codeine [Ligand Id: 1673] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL485 (Codeine, Codeine monohydrate, Codeinum, Codeinum monohydricum, Dea no. 9050, IDS-NC-005(SECT.-2))
  • δ receptor/Delta-type opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
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  • κ receptor/Kappa-type opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
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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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  • μ receptor/Mu-type opioid receptor in Human [ChEMBL: CHEMBL233] [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 recombinant delta opioid receptor expressed in C6 cells B 4.28 pKi 52207 nM Ki J Med Chem (2008) 51: 2316-2320 [PMID:18311899]
ChEMBL In vitro binding affinity against cloned human Opioid receptor delta 1 expressed in HEK 293S cells B 5.03 pIC50 >9300 nM IC50 J Med Chem (2003) 46: 34-48 [PMID:12502358]
κ receptor/Kappa-type opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL Displacement of [3H]diprenorphine from recombinant kappa opioid receptor expressed in CHO cells B 4.59 pKi 25411 nM Ki J Med Chem (2008) 51: 2316-2320 [PMID:18311899]
ChEMBL In vitro binding affinity against cloned human Opioid receptor kappa 1 expressed in HEK 293S cells B 4.82 pIC50 15000 nM IC50 J Med Chem (2003) 46: 34-48 [PMID:12502358]
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 N-terminal Flag-tagged human MRGPRX2 receptor expressed in tetracycline-induced FLP-IN/T-REX 293 cells assessed as increase in intracellular calcium release by FLIPR assay F 5 pEC50 10000 nM EC50 Nat Chem Biol (2017) 13: 529-536 [PMID:28288109]
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 5.17 pEC50 6760.83 nM EC50 Nat Chem Biol (2017) 13: 529-536 [PMID:28288109]
μ receptor/Mu-type opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL Displacement of [3H]naloxone from human mu poioid receptor expressed in HEK293 cells B 5.2 pKi 6300 nM Ki J Biol Chem (2007) 282: 27126-27132 [PMID:17616524]
ChEMBL Displacement of [3H]diprenorphine from recombinant mu opioid receptor expressed in C6 cells B 6.14 pKi 727 nM Ki J Med Chem (2008) 51: 2316-2320 [PMID:18311899]
GtoPdb - - 6.9 pKi - - - NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407]
ChEMBL In vitro binding affinity against cloned human Opioid receptor mu 1 expressed in HEK 293S cells B 6.98 pIC50 105 nM IC50 J Med Chem (2003) 46: 34-48 [PMID:12502358]
ChEMBL Activation of human mu opioid receptor expressed in HEK293a cells co-expressing YFP-labelled alphai1 and CFP-labelled beta1gamma2 Gi subunits assessed as Gi protein activation by fluorescence resonance energy transfer B 5.21 pEC50 6100 nM EC50 J Biol Chem (2007) 282: 27126-27132 [PMID:17616524]

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]