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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL841 (Imodium, Loperamide)
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
There should be some charts here, you may need to enable JavaScript!
  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
There should be some charts here, you may need to enable JavaScript!
  • β2-adrenoceptor/Beta-2 adrenergic receptor in Human [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
There should be some charts here, you may need to enable JavaScript!
  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
There should be some charts here, you may need to enable JavaScript!
  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
There should be some charts here, you may need to enable JavaScript!
  • H2 receptor/Histamine H2 receptor in Human [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
There should be some charts here, you may need to enable JavaScript!
  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • NOP receptor/Nociceptin receptor in Human [ChEMBL: CHEMBL2014] [GtoPdb: 320] [UniProtKB: P41146]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
There should be some charts here, you may need to enable JavaScript!
  • SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
There should be some charts here, you may need to enable JavaScript!
  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
There should be some charts here, you may need to enable JavaScript!
  • Nav1.5/Sodium channel protein type V alpha subunit in Human [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
There should be some charts here, you may need to enable JavaScript!
  • Organic cation transporter 1/Solute carrier family 22 member 1 in Human [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
There should be some charts here, you may need to enable JavaScript!
  • TEK receptor tyrosine kinase/Tyrosine-protein kinase TIE-2 in Human [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763]
There should be some charts here, you may need to enable JavaScript!
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 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]