ArrestinDb

GEPIRONE

Agent/drug
Bioactivity

GEPIRONE

SMILES	CC1(C)CC(=O)N(CCCCN2CCN(c3ncccn3)CC2)C(=O)C1
InChIKey	QOIGKGMMAGJZNZ-UHFFFAOYSA-N

Chemical Properties

Hydrogen bond acceptors	6
Hydrogen bond donors	0
Rotatable bonds	6
Molecular weight (Da)	359.2

Database connections

ChEMBL_compound_ids PubChem DrugBank PubChem GPCRdb

Bioactivities

Affinity
Potency

Search:

Receptor					Activity				Source

Protein	Gene	Species	Family	Class	Type	Min	Avg	Max	Database

5-HT_1A	5HT1A	Rat	5-Hydroxytryptamine	A	pKi	7.16	7.33	7.50	ChEMBL
5-HT_1A	5HT1A	Human	5-Hydroxytryptamine	A	pKd	7.10	7.10	7.10	ChEMBL
5-HT_1A	5HT1A	Human	5-Hydroxytryptamine	A	pKi	7.50	7.70	7.89	ChEMBL
5-HT_1A	5HT1A	Rat	5-Hydroxytryptamine	A	pKi	7.15	7.15	7.15	PDSP Ki database
5-HT_1A	A0A4X1UTF5	Pig	5-Hydroxytryptamine	A	pKi	7.05	7.05	7.05	PDSP Ki database
5-HT_1A	5HT1A	Human	5-Hydroxytryptamine	A	pKi	8.10	8.10	8.10	Drug Central
5-HT_1A	5HT1A	Rat	5-Hydroxytryptamine	A	pKi	8.12	8.12	8.12	Drug Central
5-HT_1B	5HT1B	Rat	5-Hydroxytryptamine	A	pKi	5.00	5.00	5.00	PDSP Ki database
5-HT_2A	5HT2A	Human	5-Hydroxytryptamine	A	pKi	5.44	5.44	5.44	ChEMBL
5-HT_2A	5HT2A	Human	5-Hydroxytryptamine	A	pKi	8.26	8.26	8.26	Drug Central
5-HT_2C	K7GSR7	Pig	5-Hydroxytryptamine	A	pKi	5.00	5.00	5.00	PDSP Ki database
5-HT_2C	5HT2C	Rat	5-Hydroxytryptamine	A	pKi	5.00	5.00	5.00	PDSP Ki database
D₂	DRD2	Human	Dopamine	A	pKi	5.37	6.30	7.24	ChEMBL
D₂	DRD2	Human	Dopamine	A	pKi	8.14	8.14	8.14	Drug Central

Showing 1 to 14 of 14 entries

Search:

Receptor					Activity				Source

Protein	Gene	Species	Family	Class	Type	Min	Avg	Max	Database

5-HT_1A	5HT1A	Human	5-Hydroxytryptamine	A	pIC50	6.94	6.94	6.94	ChEMBL
5-HT_1A	5HT1A	Human	5-Hydroxytryptamine	A	pEC50	6.54	6.54	6.54	ChEMBL

Showing 1 to 2 of 2 entries

GEPIRONE

Drug properties

Molecular type	Small molecule
Physiological/Surrogate	Surrogate
Approved drug	Yes

Clinical Trials

Phase I 0

Phase II 1

Phase III 0

Approved Yes

Database connections

ChEMBL_compound_ids PubChem DrugBank 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

5HT1A	5-HT_1A receptor	5-Hydroxytryptamine receptors	Aminergic receptors	Class A	Cocaine dependence, unspecified	6C45.2Z		0.107	2	Yes
5HT1A	5-HT_1A receptor	5-Hydroxytryptamine receptors	Aminergic receptors	Class A	Single episode depressive disorder, severe, without psychotic symptoms	6A70.3		0.634	4	Yes

Showing 1 to 2 of 2 entries