ADL5859 [Ligand Id: 9004] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL494480 (Adl-5859)
  • δ receptor/Delta-type opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
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  • MRGPRX2/Mas-related G-protein coupled receptor member X2 in Human [ChEMBL: CHEMBL5849] [GtoPdb: 157] [UniProtKB: Q96LB1]
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  • Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
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  • κ receptor in Human [GtoPdb: 318] [UniProtKB: P41145]
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  • μ receptor in Human [GtoPdb: 319] [UniProtKB: P35372]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
δ receptor/Delta-type opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
ChEMBL Displacement of [3H]diprenorphine from human delta opioid receptor in CHO cells B 9.08 pKi 0.84 nM Ki J Med Chem (2008) 51: 5893-5896 [PMID:18788723]
GtoPdb - - 9.08 pKi 0.84 nM Ki J Med Chem (2008) 51: 5893-6 [PMID:18788723]
ChEMBL Agonist activity at human delta opioid receptor in CHO cells assessed as stimulation of [35S]GTPgammaS binding F 7.7 pEC50 20 nM EC50 J Med Chem (2008) 51: 5893-5896 [PMID:18788723]
MRGPRX2/Mas-related G-protein coupled receptor member X2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5849] [GtoPdb: 157] [UniProtKB: Q96LB1]
ChEMBL Agonist activity at MRGPRX2 (unknown origin) expressed in HTLA cells assessed as induction of beta-arrestin 2 recruitment incubated for 18 to 24 hrs by PRESTO-Tango assay F 5.29 pEC50 5128.61 nM EC50 Nat Chem Biol (2017) 13: 529-536 [PMID:28288109]
Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG channel in HEK293 cells by voltage-clamp method B 4.11 pIC50 78000 nM IC50 J Med Chem (2008) 51: 5893-5896 [PMID:18788723]
κ receptor in Human [GtoPdb: 318] [UniProtKB: P41145]
GtoPdb - - 7.43 pKi 37 nM Ki J Med Chem (2008) 51: 5893-6 [PMID:18788723]
μ receptor in Human [GtoPdb: 319] [UniProtKB: P35372]
GtoPdb - - 7.49 pKi 32 nM Ki J Med Chem (2008) 51: 5893-6 [PMID:18788723]

ChEMBL data shown on this page come from version 36:

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]