loperamide [Ligand Id: 7215] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL841 (Imodium, Loperamide)
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
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  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
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  • β2-adrenoceptor/Beta-2 adrenergic receptor in Human [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
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  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
  • δ receptor/Delta opioid receptor in Rat [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
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  • H2 receptor/Histamine H2 receptor in Human [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
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  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
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  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
  • μ receptor/Mu opioid receptor in Rat [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
  • Mu opioid receptor in Guinea pig [ChEMBL: CHEMBL4354] [UniProtKB: P97266]
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  • NOP receptor/Nociceptin receptor in Human [ChEMBL: CHEMBL2014] [GtoPdb: 320] [UniProtKB: P41146]
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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  • SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
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  • Nav1.5/Sodium channel protein type V alpha subunit in Human [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
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  • Organic cation transporter 1/Solute carrier family 22 member 1 in Human [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
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  • TEK receptor tyrosine kinase/Tyrosine-protein kinase TIE-2 in Human [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 5.6 pKi 2517 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 5.21 pIC50 6219 nM IC50 DrugMatrix in vitro pharmacology data
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
ChEMBL DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) B 6.27 pKi 534 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) B 6.02 pIC50 965 nM IC50 DrugMatrix in vitro pharmacology data
β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
ChEMBL DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177) B 5.68 pKi 2066 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177) B 5.52 pIC50 3005 nM IC50 DrugMatrix in vitro pharmacology data
Calmodulin in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6092] [UniProtKB: P62157]
ChEMBL Binding affinity to bovine brain CaM by FTPFACE analysis B 5.46 pKd 3500 nM Kd Eur J Med Chem (2016) 116: 36-45 [PMID:27043269]
ChEMBL Displacement of [3H]trifluoperazine from bovine brain CaM in presence of calcium B 4.92 pIC50 12000 nM IC50 Eur J Med Chem (2016) 116: 36-45 [PMID:27043269]
Carboxylesterase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3180] [UniProtKB: O00748]
ChEMBL Inhibition of human CES2A using 4-methylumbelliferone as a substrate B 5.82 pKi 1500 nM Ki Eur J Med Chem (2021) 209: 112856-112856 [PMID:33007602]
ChEMBL Inhibition of hCES2A in human liver microsome assessed as reduction in fluorescein diacetate hydrolysis preincubated for 10 mins followed by substrate addition measured after 20 mins by fluorescence analysis B 5.17 pIC50 6800 nM IC50 Eur J Med Chem (2021) 209: 112856-112856 [PMID:33007602]
ChEMBL Inhibition of human CE2 using fluorescein diacetate as substrate preincubated for 10 mins followed by substrate addition and measured after 10 mins by luminescence assay B 5.34 pIC50 4600 nM IC50 J Nat Prod (2020) 83: 489-496 [PMID:32058719]
ChEMBL Inhibition of CE2 in human liver microsomes using fluorescein diacetate as substrate preincubated for 10 mins followed by substrate addition measured after 20 mins by luminescence assay B 5.39 pIC50 4060 nM IC50 Eur J Med Chem (2018) 145: 717-725 [PMID:29353723]
CYP2D6/Cytochrome P450 2D6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL289] [GtoPdb: 1329] [UniProtKB: P10635]
ChEMBL DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) B 5.7 pIC50 2000 nM IC50 DrugMatrix in vitro pharmacology data
δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
ChEMBL DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole) B 6.5 pKi 316 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole) B 6.05 pIC50 896 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Inhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranes F 6.81 pEC50 156 nM EC50 J Med Chem (2004) 47: 5009-5020 [PMID:15456245]
δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
ChEMBL Binding affinity for delta opioid receptor of rat brain B 7.3 pKi 50.1 nM Ki J Med Chem (2004) 47: 5009-5020 [PMID:15456245]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Displacement of [3H]-N-methylspiperone from human dopamine D2 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis B 5.24 pKi 5790 nM Ki J Med Chem (2021) 64: 7778-7808 [PMID:34011153]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Displacement of [3H]-N-methylspiperone from human dopamine D3 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis B 5.71 pKi 1940 nM Ki J Med Chem (2021) 64: 7778-7808 [PMID:34011153]
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 6.34 pKi 454 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 5.87 pIC50 1337 nM IC50 DrugMatrix in vitro pharmacology data
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis B 5.73 pKi 1850 nM Ki J Med Chem (2021) 64: 7778-7808 [PMID:34011153]
H2 receptor/Histamine H2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
ChEMBL DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) B 5.52 pKi 3030 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) B 5.51 pIC50 3081 nM IC50 DrugMatrix in vitro pharmacology data
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine) B 5.9 pKi 1250 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine) B 5.51 pIC50 3125 nM IC50 DrugMatrix in vitro pharmacology data
Menin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1615381] [UniProtKB: O00255]
ChEMBL Displacement of FITC-MBM1 from full length human menin measured after 2 hrs by fluorescence polarization assay B 4.16 pIC50 69000 nM IC50 Bioorg Med Chem (2018) 26: 356-365 [PMID:29254892]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) B 9.23 pKi 0.59 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Binding affinity for recombinant human mu-opioid receptor was determined by using [3H]- diprenophine radioligand B 9.28 pKi 0.53 nM Ki Bioorg Med Chem Lett (2004) 14: 5275-5279 [PMID:15454210]
GtoPdb - - 9.28 pKi 0.53 nM Ki Bioorg Med Chem Lett (2004) 14: 5275-9 [PMID:15454210]
ChEMBL Displacement of [3H]DAMGO from human mu opioid receptor expressed in HEK293 cell membrane incubated for 60 mins by radioligand binding assay B 9.57 pKi 0.27 nM Ki J Med Chem (2021) 64: 7778-7808 [PMID:34011153]
ChEMBL DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) B 8.84 pIC50 1.45 nM IC50 DrugMatrix in vitro pharmacology data
μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
ChEMBL Binding affinity for Mu opioid receptor of rat brain B 9.8 pKi 0.16 nM Ki J Med Chem (2004) 47: 5009-5020 [PMID:15456245]
Mu opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266]
ChEMBL Inhibition of mu opioid receptor mediated GTPgammaS binding to CHO cell membranes F 7.24 pEC50 58 nM EC50 J Med Chem (2004) 47: 5009-5020 [PMID:15456245]
NOP receptor/Nociceptin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2014] [GtoPdb: 320] [UniProtKB: P41146]
ChEMBL Binding affinity for opioid receptor like 1 expressed in HEK293 cells B 5 pKi >10000 nM Ki Bioorg Med Chem Lett (2004) 14: 5275-5279 [PMID:15454210]
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells F 5.6 pIC50 2500 nM IC50 Anesthesiology (2002) 96: 913-920 [PMID:11964599]
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 5.58 pKi 2613 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 5.39 pIC50 4105 nM IC50 DrugMatrix in vitro pharmacology data
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) B 5.93 pKi 1170 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) B 5.66 pIC50 2202 nM IC50 DrugMatrix in vitro pharmacology data
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) B 6.58 pKi 264 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) B 6.2 pIC50 628 nM IC50 DrugMatrix in vitro pharmacology data
Nav1.5/Sodium channel protein type V alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
ChEMBL Inhibition of human Nav1.5 channel expressed in HEK293 cells at holding potential of -70 mV by whole cell patch clamp assay B 6.62 pIC50 239 nM IC50 Bioorg Med Chem Lett (2018) 28: 446-451 [PMID:29274816]
Organic cation transporter 1/Solute carrier family 22 member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
ChEMBL Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy B 4.63 pIC50 23700 nM IC50 J Med Chem (2008) 51: 5932-5942 [PMID:18788725]
TEK receptor tyrosine kinase/Tyrosine-protein kinase TIE-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763]
ChEMBL Binding affinity to human recombinant Tie2 by SPR assay B 5.23 pKd 5900 nM Kd Bioorg Med Chem Lett (2012) 22: 2388-2392 [PMID:22406116]

ChEMBL data shown on this page come from version 32:

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]