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Compound Detail

CHEMBL1480

FELODIPINE
💊 Approved Drug
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💊 Approved Drug
CCOC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1c1cccc(Cl)c1Cl
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL1480
Name FELODIPINE
Phase Approved
Structure Type MOL
InChI Key RZTAMFZIAATZDJ-UHFFFAOYSA-N
Therapeutic ✓ Yes

Known Names

C08CA02 Cabren Cardioplen xl Felodipine Felodipine component of lexxel Felodipino Felogen xl Felotens xl Folpik xl H 154/82 H-154/82 Keloc sr +7 more
12
Targets
25
Activities
3
Assay Types
30
PK Parameters
20
Publications
19
Known Names
7
Indications
2
Mechanisms

Molecular Properties

384.3
MW (Da)
3.96
ALogP
5
HBA
1
HBD
64.6
PSA (Ų)
0.80
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
First Approval 1991
Availability Prescription
Chirality Racemic

Routes of Administration

Oral

Flags

Natural Product
USAN Stem -dipine; -pine
USAN Year 1985

Extended Properties

Molecular Formula C18H19Cl2NO4
MW 384.26
Aromatic Rings 1
Heavy Atoms 25
NP-Likeness -0.81

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Mineralocorticoid receptor antagonist ANTAGONIST Mineralocorticoid receptor ✓ ✓
Voltage-gated L-type calcium channel blocker BLOCKER Voltage-gated L-type calcium channel ✓ ✓

Indications

Cardiovascular Diseases Diabetes Mellitus Hypertension Atherosclerosis Coronary Disease Diabetes Mellitus, Type 2 Hypercholesterolemia

ATC Classification

C08CA02
felodipine
Level 1: CARDIOVASCULAR SYSTEM
Level 2: CALCIUM CHANNEL BLOCKERS

Activity Summary

IC50 18 meas. best 10.09
EC50 4 meas. best 5.72
Ki 3 meas. best 10.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
 Ki 10.28 8.99 0.1 2
Unchecked
CHEMBL612545
 IC50 10.09 8.865 0.1 2
Cavia porcellus
CHEMBL369
 IC50 8.84 8.84 1.4 1
Adenosine receptor A3
CHEMBL256
 Ki 6.22 6.22 597.0 1
Adenosine receptor A3
CHEMBL256
 IC50 5.98 5.98 1057.0 1
Nuclear receptor subfamily 1 group I member 2
CHEMBL3401
 EC50 5.72 5.4267 1900.0 3
Cytochrome P450 2C9
CHEMBL3397
 IC50 5.34 5.34 4579.5 1
Bile acid receptor
CHEMBL2047
 IC50 5.3 5.3 4960.0 1
Plasmodium falciparum
CHEMBL364
 IC50 5.1 4.9286 7943.3 7
Danio rerio
CHEMBL613963
 IC50 5.04 5.04 9210.0 1
Nuclear receptor subfamily 1 group I member 2
CHEMBL2146315
 EC50 4.63 4.63 23400.0 1
ATP-dependent translocase ABCB1
CHEMBL4302
 IC50 4.58 4.535 26300.0 2
Sodium channel alpha subunits; brain (Types I, II, III)
CHEMBL2096682
 IC50 4.43 4.43 37000.0 1
Bile salt export pump
CHEMBL6020
 IC50 4.16 4.16 69700.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 41.12 ng.hr.mL-1 Homo sapiens
CL 38.0 mL.min-1.kg-1 Canis lupus familiaris
CL 39.0 mL.min-1.kg-1 Canis lupus familiaris
CL 11.8 mL.min-1.kg-1 -
CL 83.3 mL.min-1.kg-1 Rattus norvegicus
CL 19.5 mL.min-1.kg-1 Canis lupus familiaris
CL 11.0 mL.min-1.kg-1 Homo sapiens
CL 38.0 mL.min-1.kg-1 Canis lupus familiaris
CL 11.0 mL.min-1.kg-1 Homo sapiens
CL 11.0 mL.min-1.kg-1 Homo sapiens
CL 11.0 mL.min-1.kg-1 Homo sapiens
CL 84.7 mL.min-1.kg-1 Rattus norvegicus
CL 11.0 mL.min-1.kg-1 Homo sapiens
CL 11.1 mL.min-1.kg-1 Homo sapiens
CL 15.7 mL.min-1.kg-1 Macaca
CL 19.5 mL.min-1.kg-1 Canis lupus familiaris
CL 145.7 mL.min-1.g-1 Homo sapiens
CL 0.8 L/min Homo sapiens
Cmax 7.0 nM Homo sapiens
Cmax 23.0 nM Homo sapiens
Cmax 20.0 nM Homo sapiens
Cmin ss 2.0 nmol/L Homo sapiens
Cmin ss 7.0 nmol/L Homo sapiens
Cmin ss 0.5 nmol/L Homo sapiens
F 20.0 % Homo sapiens
F 5.0 % Homo sapiens
Fu 0.004 - -
Fu 0.0001 - -
Fu 0.004 - Homo sapiens
Fu 0.0036 - Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked Ki = 0.053 nM 10.28 DRUGMATRIX: Calcium Channel Type L, Dihydropyridine radioligand binding (ligand:... -
Unchecked IC50 = 0.082 nM 10.09 DRUGMATRIX: Calcium Channel Type L, Dihydropyridine radioligand binding (ligand:... -
Cavia porcellus IC50 = 1.45 nM 8.84 Calcium channel antagonist activity against carbachol-induced contractile respon... 8917646
Unchecked Ki = 20.0 nM 7.7 DRUGMATRIX: Calcium Channel Type L, Benzothiazepine radioligand binding (ligand:... -
Unchecked IC50 = 23.0 nM 7.64 DRUGMATRIX: Calcium Channel Type L, Benzothiazepine radioligand binding (ligand:... -
Adenosine receptor A3 Ki = 597.0 nM 6.22 DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) -
Adenosine receptor A3 IC50 = 1057.0 nM 5.98 DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) -
Nuclear receptor subfamily 1 group I member 2 EC50 = 1900.0 nM 5.72 Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induc... 20966043
Nuclear receptor subfamily 1 group I member 2 EC50 = 3900.0 nM 5.41 Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by l... 20966043
Cytochrome P450 2C9 IC50 = 4579.5 nM 5.34 DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) -
Bile acid receptor IC50 = 4960.0 nM 5.3 Antagonist activity at human GTS-tagged FXR after 20 mins by TR-FRET assay 23688559
Nuclear receptor subfamily 1 group I member 2 EC50 = 7100.0 nM 5.15 Competitive binding affinity to human PXR LBD (111 to 434) by TR-FRET assay 20966043
Plasmodium falciparum IC50 = 7943.28 nM 5.1 Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR gr... 19734910
Danio rerio IC50 = 9210.0 nM 5.04 PUBCHEM_BIOASSAY: In Vivo Angiogenesis Dose-Response Confirmation. (Class of ass... -
Plasmodium falciparum IC50 = 10000.0 nM 5.0 Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR g... 19734910
Plasmodium falciparum IC50 = 12589.25 nM 4.9 Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR g... 19734910
Plasmodium falciparum IC50 = 12589.25 nM 4.9 Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR g... 19734910
Plasmodium falciparum IC50 = 12589.25 nM 4.9 Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR g... 19734910
Plasmodium falciparum IC50 = 12589.25 nM 4.9 Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR g... 19734910
Plasmodium falciparum IC50 = 15848.93 nM 4.8 Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR g... 19734910

Literature References

PubMed DOI Target Context # Activities
16472241 10.2174/1570163043334794 Hepatotoxicity 18
22194678 10.1371/journal.pcbi.1002310 Hepatotoxicity 14
15646539 10.1016/s0399-8320(04)95062-2 Unchecked 11
20070106 10.1021/jm901371v Homo sapiens 8
8917646 10.1021/jm960531r Mus musculus 8
20966043 10.1124/dmd.110.035105 Nuclear receptor subfamily 1 group I member 2 8
15646539 10.1016/s0399-8320(04)95062-2 NON-PROTEIN TARGET 8
16621936 10.1124/dmd.105.006619 ADMET 8
19734910 10.1038/nchembio.215 Plasmodium falciparum 7
12061889 10.1021/jm0200409 ADMET 5
37468498 10.1038/s41467-023-40064-9 Alpha-1A adrenergic receptor 4
18426954 10.1124/dmd.108.020479 ADMET 4
11716514 10.1006/bbrc.2001.6000 ATP-dependent translocase ABCB1 3
2153819 10.1021/jm00164a019 Canis familiaris 3
37468498 10.1038/s41467-023-40064-9 Alpha-2A adrenergic receptor 3
20014752 10.1021/tx900326k Hepatotoxicity 3
11311053 10.1021/jm000407e ADMET 3
37468498 10.1038/s41467-023-40064-9 5-hydroxytryptamine receptor 2B 3
1992115 10.1021/jm00105a004 Canis familiaris 3
2943898 10.1021/jm00159a022 Canis familiaris 3

Data from ChEMBL 36 via Core Engine