Compound Detail
CHEMBL1093
ARTICAINE 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL1093 |
| Name | ARTICAINE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | QTGIAADRBBLJGA-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
20
Publications
5
Known Names
4
Indications
Molecular Properties
284.4
MW (Da)
2.17
ALogP
5
HBA
2
HBD
67.4
PSA (Ų)
0.79
QED
0
Ro5 Violations
6
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 2000 |
| Availability | Prescription |
| Chirality | Racemic |
Indications
Pulpitis Pain Periodontitis Renal Insufficiency
ATC Classification
N01BB08
articaine
Level 1: NERVOUS SYSTEM
Level 2: ANESTHETICS
N01BB58
articaine, combinations
Level 1: NERVOUS SYSTEM
Level 2: ANESTHETICS
Activity Summary
IC50 4 meas. best 4.29
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Sodium channel alpha subunits; brain (Types I, II, III) CHEMBL2096682 | IC50 | 4.29 | 4.29 | 51000.0 | 1 |
| Unchecked CHEMBL612545 | IC50 | 4.29 | 4.29 | 51000.0 | 2 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Sodium channel alpha subunits; brain (Types I, II, III) | IC50 | = | 51000.0 | nM | 4.29 | Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on vol... | 2579237 |
| Unchecked | IC50 | = | 51000.0 | nM | 4.29 | Displacement of [3H]-BTX-B from neuronal voltage-gated sodium channel in rat cer... | 19346132 |
| Unchecked | IC50 | = | 51286.14 | nM | 4.29 | Displacement of [3H]-BTX-B from neuronal voltage-gated sodium channel in rat cer... | 19346132 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 22194678 | 10.1371/journal.pcbi.1002310 | Hepatotoxicity | 14 |
| 2579237 | 10.1021/jm00381a019 | Sodium channel alpha subunits; brain (Types I, II, III) | 3 |
| - | 10.6019/CHEMBL4651402 | SARS-CoV-2 | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Thromboxane A2 receptor | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Prostaglandin G/H synthase 1 | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Alpha-1A adrenergic receptor | 2 |
| - | 10.6019/CHEMBL4808148 | Histone deacetylase 6 | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Muscarinic acetylcholine receptor M1 | 2 |
| 19346132 | 10.1016/j.bmc.2008.10.031 | Unchecked | 2 |
| 24332655 | 10.1016/j.bmc.2013.11.049 | Unchecked | 1 |
| 38318365 | 10.1016/j.isci.2024.108907 | Deoxynucleoside triphosphate triphosphohydrolase SAMHD1 | 1 |
| 12873507 | 10.1016/s0960-894x(03)00535-3 | NON-PROTEIN TARGET | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | D(1A) dopamine receptor | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Voltage-gated inwardly rectifying potassium channel KCNH2 | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Sodium-dependent dopamine transporter | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Estrogen receptor | 1 |
| 7381857 | 10.1021/jm00179a017 | Cavia porcellus | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Sodium-dependent noradrenaline transporter | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Sodium-dependent serotonin transporter | 1 |
| 7381857 | 10.1021/jm00179a017 | Albumin | 1 |
Data from ChEMBL 36 via Core Engine