ChEMBL ligand: CHEMBL841 (Imodium, Loperamida, 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!
Calmodulin in Bovine [ChEMBL: CHEMBL6092] [UniProtKB: P62157] There should be some charts here, you may need to enable JavaScript!
carboxylesterase 2/Carboxylesterase 2 in Human [ChEMBL: CHEMBL3180] [GtoPdb: 3298] [UniProtKB: O00748] There should be some charts here, you may need to enable JavaScript!
CYP2D6/Cytochrome P450 2D6 in Human [ChEMBL: CHEMBL289] [GtoPdb: 1329] [UniProtKB: P10635] 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!
Menin in Human [ChEMBL: CHEMBL1615381] [UniProtKB: O00255] 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!
ABCB1/P-glycoprotein 1 in Human [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183] 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/Carboxylesterase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3180] [GtoPdb: 3298] [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 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]