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Compound Detail

CHEMBL418995

AMINEPTINE
💊 Approved Drug
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💊 Approved Drug
O=C(O)CCCCCCNC1c2ccccc2CCc2ccccc21
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL418995
Name AMINEPTINE
Phase Approved
Structure Type MOL
InChI Key ONNOFKFOZAJDHT-UHFFFAOYSA-N

Known Names

Amineptin Amineptina Amineptine Dea no. 1219
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
20
Publications
4
Known Names
1
Indications
1
Mechanisms

Molecular Properties

337.5
MW (Da)
4.50
ALogP
2
HBA
2
HBD
49.3
PSA (Ų)
0.70
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Withdrawn
Chirality Achiral

Flags

Withdrawn

Extended Properties

Molecular Formula C22H27NO2
MW 337.46
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness 0.20

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Dopamine D1 and D2 receptor antagonist ANTAGONIST Dopamine D1 and D2 receptor ✓ ✓

Indications

Depressive Disorder

ATC Classification

N06AA19
amineptine
Level 1: NERVOUS SYSTEM
Level 2: PSYCHOANALEPTICS

Drug Warnings

Withdrawn
dermatological toxicity
Abuse; Dependence; Severe Acne
Country: France; Thailand; United Arab Emirates; Vietnam; Morocco   Year: 1999
Withdrawn
drug misuse
Potential for abuse and risk of dependence; Follows the decision taken by France to suspend amineptine on the basis of abuse and dependency potential
Country: France; Thailand; United Arab Emirates; Vietnam; Morocco   Year: 1999
Withdrawn
drug misuse
Potential for abuse and risk of dependence
Country: France; Thailand; United Arab Emirates; Vietnam; Morocco   Year: 1999
Withdrawn
drug misuse
Abuse; Dependence; Severe Acne
Country: France; Thailand; United Arab Emirates; Vietnam; Morocco   Year: 1999
Withdrawn
drug misuse
Potential for abuse and risk of dependence
Country: France; Thailand; United Arab Emirates; Vietnam; Morocco   Year: 1999
Withdrawn
drug misuse
Potential for abuse and risk of dependence; Follows the decision taken by France to suspend amineptine on the basis of abuse and dependency potential
Country: France; Thailand; United Arab Emirates; Vietnam; Morocco   Year: 1999
Withdrawn
drug misuse
Abuse; Dependence; Severe Acne
Country: France; Thailand; United Arab Emirates; Vietnam; Morocco   Year: 1999

Activity Summary

IC50 1 meas. best 6.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium-dependent dopamine transporter
CHEMBL338
 IC50 6.0 6.0 1000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Sodium-dependent dopamine transporter IC50 = 1000.0 nM 6.0 Inhibition of dopamine transporter-mediated [3H]dopamine uptake in Wistar rat st... 8676127

Literature References

PubMed DOI Target Context # Activities
15646539 10.1016/s0399-8320(04)95062-2 Unchecked 11
15646539 10.1016/s0399-8320(04)95062-2 NON-PROTEIN TARGET 8
20014752 10.1021/tx900326k Hepatotoxicity 3
37468498 10.1038/s41467-023-40064-9 Nuclear receptor subfamily 1 group I member 2 3
37468498 10.1038/s41467-023-40064-9 Progesterone receptor 2
19188399 10.1128/aac.00956-08 Pleiotropic ABC efflux transporter of multiple drugs 2
37468498 10.1038/s41467-023-40064-9 Muscarinic acetylcholine receptor M2 2
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
37468498 10.1038/s41467-023-40064-9 Gamma-aminobutyric acid receptor subunit alpha-1 2
37468498 10.1038/s41467-023-40064-9 Alpha-2A adrenergic receptor 2
37468498 10.1038/s41467-023-40064-9 5-hydroxytryptamine receptor 2B 2
37468498 10.1038/s41467-023-40064-9 Androgen receptor 2
10447960 10.1021/jm9910369 ADMET 2
37468498 10.1038/s41467-023-40064-9 5-hydroxytryptamine receptor 1A 2
37468498 10.1038/s41467-023-40064-9 Alpha-1A adrenergic receptor 2
26948801 10.1016/j.drudis.2016.02.015 Homo sapiens 2
37468498 10.1038/s41467-023-40064-9 5-hydroxytryptamine receptor 2A 2
37468498 10.1038/s41467-023-40064-9 Cannabinoid receptor 1 2
8676127 10.1021/np50124a001 Unchecked 2
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2

Data from ChEMBL 36 via Core Engine