8770-8789 [PMID:23072213]
GtoPdb - - 7.77 pEC50 17 nM EC50 J Med Chem (2012) 55: 8770-89 [PMID:23072213]
ChEMBL Positive allosteric modulation of wild-type human mGlu2 receptor expressed in CHO-K1 cells assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins by scintillation counting method B 8.32 pEC50 4.8 nM EC50 J Med Chem (2016) 59: 8495-8507 [PMID:27579727]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL PDSP Secondary Binding target: SIGMAR1 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. B 6.01 pKi 982.65 nM Ki EUbOPEN Chemogenomics Library - PDSP Secondary Binding

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]