nifedipine

Ligand id: 2514

Name: nifedipine

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View more information in the IUPHAR Pharmacology Education Project: nifedipine

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 5
Hydrogen bond donors 1
Rotatable bonds 6
Topological polar surface area 107.77
Molecular weight 346.12
XLogP 3.91
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

View interactive charts of activity data from GtoPdb and ChEMBL (where available) across species

Selectivity at ion channels
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Affinity Units Concentration range (M) Reference
Kv1.2 Rn Channel blocker Pore blocker 4.7 pKd - 2
pKd 4.7 (Kd 1.8x10-5 M) [2]
Kv1.5 Hs Channel blocker - 4.1 pKd - 2
pKd 4.1 [2]
Cav1.2 Rn Gating inhibitor Antagonist 7.7 pIC50 - 6-7
pIC50 7.7 There was a 100-fold difference for nifedipine on smooth (pIC50 8.5) versus cardiac (pIC50 6.5) cells in vitro (Perez-Vizcaino et al. 1993). [6-7]
Voltage: -80.0 mV
Cav1.3 Hs Gating inhibitor Antagonist 7.7 pIC50 - 8
pIC50 7.7 (IC50 2.01x10-8 M) [8]
Description: Recombinant Cav1.3 calcium channel complexes expressed in tsA-cells
Cav1.1 Rn Gating inhibitor Antagonist 6.3 pIC50 1x10-7 - 1x10-4 4
pIC50 6.3 Conc range: 1x10-7 - 1x10-4 M [4]
Voltage: -90.0 mV
Cav1.4 Hs Gating inhibitor Antagonist 6.0 pIC50 - 5
pIC50 6.0 [5]
Voltage: -100.0 mV
glycine receptor α1 subunit Hs Antagonist Antagonist 5.5 pIC50 -
pIC50 5.5 (IC50 3.3x10-6 M)
glycine receptor β subunit Hs Antagonist Antagonist 4.9 – 5.9 pIC50 -
pIC50 5.9 (IC50 1.2x10-6 M) when co-expressed with the α1 subunit
pIC50 4.9 (IC50 1.14x10-5 M) when co-expressed with the α3 subunit
Kv1.7 Mm Channel blocker - 4.9 pIC50 - 3
pIC50 4.9 [3]
glycine receptor α3 subunit Hs Antagonist Antagonist 4.5 pIC50 -
pIC50 4.5 (IC50 2.92x10-5 M)
Kv1.1 Mm Channel blocker - 4.0 pIC50 - 2
pIC50 4.0 [2]
Kv3.1 Mm Channel blocker - 3.9 pIC50 - 2
pIC50 3.9 [2]
TRPM3 Hs Activator - - - -
Selectivity at nuclear hormone receptors
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Affinity Units Concentration range (M) Reference
Pregnane X receptor Hs Agonist Agonist - - - 1
[1]