piperine [Ligand Id: 2489] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL43185 (Bioperine, FEMA NO. 2909, NSC-21727, Piperine) |
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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 human PMNL 5-LOX using arachidonic acid as substrate after 5 mins by HPLC method | B | 4.27 | pIC50 | 54000 | nM | IC50 | Bioorg Med Chem (2019) 27: 3745-3759 [PMID:31331653] |
| cathepsin D/Cathepsin D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2581] [GtoPdb: 2345] [UniProtKB: P07339] | ||||||||
| ChEMBL | Inhibition of cathepsin D (unknown origin) using hemoglobin as substrate after 30 min by spectrophotometric analysis | B | 4.37 | pIC50 | 42300 | nM | IC50 | Med Chem Res (2013) 22: 3953-3958 |
| 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 | Modulation of GABAA alpha1beta2gamma2S receptor (unknown origin) expressed in Xenopus laevis oocytes assessed as potentiation of GABA-induced chloride ion current at holding potential -70 mV by two-microelectrode voltage clamp assay | B | 4.28 | pEC50 | 52400 | nM | EC50 | J Med Chem (2014) 57: 5602-5619 [PMID:24905252] |
| Monoamine oxidase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1951] [GtoPdb: 2489] [UniProtKB: P21397] | ||||||||
| ChEMBL | Inhibition of MAO-A assessed as inhibition of kyneuramine conversion to 4-hydroxyquinoline after 20 mins by fluorescence assay | B | 4.23 | pIC50 | 58980 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 7183-7188 [PMID:23102654] |
| Monoamine oxidase A in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3681] [GtoPdb: 2489] [UniProtKB: Q64133] | ||||||||
| ChEMBL | Inhibition of mouse brain MAOA | B | 4.72 | pKi | 19000 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 537-540 [PMID:19969454] |
| Monoamine oxidase A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3358] [UniProtKB: P21396] | ||||||||
| ChEMBL | Inhibition of MAOA in rat brain mitochondria | B | 4.31 | pKi | 49300 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 537-540 [PMID:19969454] |
| ChEMBL | Inhibition of MAO-A in Sprague-Dawley rat brain homogenate using kynuramine as substrate preincubated for 10 mins measured by fluorimetric assay | B | 6.39 | pIC50 | 404 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 3343-3348 [PMID:22475561] |
| Monoamine oxidase B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2039] [GtoPdb: 2490] [UniProtKB: P27338] | ||||||||
| ChEMBL | Inhibition of human microsomal MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells assessed as reduction in 4-hydroxyquinoline formation using kynuramine as substrate preincubated with substrate for 10 mins followed by enzyme addition by spectrophotometric analysis | B | 5.98 | pIC50 | 1050 | nM | IC50 | Eur J Med Chem (2020) 185: 111770-111770 [PMID:31711793] |
| ChEMBL | Inhibition of MAO-B assessed as inhibition of kyneuramine conversion to 4-hydroxyquinoline after 20 mins by fluorescence assay | B | 6.32 | pIC50 | 483 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 7183-7188 [PMID:23102654] |
| Monoamine oxidase B in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3050] [GtoPdb: 2490] [UniProtKB: Q8BW75] | ||||||||
| ChEMBL | Inhibition of mouse brain MAOB | B | 5.5 | pKi | 3190 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 537-540 [PMID:19969454] |
| Monoamine oxidase B in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2993] [GtoPdb: 2490] [UniProtKB: P19643] | ||||||||
| ChEMBL | Inhibition of MAOB in rat brain mitochondria | B | 4.04 | pKi | 91300 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 537-540 [PMID:19969454] |
| ChEMBL | Inhibition of MAO-B in Sprague-Dawley rat brain homogenate using kynuramine as substrate preincubated for 10 mins measured by fluorimetric assay | B | 6.59 | pIC50 | 260 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 3343-3348 [PMID:22475561] |
| ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183] | ||||||||
| ChEMBL | TP_TRANSPORTER: inhibition of Cyclosporin A transepithelial transport (basal to apical) (Cyclosporin A: 1 uM) in Caco-2 cells | F | 4.13 | pIC50 | 74100 | nM | IC50 | J Pharmacol Exp Ther (2002) 302: 645-650 [PMID:12130727] |
| ChEMBL | TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells | F | 4.81 | pIC50 | 15500 | nM | IC50 | J Pharmacol Exp Ther (2002) 302: 645-650 [PMID:12130727] |
| TRPV1/Vanilloid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4794] [GtoPdb: 507] [UniProtKB: Q8NER1] | ||||||||
| GtoPdb | - | - | 5 | pEC50 | - | - | - | Br J Pharmacol (2005) 144: 781-90 [PMID:15685214] |
| ChEMBL | Agonist activity at human TRPV1 expressed in tetracycline-stimulated HEK293 cells assessed as increase in intracellular calcium levels by fluorimetric assay | F | 5.5 | pEC50 | 3162.28 | nM | EC50 | Bioorg Med Chem (2010) 18: 3299-3306 [PMID:20381363] |
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]
