Biased Signaling Atlas

diphenhydramine

Agent/drug
Bioactivity

diphenhydramine

SMILES	CN(C)CCOC(c1ccccc1)c1ccccc1
InChIKey	ZZVUWRFHKOJYTH-UHFFFAOYSA-N

Chemical Properties

Hydrogen bond acceptors	2
Hydrogen bond donors	0
Rotatable bonds	6
Molecular weight (Da)	255.2

Database connections

PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank Drug Central PubChem PubChem GPCRdb
Ligand site mutations	TAS2R40

Search:

Receptor					Activity				Source

Protein	Gene	Species	Family	Class	Type	Min	Avg	Max	Database

5-HT_2A	5HT2A	Human	5-Hydroxytryptamine	A	pKi	6.43	6.43	6.43	ChEMBL
5-HT_2A	5HT2A	Human	5-Hydroxytryptamine	A	pKi	8.19	8.19	8.19	Drug Central
5-HT_2B	5HT2B	Human	5-Hydroxytryptamine	A	pKi	6.15	6.15	6.15	ChEMBL
5-HT_2B	5HT2B	Human	5-Hydroxytryptamine	A	pKi	8.21	8.21	8.21	Drug Central
5-HT_2C	5HT2C	Human	5-Hydroxytryptamine	A	pKi	6.29	6.29	6.29	ChEMBL
5-HT_2C	5HT2C	Human	5-Hydroxytryptamine	A	pKi	8.20	8.20	8.20	Drug Central
H₁	HRH1	Human	Histamine	A	pKi	7.90	7.90	7.90	Guide to Pharmacology
H₁	HRH1	Guinea pig	Histamine	A	pKd	7.93	7.93	7.93	ChEMBL
H₁	HRH1	Human	Histamine	A	pKi	7.70	7.77	7.83	ChEMBL
H₁	HRH1	Human	Histamine	A	pKi	5.00	7.49	8.21	PDSP Ki database
H₁	HRH1	Rat	Histamine	A	pKi	7.77	7.77	7.77	PDSP Ki database
H₁	HRH1	Guinea pig	Histamine	A	pKi	7.86	7.97	8.04	PDSP Ki database
H₁	HRH1	Human	Histamine	A	pKi	8.11	8.11	8.11	Drug Central
H₃	HRH3	Human	Histamine	A	pKi	5.00	5.00	5.00	PDSP Ki database
H₄	HRH4	Human	Histamine	A	pKi	4.37	4.67	4.96	ChEMBL
H₄	HRH4	Human	Histamine	A	pKi	5.00	5.00	5.00	PDSP Ki database
H₄	HRH4	Human	Histamine	A	pKi	8.36	8.36	8.36	Drug Central
M₁	ACM1	Human	Acetylcholine (muscarinic)	A	pKi	7.08	7.08	7.08	ChEMBL
M₁	ACM1	Human	Acetylcholine (muscarinic)	A	pKi	8.15	8.15	8.15	Drug Central
M₁	ACM1	Human	Acetylcholine (muscarinic)	A	pKi	7.00	7.00	7.00	PDSP Ki database

Showing 1 to 20 of 32 entries

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Receptor					Activity				Source

Protein	Gene	Species	Family	Class	Type	Min	Avg	Max	Database

5-HT_2A	5HT2A	Human	5-Hydroxytryptamine	A	pIC50	5.89	5.89	5.89	ChEMBL
5-HT_2B	5HT2B	Human	5-Hydroxytryptamine	A	pIC50	5.95	5.95	5.95	ChEMBL
5-HT_2C	5HT2C	Human	5-Hydroxytryptamine	A	pIC50	6.01	6.01	6.01	ChEMBL
H₁	HRH1	Guinea pig	Histamine	A	pIC50	9.00	9.00	9.00	ChEMBL
H₁	HRH1	Human	Histamine	A	pIC50	4.08	4.98	6.77	ChEMBL
H₁	HRH1	Guinea pig	Histamine	A	pIC50	8.05	8.05	8.05	Drug Central
H₄	HRH4	Human	Histamine	A	pIC50	4.96	4.96	4.96	ChEMBL
M₁	ACM1	Human	Acetylcholine (muscarinic)	A	pIC50	6.46	6.46	6.46	ChEMBL
M₁	ACM1	Rat	Acetylcholine (muscarinic)	A	Potency	5.60	6.15	6.70	ChEMBL
M₂	ACM2	Human	Acetylcholine (muscarinic)	A	pIC50	5.98	5.98	5.98	ChEMBL
M₃	ACM3	Human	Acetylcholine (muscarinic)	A	pIC50	6.19	6.19	6.19	ChEMBL
M₄	ACM4	Human	Acetylcholine (muscarinic)	A	pIC50	6.43	6.43	6.43	ChEMBL
M₅	ACM5	Human	Acetylcholine (muscarinic)	A	pIC50	6.79	6.79	6.79	ChEMBL
TSH	TSHR	Human	Glycoprotein hormone	A	Potency	4.80	4.80	4.80	ChEMBL

Showing 1 to 14 of 14 entries

diphenhydramine

Drug properties

Molecular type	Small molecule
Physiological/Surrogate	Surrogate
Approved drug	Yes

Distribution across phases (no. indications)

Phase I 0

Phase II 3

Phase III 0

Phase IV 18

Database connections

PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank Drug Central PubChem PubChem GPCRdb
Ligand site mutations	TAS2R40

Sankey plot

Drug Information

Search:

Target					Disease

Gene	Protein	Receptor family	Ligand type	Class	Name	Phase	ICD11	ATC	Association score

HRH1	H₁ receptor	Histamine receptors	Aminergic receptors	A	Acute nasopharyngitis	4	CA00	R06A, D04A	0.605
HRH1	H₁ receptor	Histamine receptors	Aminergic receptors	A	Allergic or hypersensitivity conditions of unspecified type	4	4A8Z	R06A, D04A	0.494
HRH1	H₁ receptor	Histamine receptors	Aminergic receptors	A	Allergic rhinitis due to other seasonal allergens	4	CA08.01	R06A, D04A	0.610
HRH1	H₁ receptor	Histamine receptors	Aminergic receptors	A	Allergic rhinitis, unspecified	4	CA08.0Z	R06A, D04A	0.616
HRH1	H₁ receptor	Histamine receptors	Aminergic receptors	A	Atopic eczema, unspecified	2	EA80.Z	R06A, D04A	0.474
HRH1	H₁ receptor	Histamine receptors	Aminergic receptors	A	Burns, unspecified	4	NE2Z	R06A, D04A	0.528
HRH1	H₁ receptor	Histamine receptors	Aminergic receptors	A	Chronic rhinitis	4	CA09.0	R06A, D04A	0.571
HRH1	H₁ receptor	Histamine receptors	Aminergic receptors	A	Cough	4	MD12	R06A, D04A	0.603
HRH1	H₁ receptor	Histamine receptors	Aminergic receptors	A	Dizziness and giddiness, unspecified	4	MB48.Z	R06A, D04A	0.462
HRH1	H₁ receptor	Histamine receptors	Aminergic receptors	A	Insomnia disorders, unspecified	2	7A0Z	R06A, D04A	0.579
HRH1	H₁ receptor	Histamine receptors	Aminergic receptors	A	Motion sickness	4	NF08.3	R06A, D04A	0.598
HRH1	H₁ receptor	Histamine receptors	Aminergic receptors	A	Nasal congestion	4	MD11.9	R06A, D04A	0.607
HRH1	H₁ receptor	Histamine receptors	Aminergic receptors	A	Nausea	4	MD90.0	R06A, D04A	0.592
HRH1	H₁ receptor	Histamine receptors	Aminergic receptors	A	Nausea or vomiting	4	MD90	R06A, D04A	0.526
HRH1	H₁ receptor	Histamine receptors	Aminergic receptors	A	Oral aphthae or aphtha-like ulceration	2	DA01.10	R06A, D04A	0.092
HRH1	H₁ receptor	Histamine receptors	Aminergic receptors	A	Oral mucositis	4	DA01.11	R06A, D04A	0.259
HRH1	H₁ receptor	Histamine receptors	Aminergic receptors	A	Pain, unspecified	4	MG3Z	R06A, D04A	0.591
HRH1	H₁ receptor	Histamine receptors	Aminergic receptors	A	Pruritus, unspecified	4	EC90.Z	R06A, D04A	0.602
HRH1	H₁ receptor	Histamine receptors	Aminergic receptors	A	Sunburn, unspecified	4	EJ40.Z	R06A, D04A	0.567
HRH1	H₁ receptor	Histamine receptors	Aminergic receptors	A	Urticaria of unspecified type	4	EB05	R06A, D04A	0.606

Showing 1 to 20 of 21 entries

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Main reference

diphenhydramine

diphenhydramine

Chemical Properties

Database connections

Bioactivities

diphenhydramine

Drug properties

Distribution across phases (no. indications)

Database connections

Sankey plot

Drug Information