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Compound Detail

CHEMBL1275868

AZELNIDIPINE
🧪 Phase III
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🧪 Phase III
CC1=C(C(=O)OC(C)C)C(c2cccc([N+](=O)[O-])c2)C(C(=O)OC2CN(C(c3ccccc3)c3ccccc3)C2)=C(N)N1

Basic Information

ChEMBL ID CHEMBL1275868
Name AZELNIDIPINE
Phase Phase III
Structure Type MOL
InChI Key ZKFQEACEUNWPMT-UHFFFAOYSA-N

Known Names

Azelnidipine Azelnidipino Calblock CS-905 CS905
7
Targets
10
Activities
1
Assay Types
1
PK Parameters
20
Publications
5
Known Names
1
Mechanisms

Molecular Properties

582.7
MW (Da)
4.69
ALogP
9
HBA
2
HBD
137.0
PSA (Ų)
0.21
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Racemic

Flags

Natural Product
USAN Stem -dipine; -pine

Extended Properties

Molecular Formula C33H34N4O6
MW 582.66
Aromatic Rings 3
Heavy Atoms 43
NP-Likeness -0.70

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Voltage-gated L-type calcium channel blocker BLOCKER Voltage-gated L-type calcium channel

Activity Summary

IC50 10 meas. best 5.91

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 5.91 5.345 1234.0 4
Trypanosoma cruzi
CHEMBL368
IC50 5.54 5.54 2900.0 1
Leishmania braziliensis
CHEMBL612878
IC50 4.86 4.86 13670.0 1
Leishmania major
CHEMBL612879
IC50 4.77 4.77 17060.0 1
Leishmania amazonensis
CHEMBL612877
IC50 4.69 4.69 20540.0 1
Leishmania chagasi
CHEMBL612790
IC50 4.48 4.48 33390.0 1
LLC-MK2
CHEMBL614691
IC50 4.47 4.47 33480.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 33.9 mL.min-1.g-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
37468498 10.1038/s41467-023-40064-9 Gamma-aminobutyric acid receptor subunit alpha-1 2
37468498 10.1038/s41467-023-40064-9 Nuclear receptor subfamily 1 group I member 2 2
37468498 10.1038/s41467-023-40064-9 5-hydroxytryptamine receptor 2A 2
37468498 10.1038/s41467-023-40064-9 Cannabinoid receptor 1 2
37468498 10.1038/s41467-023-40064-9 Alpha-2A adrenergic receptor 2
20934347 10.1016/j.bmc.2010.09.015 Unchecked 2
37468498 10.1038/s41467-023-40064-9 Androgen receptor 2
37468498 10.1038/s41467-023-40064-9 Muscarinic acetylcholine receptor M2 2
37468498 10.1038/s41467-023-40064-9 Alpha-1A adrenergic receptor 2
20934347 10.1016/j.bmc.2010.09.015 Leishmania chagasi 2
37468498 10.1038/s41467-023-40064-9 Progesterone receptor 2
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
37468498 10.1038/s41467-023-40064-9 5-hydroxytryptamine receptor 2B 2
- 10.1101/2020.04.21.054387 SARS-CoV-2 1
- 10.6019/CHEMBL4495564 Replicase polyprotein 1ab 1
22197392 10.1016/j.bmcl.2011.12.005 Liver microsomes 1
20934347 10.1016/j.bmc.2010.09.015 ADMET 1
20934347 10.1016/j.bmc.2010.09.015 Trypanosoma cruzi 1
20934347 10.1016/j.bmc.2010.09.015 Leishmania major 1

Data from ChEMBL 36 via Core Engine