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Compound Detail

CHEMBL1237132

CLEVIDIPINE
💊 Approved Drug
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💊 Approved Drug
CCCC(=O)OCOC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1c1cccc(Cl)c1Cl
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL1237132
Name CLEVIDIPINE
Phase Approved
Structure Type MOL
InChI Key KPBZROQVTHLCDU-UHFFFAOYSA-N
Therapeutic ✓ Yes

Known Names

Clevidepine Clevidepine butyrate Clevidipine Clevidipino Cleviprex H-324/38 H324/38
2
Targets
3
Activities
1
Assay Types
4
PK Parameters
11
Publications
7
Known Names
6
Indications
1
Mechanisms

Molecular Properties

456.3
MW (Da)
4.25
ALogP
7
HBA
1
HBD
90.9
PSA (Ų)
0.48
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
First Approval 2008
Availability Prescription
Chirality Racemic

Routes of Administration

Parenteral

Flags

Natural Product
USAN Stem -dipine; -pine
USAN Year 2009

Extended Properties

Molecular Formula C21H23Cl2NO6
MW 456.32
Aromatic Rings 1
Heavy Atoms 30
NP-Likeness -0.42

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 Hypertension, Malignant Stroke Scoliosis Vascular Diseases

ATC Classification

C08CA16
clevidipine
Level 1: CARDIOVASCULAR SYSTEM
Level 2: CALCIUM CHANNEL BLOCKERS

Activity Summary

IC50 3 meas. best 8.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Voltage-dependent L-type calcium channel subunit alpha-1C
CHEMBL2366456
 IC50 8.15 7.625 7.1 2
Bile salt export pump
CHEMBL6020
 IC50 4.44 4.44 36350.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 142.0 mL.min-1.kg-1 Homo sapiens
Fu 0.0038 - Homo sapiens
MRT 0.07 hr Homo sapiens
T1/2 0.3 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Voltage-dependent L-type calcium channel subunit alpha-1C IC50 = 7.1 nM 8.15 Inhibition of L-type calcium channel measured using whole-cell patch clamp in gu... 22761000
Voltage-dependent L-type calcium channel subunit alpha-1C IC50 = 78.8 nM 7.1 Inhibition of L-type calcium channel measured using whole-cell patch clamp in gu... 22761000
Bile salt export pump IC50 = 36350.0 nM 4.44 Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21... 22961681

Literature References

PubMed DOI Target Context # Activities
18426954 10.1124/dmd.108.020479 ADMET 4
- 10.6019/CHEMBL4495565 SARS-CoV-2 4
22761000 10.1002/jat.2784 Voltage-dependent L-type calcium channel subunit alpha-1C 2
26948801 10.1016/j.drudis.2016.02.015 Homo sapiens 2
- 10.6019/CHEMBL4495564 Replicase polyprotein 1ab 2
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
18426954 10.1124/dmd.108.020479 NON-PROTEIN TARGET 1
22961681 10.1124/dmd.112.047068 Bile salt export pump 1
- 10.1101/2020.04.03.023846 SARS-CoV-2 1
- 10.21203/rs.3.rs-23951/v1 SARS-CoV-2 1
- 10.1101/2020.04.21.054387 SARS-CoV-2 1

Data from ChEMBL 36 via Core Engine