piperine [Ligand Id: 2489] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL43185 (Bioperine, FEMA NO. 2909, NSC-21727, Piperine)
  • 5-LOX/Arachidonate 5-lipoxygenase in Human [ChEMBL: CHEMBL215] [GtoPdb: 1385] [UniProtKB: P09917]
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  • dihydroorotate dehydrogenase (quinone)/Dihydroorotate dehydrogenase in Human [ChEMBL: CHEMBL1966] [GtoPdb: 2604] [UniProtKB: Q02127]
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  • GABAA receptor α1 subunit/GABAA receptor γ2 subunit/GABAA receptor β2 subunit/GABA-A receptor; alpha-1/beta-2/gamma-2 in Human [ChEMBL: CHEMBL2095172] [GtoPdb: 404414411] [UniProtKB: P14867P18507P47870]
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  • histone deacetylase 6/Histone deacetylase 6 in Human [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
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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
dihydroorotate dehydrogenase (quinone)/Dihydroorotate dehydrogenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1966] [GtoPdb: 2604] [UniProtKB: Q02127]
ChEMBL Binding affinity to N-terminal 6His-tagged recombinant human DHODH expressed in Escherichia coli strain BL21 (DE3) by isothermal titration calorimetry analysis B 6.15 pKi 710 nM Ki Eur J Med Chem (2022) 232: 114176-114176 [PMID:35151222]
ChEMBL Inhibition of N-terminal 6His-tagged recombinant human DHODH expressed in Escherichia coli strain BL21 (DE3) using dihydroorotate as substrate and CoQ6 as co-substrate incubated for 10 mins by DCIP dye based analysis B 6.06 pIC50 880 nM IC50 Eur J Med Chem (2022) 232: 114176-114176 [PMID:35151222]
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: 404414411] [UniProtKB: P14867P18507P47870]
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]
ChEMBL Positive allosteric modulation of GABAA alpha1beta2gamma2 receptor (unknown origin) stably expressed in CHO cells assessed as activation of GABA-induced response in presence of GABA by FLIPR assay B 5.24 pEC50 5800 nM EC50 J Nat Prod (2022) 85: 1201-1210 [PMID:35475609]
histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
ChEMBL Determination of IC50 values for inhibition of enzymatic assay of human HDAC6 with custom peptide substrate B 5.98 pIC50 1044 nM IC50 HDAC6 screening dataset using tau-based substrate in an enzymatic assay yields selective inhibitors and activators
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 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]