dronedarone [Ligand Id: 7465] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL184412 (Dronedarone, SR-33589, SR33589) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibitory concentration against IKr potassium channel | B | 5.52 | pIC50 | 3000 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 4771-4777 [PMID:15324906] |
| ChEMBL | Inhibition of human ERG | B | 6.5 | pIC50 | 316.23 | nM | IC50 | Eur J Med Chem (2011) 46: 618-630 [PMID:21185626] |
| NLRP3/NACHT, LRR and PYD domains-containing protein 3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3779755] [GtoPdb: 1770] [UniProtKB: Q8R4B8] | ||||||||
| ChEMBL | Inhibition of NLRP3 inflammasome in LPS-primed mouse J774.A1 cells assessed as reduction in IL-1beta secretion preincubated with compound for 1 hr followed by nigericin stimulation for 1 hr by ELISA | B | 5.16 | pIC50 | 6840 | nM | IC50 | Bioorg Med Chem Lett (2021) 46: 128160-128160 [PMID:34062252] |
| Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366456] [UniProtKB: O35505] | ||||||||
| ChEMBL | Inhibition of Cav1.2 calcium current measured using whole cell patch clamp in guinea pig ventricular myocytes | F | 6.4 | pIC50 | 400 | nM | IC50 | IC50 data for the L-type calcium channel extracted from a set of literature articles |
| Kv1.5 in Human [GtoPdb: 542] [UniProtKB: P22460] | ||||||||
| GtoPdb | Whole cell patch clamp experiment using HEK293 cells expressing human Kv1.5. | - | 5.63 | pIC50 | 2370 | nM | IC50 | Eur J Med Chem (2014) 81: 89-94 [PMID:24824064] |
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]
