GPCRdb

phentolamine

Agent/drug
Bioactivity

phentolamine

SMILES	Cc1ccc(N(CC2=NCCN2)c2cccc(O)c2)cc1
InChIKey	MRBDMNSDAVCSSF-UHFFFAOYSA-N

Chemical Properties

Hydrogen bond acceptors	4
Hydrogen bond donors	2
Rotatable bonds	4
Molecular weight (Da)	281.2

Database connections

PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank Drug Central PubChem PubChem GPCRdb
Ligand site mutations	α_1A α_1B α_2A

Search:

Receptor					Activity				Source

Protein	Gene	Species	Family	Class	Type	Min	Avg	Max	Database

α_1A	ADA1A	Human	Adrenoceptors	A	pKi	8.20	8.40	8.60	Guide to Pharmacology
α_1A	ADA1A	Rat	Adrenoceptors	A	pKi	8.10	8.10	8.10	Guide to Pharmacology
α_1A	ADA1A	Rabbit	Adrenoceptors	A	pKd	8.20	8.20	8.20	ChEMBL
α_1A	ADA1A	Bovine	Adrenoceptors	A	pKi	8.17	8.63	9.10	ChEMBL
α_1A	ADA1A	Rat	Adrenoceptors	A	pKi	8.33	8.33	8.33	ChEMBL
α_1A	ADA1A	Human	Adrenoceptors	A	pKd	7.49	7.49	7.49	ChEMBL
α_1A	ADA1A	Human	Adrenoceptors	A	pKi	7.92	8.51	9.22	ChEMBL
α_1A	ADA1A	Bovine	Adrenoceptors	A	pKi	8.09	8.09	8.09	Drug Central
α_1A	ADA1A	Human	Adrenoceptors	A	pKi	8.08	8.08	8.08	Drug Central
α_1B	ADA1B	Human	Adrenoceptors	A	pKi	6.60	7.05	7.50	Guide to Pharmacology
α_1B	ADA1B	Golden hamster	Adrenoceptors	A	pKi	6.66	6.66	6.66	ChEMBL
α_1B	ADA1B	Rat	Adrenoceptors	A	pKi	7.35	7.35	7.35	ChEMBL
α_1B	ADA1B	Human	Adrenoceptors	A	pKi	7.32	7.82	8.32	ChEMBL
α_1B	ADA1B	Human	Adrenoceptors	A	pKi	7.74	7.74	7.74	PDSP Ki database
α_1B	ADA1B	Rat	Adrenoceptors	A	pKi	6.47	6.47	6.47	PDSP Ki database
α_1B	ADA1B	Human	Adrenoceptors	A	pKi	8.14	8.14	8.14	Drug Central
α_1B	ADA1B	Rat	Adrenoceptors	A	pKi	8.13	8.13	8.13	Drug Central
α_1B	ADA1B	Golden hamster	Adrenoceptors	A	pKi	8.18	8.18	8.18	Drug Central
α_1D	ADA1D	Human	Adrenoceptors	A	pKi	6.80	7.50	8.20	Guide to Pharmacology
α_1D	ADA1D	Human	Adrenoceptors	A	pKi	7.71	7.93	8.12	ChEMBL

Showing 1 to 20 of 68 entries

Search:

Receptor					Activity				Source

Protein	Gene	Species	Family	Class	Type	Min	Avg	Max	Database

α_1A	ADA1A	Rat	Adrenoceptors	A	pIC50	7.96	7.96	7.96	ChEMBL
α_1A	ADA1A	Human	Adrenoceptors	A	pIC50	8.96	8.96	8.96	ChEMBL
α_1A	ADA1A	Rat	Adrenoceptors	A	pIC50	8.10	8.10	8.10	Drug Central
α_1B	ADA1B	Rat	Adrenoceptors	A	pIC50	7.09	7.09	7.09	ChEMBL
α_1B	ADA1B	Human	Adrenoceptors	A	pIC50	7.97	7.97	7.97	ChEMBL
α_1D	ADA1D	Human	Adrenoceptors	A	pIC50	7.66	7.78	7.90	ChEMBL
α_2A	ADA2A	Human	Adrenoceptors	A	pEC50	7.10	7.10	7.10	Guide to Pharmacology
α_2A	ADA2A	Human	Adrenoceptors	A	pIC50	8.22	8.22	8.22	ChEMBL
α_2B	ADA2B	Human	Adrenoceptors	A	pIC50	7.75	7.75	7.75	ChEMBL
α_2C	ADA2C	Human	Adrenoceptors	A	pIC50	6.96	6.96	6.96	ChEMBL
5-HT_2A	5HT2A	Human	5-Hydroxytryptamine	A	pIC50	6.45	6.45	6.45	ChEMBL
5-HT_2B	5HT2B	Human	5-Hydroxytryptamine	A	pIC50	5.42	5.42	5.42	ChEMBL
5-HT_2C	5HT2C	Human	5-Hydroxytryptamine	A	pIC50	6.40	6.40	6.40	ChEMBL
H₁	HRH1	Rat	Histamine	A	pIC50	4.90	4.90	4.90	ChEMBL
H₁	HRH1	Rat	Histamine	A	pIC50	8.31	8.31	8.31	Drug Central
M₁	ACM1	Rat	Acetylcholine (muscarinic)	A	Potency	5.35	5.35	5.35	ChEMBL
TSH	TSHR	Human	Glycoprotein hormone	A	Potency	4.40	4.40	4.40	ChEMBL

Showing 1 to 17 of 17 entries

phentolamine

Drug properties

Molecular type	Small molecule
Physiological/Surrogate	Surrogate
Approved drug	Yes

Clinical Trials

Phase I 6

Phase II 6

Phase III 6

Approved Yes

Database connections

PubChem Guide To Pharmacology ChEMBL_compound_ids DrugBank Drug Central PubChem PubChem GPCRdb
Ligand site mutations	α_1A α_1B α_2A

Sankey plot

Drug Information

Search:

Target					Disease				Phase

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

ADA1A	α_1A-adrenoceptor	Adrenoceptors	Aminergic receptors	Class A	Anomalies of pupillary function	LA11.62	V03A, C04A	0.542	3	Yes
ADA1A	α_1A-adrenoceptor	Adrenoceptors	Aminergic receptors	Class A	Diseases of the circulatory system, unspecified	BE2Z	V03A, C04A	0.596	4	Yes
ADA1A	α_1A-adrenoceptor	Adrenoceptors	Aminergic receptors	Class A	Hypoglycaemia without associated diabetes	5A41	V03A, C04A	0.079	1	Yes
ADA1A	α_1A-adrenoceptor	Adrenoceptors	Aminergic receptors	Class A	Presbyopia	9D00.3	V03A, C04A	0.299	2	Yes
ADA1B	α_1B-adrenoceptor	Adrenoceptors	Aminergic receptors	Class A	Anomalies of pupillary function	LA11.62	V03A, C04A	0.487	3	Yes
ADA1B	α_1B-adrenoceptor	Adrenoceptors	Aminergic receptors	Class A	Diseases of the circulatory system, unspecified	BE2Z	V03A, C04A	0.591	4	Yes
ADA1B	α_1B-adrenoceptor	Adrenoceptors	Aminergic receptors	Class A	Hypoglycaemia without associated diabetes	5A41	V03A, C04A	0.079	1	Yes
ADA1B	α_1B-adrenoceptor	Adrenoceptors	Aminergic receptors	Class A	Presbyopia	9D00.3	V03A, C04A	0.299	2	Yes
ADA1D	α_1D-adrenoceptor	Adrenoceptors	Aminergic receptors	Class A	Anomalies of pupillary function	LA11.62	V03A, C04A	0.488	3	Yes
ADA1D	α_1D-adrenoceptor	Adrenoceptors	Aminergic receptors	Class A	Diseases of the circulatory system, unspecified	BE2Z	V03A, C04A	0.634	4	Yes
ADA1D	α_1D-adrenoceptor	Adrenoceptors	Aminergic receptors	Class A	Hypoglycaemia without associated diabetes	5A41	V03A, C04A	0.081	1	Yes
ADA1D	α_1D-adrenoceptor	Adrenoceptors	Aminergic receptors	Class A	Presbyopia	9D00.3	V03A, C04A	0.299	2	Yes
ADA2A	α_2A-adrenoceptor	Adrenoceptors	Aminergic receptors	Class A	Anomalies of pupillary function	LA11.62	V03A, C04A	0.484	3	Yes
ADA2A	α_2A-adrenoceptor	Adrenoceptors	Aminergic receptors	Class A	Diseases of the circulatory system, unspecified	BE2Z	V03A, C04A	0.590	4	Yes
ADA2A	α_2A-adrenoceptor	Adrenoceptors	Aminergic receptors	Class A	Hypoglycaemia without associated diabetes	5A41	V03A, C04A	0.018	1	Yes
ADA2A	α_2A-adrenoceptor	Adrenoceptors	Aminergic receptors	Class A	Presbyopia	9D00.3	V03A, C04A	0.368	2	Yes
ADA2B	α_2B-adrenoceptor	Adrenoceptors	Aminergic receptors	Class A	Anomalies of pupillary function	LA11.62	V03A, C04A	0.484	3	Yes
ADA2B	α_2B-adrenoceptor	Adrenoceptors	Aminergic receptors	Class A	Diseases of the circulatory system, unspecified	BE2Z	V03A, C04A	0.588	4	Yes
ADA2B	α_2B-adrenoceptor	Adrenoceptors	Aminergic receptors	Class A	Hypoglycaemia without associated diabetes	5A41	V03A, C04A	0.018	1	Yes
ADA2B	α_2B-adrenoceptor	Adrenoceptors	Aminergic receptors	Class A	Presbyopia	9D00.3	V03A, C04A	0.368	2	Yes

Showing 1 to 20 of 24 entries

Join us

Cite us

Main reference

phentolamine

phentolamine

Chemical Properties

Database connections

Bioactivities

phentolamine

Drug properties

Clinical Trials

Database connections

Sankey plot

Drug Information