diphenoxylate [Ligand Id: 7164] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1201294 (Diphenoxylate, IDS-ND-016)
  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
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  • Kv1.3/Voltage-gated potassium channel subunit Kv1.3 in Human [ChEMBL: CHEMBL4633] [GtoPdb: 540] [UniProtKB: P22001]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL Displacement of [3H]DAMGO from human mu opioid receptor expressed in HEK293 cell membrane incubated for 60 mins by radioligand binding assay B 7.91 pKi 12.37 nM Ki J Med Chem (2021) 64: 7778-7808 [PMID:34011153]
Kv1.3/Voltage-gated potassium channel subunit Kv1.3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4633] [GtoPdb: 540] [UniProtKB: P22001]
ChEMBL Inhibition of Kv1.3 expressed in mouse L929 cells exposed to depolarizing step pulses from -80 mV to +40 mV by whole cell patch clamp method B 5.3 pIC50 5000 nM IC50 Bioorg Med Chem Lett (2012) 22: 7106-7109 [PMID:23084278]

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]