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Compound Detail

CHEMBL1214124

PERAMPANEL
💊 Approved Drug
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💊 Approved Drug
N#Cc1ccccc1-c1cc(-c2ccccn2)cn(-c2ccccc2)c1=O
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL1214124
Name PERAMPANEL
Phase Approved
Structure Type MOL
InChI Key PRMWGUBFXWROHD-UHFFFAOYSA-N
Therapeutic ✓ Yes

Known Names

E-2007 E2007 ER-155055-90 Fycompa Perampanel
3
Targets
10
Activities
1
Assay Types
11
PK Parameters
20
Publications
5
Known Names
17
Indications
1
Mechanisms

Molecular Properties

349.4
MW (Da)
4.44
ALogP
4
HBA
0
HBD
58.7
PSA (Ų)
0.55
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
First Approval 2012
Availability Prescription
Chirality Achiral

Routes of Administration

Oral

Flags

Black Box Warning Natural Product First in Class
USAN Stem -ampa-
USAN Year 2006

Extended Properties

Molecular Formula C23H15N3O
MW 349.39
Aromatic Rings 4
Heavy Atoms 27
NP-Likeness -1.26

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Glutamate receptor ionotropic AMPA antagonist ANTAGONIST Glutamate receptor ionotropic AMPA ✓ ✓

Indications

Epilepsies, Partial Epilepsy Seizures Epilepsy, Tonic-Clonic Epilepsy, Tonic-Clonic Lennox Gastaut Syndrome Parkinson Disease Amyotrophic Lateral Sclerosis Diabetic Neuropathies Essential Tremor Migraine Disorders Neuralgia Small Fiber Neuropathy Alcoholism Bipolar Disorder Depressive Disorder, Major Torticollis

ATC Classification

N03AX22
perampanel
Level 1: NERVOUS SYSTEM
Level 2: ANTIEPILEPTICS

Activity Summary

IC50 10 meas. best 7.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
 IC50 7.22 5.5625 60.0 4
Glutamate receptor 1
CHEMBL2009
 IC50 6.61 6.05 243.0 5
Glutamate receptor 3
CHEMBL3595
 IC50 5.68 5.68 2100.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 360.0 ng.hr.mL-1 Rattus norvegicus
AUC 560.0 ng.hr.mL-1 Rattus norvegicus
CL 0.108 mL.min-1.g-1 Rattus norvegicus
CL 0.02 mL.min-1.g-1 Mus musculus
CL 0.009 mL.min-1.g-1 Homo sapiens
CL 30.33 mL.min-1.kg-1 Rattus norvegicus
Cmax 486.56 nM Rattus norvegicus
F 64.3 % Rattus norvegicus
T1/2 70.0 hr Homo sapiens
T1/2 2.37 hr Rattus norvegicus
Tmax 0.5 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 60.0 nM 7.22 Antagonist activity at AMPA receptor in E18 rat cerebral cortical neurons assess... 23181587
Unchecked IC50 = 93.0 nM 7.03 Antagonist activity at AMPA receptor in rat cortical membrane assessed as inhibi... 20356304
Glutamate receptor 1 IC50 = 243.0 nM 6.61 Antagonist activity at human iGluA1 receptor flop isoform expressed in CHO-S cel... 27067148
Glutamate receptor 1 IC50 = 485.0 nM 6.31 Antagonist activity at human iGluA1 receptor flop isoform expressed in CHO-S cel... 27067148
Glutamate receptor 1 IC50 = 623.0 nM 6.21 Antagonist activity at human iGluA1 receptor flop isoform expressed in CHO-S cel... 27067148
Glutamate receptor 1 IC50 = 1180.0 nM 5.93 Antagonist activity at human iGluA1 receptor flop isoform expressed in CHO-S cel... 27067148
Glutamate receptor 3 IC50 = 2100.0 nM 5.68 Blockade of whole cell current in GluA3i-G (unknown origin) transfected in HEK29... 30891119
Glutamate receptor 1 IC50 = 6510.0 nM 5.19 Antagonist activity at human iGluA1 receptor flip isoform expressed in CHO-S cel... 27067148
Unchecked IC50 = 100000.0 nM 4.0 Inhibition of recombinant His6-tagged SARS-CoV-2 main protease using Dabcyl-KTSA... 33324471
Unchecked IC50 = 100000.0 nM 4.0 Inhibition of recombinant SARS-CoV-2 main protease using Dabcyl-KTSAVLQ-SGFRKM-E... 34408808

Literature References

PubMed DOI Target Context # Activities
30891119 10.1021/acsmedchemlett.8b00322 Glutamate receptor 3 18
23181587 10.1021/jm301268u Rattus norvegicus 8
27067148 10.1021/acs.jmedchem.6b00125 Glutamate receptor 1 5
23181587 10.1021/jm301268u Mus musculus 4
20356304 10.1021/jm901688m Mus musculus 3
23181587 10.1021/jm301268u Nucleic Acid 3
27067148 10.1021/acs.jmedchem.6b00125 Rattus norvegicus 3
37468498 10.1038/s41467-023-40064-9 Voltage-dependent L-type calcium channel subunit alpha-1C 2
37468498 10.1038/s41467-023-40064-9 Beta-1 adrenergic receptor 2
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
33324471 10.1021/acsmedchemlett.0c00521 Unchecked 2
- 10.6019/CHEMBL4651402 SARS-CoV-2 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 Muscarinic acetylcholine receptor M2 2
37468498 10.1038/s41467-023-40064-9 Alpha-1A adrenergic receptor 2
37468498 10.1038/s41467-023-40064-9 Beta-2 adrenergic receptor 2
23181587 10.1021/jm301268u Liver microsomes 2
37468498 10.1038/s41467-023-40064-9 5-hydroxytryptamine receptor 1A 2
37468498 10.1038/s41467-023-40064-9 Nuclear receptor subfamily 1 group I member 2 2

Data from ChEMBL 36 via Core Engine