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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 |
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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: 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] |
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]