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kainic acid 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 3201 | 487-79-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
(2S-(2 alpha,3 beta,4 beta))-2-Carboxy-4-(1-methylethenyl)-3-pyrrolidineacetic acid. Ascaricide obtained from the red alga Digenea simplex. It is a potent excitatory amino acid agonist at some types of excitatory amino acid receptors and has been used to discriminate among receptor types. Like many excitatory amino acid agonists it can cause neurotoxicity and has been used experimentally for that purpose.
|
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,ACVRL1,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GSK3B,IKBKB,ITK,JAK1,JAK2,JAK3,KDR,MAP2K6,MAP3K14,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPKAPK2,MTOR,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PIK3CD,PIK3CG,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ZAP70 | 54 | |||
| kinase-selectivity-class | ACVR2B,AXL,BRAF,CDK9,DYRK1B,EIF2AK3,EPHB4,GRK2,MAP2K6,MAP3K14,MAPK7,PIK3CD,PIK3CG,PRKDC,STK33,SYK,TEK,TGFBR1 | 18 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
None
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| MeSH PA | D000871 | Anthelmintics |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000969 | Antinematodal Agents |
| MeSH PA | D000977 | Antiparasitic Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018690 | Excitatory Amino Acid Agonists |
| CHEBI has role | CHEBI:35444 | antinematodal drug |
| CHEBI has role | CHEBI:50103 | excitatory amino acid agonist |
Drug Use | Suggest Off label Use Form| |View source of the data|
None
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 1.88 | acidic |
| pKa2 | 4.44 | acidic |
| pKa3 | 9.94 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Adenosine receptor A3 | GPCR | IC50 | 7.11 | CHEMBL | |||||
| Glutamate receptor 1 | Ion channel | Ki | 5.13 | CHEMBL | |||||
| Glutamate receptor ionotropic, kainate 1 | Ion channel | Ki | 6.75 | CHEMBL | |||||
| Glutamate receptor 2 | Ion channel | Ki | 4.91 | CHEMBL | |||||
| Glutamate receptor ionotropic, kainate 5 | Ion channel | Ki | 8.10 | CHEMBL | |||||
| Glutamate receptor 4 | Ion channel | Ki | 5.77 | CHEMBL | |||||
| Glutamate receptor ionotropic, kainate 2 | Ion channel | Ki | 7.49 | CHEMBL | |||||
| Glutamate receptor ionotropic, kainate 3 | Ion channel | Ki | 8 | CHEMBL | |||||
| Glutamate receptor 3 | Ion channel | Ki | 5.58 | PDSP | |||||
| Glutamate receptor ionotropic, kainate 4 | Ion channel | Ki | 8.64 | PDSP | |||||
| Glutamate receptor 2 | Ion channel | Ki | 5.43 | CHEMBL | |||||
| Glutamate receptor ionotropic, kainate 2 | Ion channel | Ki | 8.43 | CHEMBL | |||||
| Glutamate receptor ionotropic, kainate 1 | Ion channel | Ki | 7.15 | CHEMBL | |||||
| Glutamate receptor 1 | Ion channel | Ki | 6.32 | CHEMBL | |||||
| Glutamate receptor 3 | Ion channel | Ki | 5.70 | CHEMBL | |||||
| Glutamate receptor 4 | Ion channel | Ki | 5.45 | CHEMBL | |||||
| Glutamate receptor ionotropic, kainate 4 | Ion channel | Ki | 8.33 | CHEMBL | |||||
| Glutamate receptor ionotropic, kainate 5 | Ion channel | Ki | 7.82 | CHEMBL | |||||
| Glutamate receptor ionotropic, kainate 3 | Ion channel | Ki | 8.42 | CHEMBL | |||||
| Glutamate receptor ionotropic, AMPA | Ion channel | Ki | 7.53 | CHEMBL | |||||
| Glutamate receptor ionotropic, kainate | Ion channel | IC50 | 8.37 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D02546 | KEGG_DRUG |
| C0022471 | UMLSCUI |
| CHEBI:31746 | CHEBI |
| CHEMBL275040 | ChEMBL_ID |
| D007608 | MESH_DESCRIPTOR_UI |
| 10255 | PUBCHEM_CID |
| 1509 | INN_ID |
| SIV03811UC | UNII |
| 006209 | NDDF |
| KAI | PDB_CHEM_ID |
| SIV03811UC | INXIGHT DRUGS |
Pharmaceutical products:
None