Honokiol [Ligand Id: 11610] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL16901 (Honokiol) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 5-LOX/Arachidonate 5-lipoxygenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL215] [GtoPdb: 1385] [UniProtKB: P09917] | ||||||||
| ChEMBL | Inhibition of 5LOX-mediated LTB4 formation in stimulated human polymorphonuclear leukocytes | B | 5.38 | pIC50 | 4200 | nM | IC50 | Bioorg Med Chem (2009) 17: 4459-4465 [PMID:19481465] |
| GtoPdb | Inhibition of 5LOX-mediated LTB4 formation in stimulated human polymorphonuclear leukocytes. | - | 5.38 | pIC50 | 4200 | nM | IC50 | Bioorg Med Chem (2009) 17: 4459-65 [PMID:19481465] |
| CB1 receptor/Cannabinoid CB1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554] | ||||||||
| ChEMBL | Displacement of [3H]CP55,940 from recombinant human CB1 receptor expressed in CHO cells after 2 hrs by liquid scintillation counting | B | 5.19 | pKi | 6460 | nM | Ki | ACS Med Chem Lett (2013) 4: 41-45 [PMID:24900561] |
| ChEMBL | Displacement of [3H]CP55940 from human CB1 receptor expressed in CHO cell membranes after 2 hrs | B | 8.19 | pKi | 6.46 | nM | Ki | Eur J Med Chem (2016) 116: 252-266 [PMID:27078864] |
| ChEMBL | Agonist activity at recombinant human CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 5 mins by cAMP-competition binding assay | F | 5 | pEC50 | >10000 | nM | EC50 | ACS Med Chem Lett (2013) 4: 41-45 [PMID:24900561] |
| CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972] | ||||||||
| ChEMBL | Displacement of [3H]CP55,940 from recombinant human CB2 receptor expressed in CHO cells after 2 hrs by liquid scintillation counting | B | 5.25 | pKi | 5610 | nM | Ki | ACS Med Chem Lett (2013) 4: 41-45 [PMID:24900561] |
| ChEMBL | Displacement of [3H]CP55940 from human CB2 receptor expressed in CHO cell membranes after 2 hrs | B | 8.25 | pKi | 5.61 | nM | Ki | Eur J Med Chem (2016) 116: 252-266 [PMID:27078864] |
| Cyclooxygenase-1 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2949] [UniProtKB: P05979] | ||||||||
| ChEMBL | Inhibition of COX1 in ram seminal vesicle by enzyme immunoassay | B | 5.74 | pIC50 | 1800 | nM | IC50 | Bioorg Med Chem (2009) 17: 4459-4465 [PMID:19481465] |
| Cyclooxygenase-2 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4102] [UniProtKB: P79208] | ||||||||
| ChEMBL | Inhibition of COX2 in sheep placental vesicle by enzyme immunoassay | B | 5.68 | pIC50 | 2100 | nM | IC50 | Bioorg Med Chem (2009) 17: 4459-4465 [PMID:19481465] |
| GABAA receptor α1 subunit/GABAA receptor γ2 subunit/GABAA receptor β2 subunit/GABA-A receptor; alpha-1/beta-2/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095172] [GtoPdb: 404, 414, 411] [UniProtKB: P14867, P18507, P47870] | ||||||||
| ChEMBL | Partial agonist activity at GABAAalpha1beta2gamma2s receptor (unknown origin) expressed in Xenopus laevis oocytes assessed as induction of chloride current by two-microelectrode voltage-clamp method | B | 4.12 | pEC50 | 76200 | nM | EC50 | Bioorg Med Chem (2015) 23: 6757-6762 [PMID:26410663] |
| GABAA receptor α1 subunit/GABAA receptor β3 subunit/GABA-A receptor alpha-1/beta-3 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4106151] [GtoPdb: 404, 412] [UniProtKB: P14867, P28472] | ||||||||
| ChEMBL | Modulation of GABA Aalpha1beta3 receptor expressed in Xenopus laevis oocytes assessed as potentiation of GABA-induced chloride current at holding potential -70 mV by two-microelectrode voltage clamp technique | B | 4.22 | pEC50 | 59600 | nM | EC50 | J Med Chem (2011) 54: 5349-5361 [PMID:21699169] |
| GABAA receptor α1 subunit/GABAA receptor β2 subunit/GABA-A receptor; GABA-A site (alpha1/beta2 interface) in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907597] [GtoPdb: 404, 411] [UniProtKB: P14867, P47870] | ||||||||
| ChEMBL | Modulation of GABA Aalpha1beta2 receptor expressed in Xenopus laevis oocytes assessed as potentiation of GABA-induced chloride current at holding potential -70 mV by two-microelectrode voltage clamp technique | B | 4.41 | pEC50 | 39300 | nM | EC50 | J Med Chem (2011) 54: 5349-5361 [PMID:21699169] |
| GABAA receptor α1 subunit/GABAA receptor β1 subunit/Gamma-aminobutyric acid receptor subunit alpha-1/ beta-1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3885570] [GtoPdb: 404, 410] [UniProtKB: P14867, P18505] | ||||||||
| ChEMBL | Modulation of GABA Aalpha1beta1 receptor expressed in Xenopus laevis oocytes assessed as potentiation of GABA-induced chloride current at holding potential -70 mV by two-microelectrode voltage clamp technique | B | 4.24 | pEC50 | 57000 | nM | EC50 | J Med Chem (2011) 54: 5349-5361 [PMID:21699169] |
| GABAA receptor α2 subunit/GABAA receptor β2 subunit/Gamma-aminobutyric acid receptor subunit alpha-2/beta-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3885571] [GtoPdb: 405, 411] [UniProtKB: P47869, P47870] | ||||||||
| ChEMBL | Modulation of GABA Aalpha2beta2 receptor expressed in Xenopus laevis oocytes assessed as potentiation of GABA-induced chloride current at holding potential -70 mV by two-microelectrode voltage clamp technique | B | 4.33 | pEC50 | 46400 | nM | EC50 | J Med Chem (2011) 54: 5349-5361 [PMID:21699169] |
| GABAA receptor α3 subunit/GABAA receptor β2 subunit/Gamma-aminobutyric acid receptor subunit alpha-3/ beta-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3885572] [GtoPdb: 406, 411] [UniProtKB: P34903, P47870] | ||||||||
| ChEMBL | Modulation of GABA Aalpha3beta2 receptor expressed in Xenopus laevis oocytes assessed as potentiation of GABA-induced chloride current at holding potential -70 mV by two-microelectrode voltage clamp technique | B | 4.28 | pEC50 | 52400 | nM | EC50 | J Med Chem (2011) 54: 5349-5361 [PMID:21699169] |
| GABAA receptor α5 subunit/GABAA receptor β2 subunit/Gamma-aminobutyric acid receptor subunit alpha-5/beta-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3885576] [GtoPdb: 408, 411] [UniProtKB: P31644, P47870] | ||||||||
| ChEMBL | Modulation of GABA Aalpha5beta2 receptor expressed in Xenopus laevis oocytes assessed as potentiation of GABA-induced chloride current at holding potential -70 mV by two-microelectrode voltage clamp technique | B | 4.63 | pEC50 | 23400 | nM | EC50 | J Med Chem (2011) 54: 5349-5361 [PMID:21699169] |
| sirtuin 3/NAD-dependent deacetylase sirtuin 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4461] [GtoPdb: 2709] [UniProtKB: Q9NTG7] | ||||||||
| ChEMBL | Activation of recombinant human SIRT3 assessed as lysyl deacetylase activity using (Gln-Pro-Lys-Lys(Ac)) peptide substrate by fluorescent assay | B | 6.77 | pEC50 | 170 | nM | EC50 | J Med Chem (2021) 64: 14192-14216 [PMID:34605238] |
| Neuraminidase in Influenza A virus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6135] [UniProtKB: B4URF0] | ||||||||
| ChEMBL | Inhibition of Influenza A virus (A/Puerto Rico/8/1934(H1N1)) neuraminidase by chemiluminescence based assay | B | 4.52 | pIC50 | 30100 | nM | IC50 | J Nat Prod (2014) 77: 563-570 [PMID:24313801] |
| ChEMBL | Inhibition of oseltamivir-resistant Influenza A virus H1N1 B/55/08 neuraminidase by chemiluminescence based assay | B | 5.86 | pIC50 | 1390 | nM | IC50 | J Nat Prod (2014) 77: 563-570 [PMID:24313801] |
| Retinoid X receptor-α/Retinoid X receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2061] [GtoPdb: 610] [UniProtKB: P19793] | ||||||||
| ChEMBL | Agonist activity at RXRalpha in HEK293 cells assessed as transcriptional activation after 48 hrs by luciferase reporter gene assay | F | 4.93 | pEC50 | 11800 | nM | EC50 | J Nat Prod (2010) 73: 1332-1336 [PMID:20695472] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
