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Compound Detail

CHEMBL87493

FENFLURAMINE
💊 Approved Drug
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💊 Approved Drug
CCNC(C)Cc1cccc(C(F)(F)F)c1
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL87493
Name FENFLURAMINE
Phase Approved
Structure Type MOL
InChI Key DBGIVFWFUFKIQN-UHFFFAOYSA-N
Therapeutic ✓ Yes

Known Names

Acino Brabafen Fenfluramin Fenfluramina Fenfluramine J5.760F Obedrex Pesos Phenfluramine Ponderax pa Rotondin S-768 +4 more
2
Targets
2
Activities
1
Assay Types
1
PK Parameters
20
Publications
16
Known Names
5
Indications

Molecular Properties

231.3
MW (Da)
3.25
ALogP
1
HBA
1
HBD
12.0
PSA (Ų)
0.84
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
First Approval 1963
Availability Withdrawn
Chirality Racemic

Routes of Administration

Oral

Flags

Black Box Warning Withdrawn
USAN Year 1965

Extended Properties

Molecular Formula C12H16F3N
MW 231.26
Aromatic Rings 1
Heavy Atoms 16
NP-Likeness -0.98

Indications

Epilepsy Obesity Lennox Gastaut Syndrome Spasms, Infantile Cocaine-Related Disorders

ATC Classification

A08AA02
fenfluramine
Level 1: ALIMENTARY TRACT AND METABOLISM
Level 2: ANTIOBESITY PREPARATIONS, EXCL. DIET PRODUCTS
N03AX26
fenfluramine
Level 1: NERVOUS SYSTEM
Level 2: ANTIEPILEPTICS

Drug Warnings

Withdrawn
respiratory toxicity
heart valve damage and pulmonary arterial hypertension
Country: France; China; United States   Year: 1997
Withdrawn
respiratory toxicity
arterial pulmonary hypertension
Country: France; China; United States   Year: 1997
Withdrawn
cardiotoxicity
heart valve damage and pulmonary arterial hypertension
Country: France; China; United States   Year: 1997

Activity Summary

EC50 2 meas. best 6.97

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium-dependent serotonin transporter
CHEMBL313
 EC50 6.97 6.97 108.0 1
Unchecked
CHEMBL612545
 EC50 6.13 6.13 740.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 79.0 % Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Sodium-dependent serotonin transporter EC50 = 108.0 nM 6.97 Activity at SERT in rat synaptosomes assessed as release of [3H]HT after 5 mins ... 28244748
Unchecked EC50 = 740.0 nM 6.13 Activity at NET in rat synaptosomes assessed as release of [3H]NE after 30 mins ... 28244748

Literature References

PubMed DOI Target Context # Activities
16472241 10.2174/1570163043334794 Hepatotoxicity 18
37468498 10.1038/s41467-023-40064-9 Alpha-1A adrenergic receptor 4
17428028 10.1021/ci6004542 Phospholipidosis 3
37468498 10.1038/s41467-023-40064-9 5-hydroxytryptamine receptor 2B 3
37468498 10.1038/s41467-023-40064-9 Muscarinic acetylcholine receptor M2 3
37468498 10.1038/s41467-023-40064-9 Cannabinoid receptor 1 3
37468498 10.1038/s41467-023-40064-9 Alpha-2A adrenergic receptor 3
37468498 10.1038/s41467-023-40064-9 5-hydroxytryptamine receptor 1A 3
10891117 10.1021/jm0000564 ADMET 2
37468498 10.1038/s41467-023-40064-9 Beta-2 adrenergic receptor 2
37468498 10.1038/s41467-023-40064-9 Gamma-aminobutyric acid receptor subunit alpha-1 2
37468498 10.1038/s41467-023-40064-9 D(1A) dopamine receptor 2
37468498 10.1038/s41467-023-40064-9 Histamine H2 receptor 2
- 10.6019/CHEMBL4651402 SARS-CoV-2 2
621713 10.1021/jm00200a008 Mus musculus 2
37468498 10.1038/s41467-023-40064-9 5-hydroxytryptamine receptor 2A 2
18032040 10.1016/j.bmcl.2007.10.115 Rattus norvegicus 2
10891117 10.1021/jm0000564 No relevant target 2
37468498 10.1038/s41467-023-40064-9 Histamine H1 receptor 1
621713 10.1021/jm00200a008 Canis familiaris 1

Data from ChEMBL 36 via Core Engine