GPCRdb

loperamide

Agent/drug
Bioactivity

loperamide

SMILES	CN(C)C(=O)C(CCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1
InChIKey	RDOIQAHITMMDAJ-UHFFFAOYSA-N

Chemical Properties

Hydrogen bond acceptors	3
Hydrogen bond donors	1
Rotatable bonds	7
Molecular weight (Da)	476.2

Database connections

PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank Drug Central PubChem GPCRdb

Bioactivities

Affinity
Potency

Search:

Receptor					Activity				Source

Protein	Gene	Species	Family	Class	Type	Min	Avg	Max	Database

α_1A	ADA1A	Rat	Adrenoceptors	A	pKi	5.60	5.60	5.60	ChEMBL
α_1B	ADA1B	Rat	Adrenoceptors	A	pKi	6.27	6.27	6.27	ChEMBL
α_1B	ADA1B	Human	Adrenoceptors	A	pKi	5.43	5.43	5.43	ChEMBL
α_1B	ADA1B	Rat	Adrenoceptors	A	pKi	8.20	8.20	8.20	Drug Central
α_1D	ADA1D	Human	Adrenoceptors	A	pKi	8.25	8.25	8.25	Drug Central
β₂	ADRB2	Human	Adrenoceptors	A	pKi	5.68	5.68	5.68	ChEMBL
β₂	ADRB2	Human	Adrenoceptors	A	pKi	8.25	8.25	8.25	Drug Central
δ	OPRD	Rat	Opioid	A	pKi	7.30	7.30	7.30	ChEMBL
δ	OPRD	Human	Opioid	A	pKi	6.50	6.54	6.58	ChEMBL
δ	OPRD	Human	Opioid	A	pKi	8.16	8.16	8.16	Drug Central
δ	OPRD	Rat	Opioid	A	pKi	8.14	8.14	8.14	Drug Central
κ	OPRK	Human	Opioid	A	pKi	5.90	6.52	7.14	ChEMBL
κ	OPRK	Human	Opioid	A	pKi	8.17	8.17	8.17	Drug Central
μ	OPRM	Human	Opioid	A	pKi	9.28	9.28	9.28	Guide to Pharmacology
μ	OPRM	Human	Opioid	A	pKi	8.59	9.17	9.57	ChEMBL
μ	OPRM	Human	Opioid	A	pKi	8.05	8.05	8.05	Drug Central
μ	OPRM	Rat	Opioid	A	pKi	8.01	8.01	8.01	Drug Central
μ	OPRM	Rat	Opioid	A	pKi	9.80	9.80	9.80	ChEMBL
5-HT_1D	5HT1D	Human	5-Hydroxytryptamine	A	pKi	5.58	5.58	5.58	ChEMBL
5-HT_2B	5HT2B	Human	5-Hydroxytryptamine	A	pKi	5.58	6.01	6.44	ChEMBL

Showing 1 to 20 of 29 entries

Search:

Receptor					Activity				Source

Protein	Gene	Species	Family	Class	Type	Min	Avg	Max	Database

α_1A	ADA1A	Rat	Adrenoceptors	A	pIC50	5.21	5.21	5.21	ChEMBL
α_1A	ADA1A	Rat	Adrenoceptors	A	pIC50	8.28	8.28	8.28	Drug Central
α_1B	ADA1B	Rat	Adrenoceptors	A	pIC50	6.01	6.01	6.01	ChEMBL
α_2A	ADA2A	Human	Adrenoceptors	A	pEC50	6.30	6.30	6.30	ChEMBL
β₂	ADRB2	Human	Adrenoceptors	A	pIC50	5.52	5.52	5.52	ChEMBL
β₂	ADRB2	Human	Adrenoceptors	A	pEC50	5.87	5.87	5.87	ChEMBL
δ	OPRD	Human	Opioid	A	pIC50	6.05	6.48	6.91	ChEMBL
δ	OPRD	Human	Opioid	A	pEC50	6.81	6.81	6.81	ChEMBL
κ	OPRK	Human	Opioid	A	pIC50	5.50	6.15	6.81	ChEMBL
μ	OPRM	Human	Opioid	A	pIC50	8.82	8.83	8.84	ChEMBL
5-HT_2B	5HT2B	Human	5-Hydroxytryptamine	A	pIC50	5.39	5.39	5.39	ChEMBL
ADGRF1	AGRF1	Human	ADGRF	B2	pEC50	5.69	5.69	5.69	ChEMBL
C3a	C3AR	Human	Complement peptide	A	pEC50	5.93	5.93	5.93	ChEMBL
C5a₁	C5AR1	Human	Complement peptide	A	pEC50	6.18	6.18	6.18	ChEMBL
C5a₂	C5AR2	Human	Complement peptide	A	pEC50	5.90	5.90	5.90	ChEMBL
D₃	DRD3	Human	Dopamine	A	pIC50	5.87	5.87	5.87	ChEMBL
FFA4	FFAR4	Human	Free fatty acid	A	pEC50	6.03	6.03	6.03	ChEMBL
FPR1	FPR1	Human	Formylpeptide	A	pEC50	6.07	6.07	6.07	ChEMBL
FPR2/ALX	FPR2	Human	Formylpeptide	A	pEC50	5.94	5.94	5.94	ChEMBL
GLP-1	GLP1R	Human	Glucagon	B1	pEC50	5.95	5.95	5.95	ChEMBL

Showing 1 to 20 of 28 entries

loperamide

Drug properties

Molecular type	Small molecule
Physiological/Surrogate	Surrogate
Approved drug	Yes

Clinical Trials

Phase I 0

Phase II 2

Phase III 1

Approved Yes

Database connections

PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank Drug Central PubChem GPCRdb

Sankey plot

Drug Information

Search:

Target					Disease				Phase

Gene	Protein	Receptor family	Ligand type	Class	Indication name	ICD11	ATC	Association score	Phase	Approved

OPRM	μ receptor	Opioid receptors	Peptide receptors	Class A	Dermatitis or eczema, unspecified	EA8Z	A07D	0.074	2	Yes
OPRM	μ receptor	Opioid receptors	Peptide receptors	Class A	Diarrhoea	ME05.1	A07D	0.606	4	Yes
OPRM	μ receptor	Opioid receptors	Peptide receptors	Class A	Faecal incontinence, unspecified	ME07.Z	A07D	0.495	3	Yes
OPRM	μ receptor	Opioid receptors	Peptide receptors	Class A	Pain, unspecified	MG3Z	A07D	0.609	2	Yes

Showing 1 to 4 of 4 entries