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| ChEMBL ligand: CHEMBL500830 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| κ receptor/Kappa-type opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
| GtoPdb | - | - | 9.9 | pKi | - | - | - |
NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407]; Binding and activity of opioid ligands at the cloned human delta, mu and kappa receptors.. The Delta Receptor (2003); Proc Natl Acad Sci USA (1995) 92: 7006-10 [PMID:7624359] |
| ChEMBL | Agonist activity at KOR (unknown origin) by Glo sensor assay | F | 9.89 | pEC50 | 0.13 | nM | EC50 | Nat Chem Biol (2017) 13: 529-536 [PMID:28288109] |
| κ receptor in Mouse [GtoPdb: 318] [UniProtKB: P33534] | ||||||||
| GtoPdb | - | - | 10 | pIC50 | - | - | - | Proc Natl Acad Sci USA (1993) 90: 6736-40 [PMID:8393575] |
| κ receptor in Rat [GtoPdb: 318] [UniProtKB: P34975] | ||||||||
| GtoPdb | - | - | 9.5 | pKi | - | - | - | Proc Natl Acad Sci USA (1993) 90: 9954-8 [PMID:8234341] |
| 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 | 4.48 | pEC50 | 33113.11 | nM | EC50 | Nat Chem Biol (2017) 13: 529-536 [PMID:28288109] |
| 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 | 5.08 | pEC50 | 8340 | nM | EC50 | Nat Chem Biol (2017) 13: 529-536 [PMID:28288109] |
| 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 | 5.19 | pEC50 | 6456.54 | nM | EC50 | Nat Chem Biol (2017) 13: 529-536 [PMID:28288109] |
| δ receptor in Human [GtoPdb: 317] [UniProtKB: P41143] | ||||||||
| GtoPdb | - | - | 7.8 | pKi | - | - | - | NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407] |
| μ receptor in Human [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| GtoPdb | - | - | 8.5 | pKi | - | - | - | NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407] |
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]