Compound Detail
CHEMBL284348
DALFAMPRIDINE 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL284348 |
| Name | DALFAMPRIDINE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | NUKYPUAOHBNCPY-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
2
Targets
10
Activities
3
Assay Types
0
PK Parameters
20
Publications
10
Known Names
19
Indications
1
Mechanisms
Molecular Properties
94.1
MW (Da)
0.66
ALogP
2
HBA
1
HBD
38.9
PSA (Ų)
0.51
QED
0
Ro5 Violations
0
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 2010 |
| Availability | Prescription |
| Chirality | Achiral |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Voltage-gated potassium channel blocker | BLOCKER | Voltage-gated potassium channel | ✓ | ✓ |
Indications
Multiple Sclerosis Ischemic Stroke Multiple Sclerosis, Chronic Progressive Multiple Sclerosis, Relapsing-Remitting Muscle Spasticity Spinal Cord Injuries Stroke Carpal Tunnel Syndrome Guillain-Barre Syndrome Memory, Short-Term Muscular Atrophy, Spinal Prostatic Diseases Sleep Apnea, Obstructive Trauma, Nervous System Wounds and Injuries Cerebral Palsy Motor Neuron Disease Renal Insufficiency Optic Neuritis
ATC Classification
N07XX07
fampridine
Level 1: NERVOUS SYSTEM
Level 2: OTHER NERVOUS SYSTEM DRUGS
Activity Summary
Kd 5 meas. best 4.54
IC50 4 meas. best 4.05
Ki 1 meas.
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Unchecked CHEMBL612545 | Kd | 4.54 | 4.54 | 29000.0 | 1 |
| Potassium voltage-gated channel subfamily A member 1 CHEMBL2309 | IC50 | 4.05 | 4.05 | 89000.0 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Unchecked | Kd | = | 29000.0 | nM | 4.54 | Selectivity for Kv1.3 voltage-gated K+ channel over IKCa1 [Ca2+] activated K+ ch... | 15084131 |
| Potassium voltage-gated channel subfamily A member 1 | IC50 | = | 89000.0 | nM | 4.05 | Inhibition of Kv1.1 (unknown origin) | 28225274 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| - | 10.1016/S0960-894X(00)80544-2 | Rattus norvegicus | 20 |
| 18023348 | 10.1016/j.bmcl.2007.10.077 | Rattus norvegicus | 8 |
| 15084131 | 10.1021/jm030523s | Unchecked | 5 |
| - | 10.6019/CHEMBL4495565 | SARS-CoV-2 | 4 |
| 21834513 | 10.1021/jm2001103 | Human immunodeficiency virus 1 | 2 |
| 1271403 | 10.1021/jm00227a008 | No relevant target | 2 |
| 28225274 | 10.1021/acs.jmedchem.6b01262 | ADMET | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Prostaglandin G/H synthase 1 | 2 |
| 28225274 | 10.1021/acs.jmedchem.6b01262 | Unchecked | 2 |
| - | 10.6019/CHEMBL4808148 | Histone deacetylase 6 | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Thromboxane A2 receptor | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Muscarinic acetylcholine receptor M1 | 2 |
| 36403421 | 10.1016/j.ejmech.2022.114935 | Phosphoserine phosphatase SerB2 | 2 |
| - | 10.6019/CHEMBL4495564 | Replicase polyprotein 1ab | 2 |
| 10514292 | 10.1021/jm990224w | Acetylcholinesterase | 2 |
| 2579237 | 10.1021/jm00381a019 | Sodium channel alpha subunits; brain (Types I, II, III) | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Alpha-1A adrenergic receptor | 2 |
| - | 10.6019/CHEMBL4651402 | SARS-CoV-2 | 2 |
| 20356304 | 10.1021/jm901688m | Mus musculus | 1 |
| 20637607 | 10.1016/j.bmcl.2010.06.090 | High affinity choline transporter 1 | 1 |
Data from ChEMBL 36 via Core Engine