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| ChEMBL ligand: CHEMBL485 (Codeine, Codeine monohydrate, Codeinum, Codeinum monohydricum, Dea no. 9050, IDS-NC-005(SECT.-2)) |
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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]