Compound Detail
CHEMBL1648
ISRADIPINE 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL1648 |
| Name | ISRADIPINE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | HMJIYCCIJYRONP-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
11
Targets
11
Activities
2
Assay Types
7
PK Parameters
20
Publications
9
Known Names
8
Indications
1
Mechanisms
Molecular Properties
371.4
MW (Da)
2.58
ALogP
8
HBA
1
HBD
103.5
PSA (Ų)
0.82
QED
0
Ro5 Violations
4
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1990 |
| Availability | Prescription |
| Chirality | Racemic |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Voltage-gated L-type calcium channel blocker | BLOCKER | Voltage-gated L-type calcium channel | ✓ | ✓ |
Indications
Cardiovascular Diseases Hypertension Parkinson Disease Bipolar Disorder Opioid-Related Disorders Substance-Related Disorders Smoking Cessation Tobacco Use Disorder
ATC Classification
C08CA03
isradipine
Level 1: CARDIOVASCULAR SYSTEM
Level 2: CALCIUM CHANNEL BLOCKERS
Activity Summary
IC50 10 meas. best 8.66
EC50 1 meas. best 6.05
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Voltage-dependent L-type calcium channel subunit alpha-1C CHEMBL1940 | IC50 | 8.66 | 8.66 | 2.2 | 1 |
| Voltage-dependent L-type calcium channel subunit alpha-1C CHEMBL2830 | IC50 | 6.97 | 6.97 | 107.0 | 1 |
| Voltage-dependent L-type calcium channel subunit alpha-1D CHEMBL4132 | IC50 | 6.66 | 6.66 | 221.0 | 1 |
| Onchocerca gutturosa CHEMBL613143 | EC50 | 6.05 | 6.05 | 890.0 | 1 |
| Cytochrome P450 2C9 CHEMBL3397 | IC50 | 5.44 | 5.44 | 3660.0 | 1 |
| Cytochrome P450 2D6 CHEMBL289 | IC50 | 5.32 | 5.32 | 4790.0 | 1 |
| Cytochrome P450 2C8 CHEMBL3721 | IC50 | 5.3 | 5.3 | 5000.0 | 1 |
| Trypanosoma cruzi CHEMBL368 | IC50 | 4.68 | 4.68 | 20800.0 | 1 |
| Cytochrome P450 1A2 CHEMBL3356 | IC50 | 4.55 | 4.55 | 28300.0 | 1 |
| Bile salt export pump CHEMBL6020 | IC50 | 4.55 | 4.55 | 28000.0 | 1 |
| Voltage-gated inwardly rectifying potassium channel KCNH2 CHEMBL240 | IC50 | 4.3 | 4.3 | 50118.7 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 0.197 | uM.hr | Homo sapiens |
| CL | 26.0 | mL.min-1.kg-1 | Homo sapiens |
| CL | 26.0 | mL.min-1.kg-1 | Homo sapiens |
| CL | 300.0 | mL.min-1.g-1 | Homo sapiens |
| Fu | 0.04 | - | Homo sapiens |
| MRT | 1.0 | hr | Homo sapiens |
| T1/2 | 3.3 | hr | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine