MES304 [Ligand Id: 13945] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3361433
  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
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  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
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  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
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  • NPFF1 receptor/Neuropeptide FF receptor 1 in Human [ChEMBL: CHEMBL5951] [GtoPdb: 300] [UniProtKB: Q9GZQ6]
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  • NPFF2 receptor/Neuropeptide FF receptor 2 in Human [ChEMBL: CHEMBL5952] [GtoPdb: 301] [UniProtKB: Q9Y5X5]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
ChEMBL Displacement of [3H]DPDPE from human DOR expressed in HEK293 cells after 60 mins by scintillation counting analysis B 5.58 pKi 2607 nM Ki J Med Chem (2014) 57: 8903-8927 [PMID:25268943]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL Displacement of [3H]U-69593 from human KOR expressed in HEK293 cells after 60 mins by scintillation counting analysis B 5.83 pKi 1470 nM Ki J Med Chem (2014) 57: 8903-8927 [PMID:25268943]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL Displacement of [3H]DAMGO from human MOR expressed in HEK293 cells after 60 mins by scintillation counting analysis B 5.3 pKi >5000 nM Ki J Med Chem (2014) 57: 8903-8927 [PMID:25268943]
NPFF1 receptor/Neuropeptide FF receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5951] [GtoPdb: 300] [UniProtKB: Q9GZQ6]
GtoPdb - - 6.95 pKi 112 nM Ki J Med Chem (2014) 57: 8903-27 [PMID:25268943];
Eur J Med Chem (2024) 269: 116330 [PMID:38522114]
ChEMBL Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis B 6.95 pKi 112 nM Ki J Med Chem (2014) 57: 8903-8927 [PMID:25268943]
ChEMBL Antagonist activity at human NPFF1 receptor expressed in CHO cells assessed as reversal of NPVF-induced inhibition of intracellular cAMP accumulation after 10 mins by liquid scintillation counting analysis relative to control F 5.59 pEC50 2600 nM EC50 J Med Chem (2014) 57: 8903-8927 [PMID:25268943]
NPFF2 receptor/Neuropeptide FF receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5952] [GtoPdb: 301] [UniProtKB: Q9Y5X5]
GtoPdb - - 7.52 pKi 30 nM Ki J Med Chem (2014) 57: 8903-27 [PMID:25268943];
Eur J Med Chem (2024) 269: 116330 [PMID:38522114]
ChEMBL Displacement of [3H]EYF from human NPFF2 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis B 7.52 pKi 30 nM Ki J Med Chem (2014) 57: 8903-8927 [PMID:25268943]
ChEMBL Antagonist activity at human NPFF2 receptor expressed in CHO cells assessed as reversal of 1DMe-induced inhibition of intracellular cAMP accumulation after 10 mins by liquid scintillation counting analysis relative to control F 6.19 pEC50 645 nM EC50 J Med Chem (2014) 57: 8903-8927 [PMID:25268943]

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]