Target family: Voltage-gated calcium channels  (Ca<sub>V</sub>) (type: vgic)
Target: Ca<sub>v</sub>1.2

Ligand: amlodipine (Synthetic organic)
Interaction type: Gating inhibitor
Action: None
Ligand approved: yes
Approval source: FDA (1992), EMA (2007)
Primary target: no
Median affinity: 9.300000190734863 pIC50
Reference (Journal): The action of amlodipine on voltage-operated calcium channels in vascular smooth muscle.
Published in: Br J Pharmacol

Ligand: BAYK 8644 (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: no
Median affinity:  -
Reference (Journal): Calcium currents recorded from a neuronal alpha 1C L-type calcium channel in Xenopus oocytes.
Published in: FEBS Lett

Ligand: benidipine (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: yes
Primary target: no
Median affinity: 5.309999942779541 pIC50
Reference (Journal): Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment.
Published in: J Appl Toxicol

Ligand: calciseptine (Peptide)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Calciseptine, a peptide isolated from black mamba venom, is a specific blocker of the L-type calcium channel.
Published in: Proc Natl Acad Sci U S A

Ligand: calciseptine (Peptide)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Evidence for a selective blockade of Cav1.2 versus Cav1.3 by the mamba toxin calciseptine in the mouse heart
Published in: Archives of Cardiovascular Diseases Supplements

Ligand: calciseptine (Peptide)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Smooth muscle relaxing and hypotensive activities of synthetic calciseptine and the homologous snake venom peptide FS2.
Published in: Jpn J Pharmacol

Ligand: Cd2+ (Inorganic)
Interaction type: Channel blocker
Action: None
Primary target: no
Median affinity:  pIC50
Reference (Journal): Inhibition by external Cd2+ of Na/Ca exchange and L-type Ca channel in rabbit ventricular myocytes.
Published in: Am J Physiol

Ligand: (-)-devapamil (Synthetic organic)
Interaction type: Gating inhibitor
Action: Antagonist
Ligand approved: no
Median affinity: 7.3 pIC50
Reference (Journal): Molecular determinants of high affinity phenylalkylamine block of L-type calcium channels.
Published in: J Biol Chem

Ligand: (-)-devapamil (Synthetic organic)
Interaction type: Gating inhibitor
Action: Antagonist
Ligand approved: no
Median affinity: 7.3 pIC50
Reference (Journal): Distinct effects of mutations in transmembrane segment IVS6 on block of L-type calcium channels by structurally similar phenylalkylamines.
Published in: Mol Pharmacol

Ligand: diltiazem (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1982)
Primary target: no
Median affinity: 6.300000190734863 pIC50
Reference (Journal): Effects of diltiazem on transmembrane potential and current of right ventricular papillary muscle of ferrets.
Published in: J Pharmacol Exp Ther

Ligand: FPL64176 (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): The calcium channel ligand FPL 64176 enhances L-type but inhibits N-type neuronal calcium currents.
Published in: Neuropharmacology

Ligand: FPL64176 (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Ca²⁺ channel activators reveal differential L-type Ca²⁺ channel pharmacology between native and stem cell-derived cardiomyocytes.
Published in: J Pharmacol Exp Ther

Ligand: (-)-(R)-efonidipine (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Identification of R(-)-isomer of efonidipine as a selective blocker of T-type Ca2+ channels.
Published in: Br J Pharmacol

Ligand: isradipine (Synthetic organic)
Interaction type: Gating inhibitor
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1990)
Primary target: no
Median affinity: 8.800000190734863 pIC50
Reference (Journal): Lower Affinity of Isradipine for L-Type Ca<sup>2+</sup> Channels during Substantia Nigra Dopamine Neuron-Like Activity: Implications for Neuroprotection in Parkinson's Disease.
Published in: J Neurosci

Ligand: isradipine (Synthetic organic)
Interaction type: Gating inhibitor
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1990)
Primary target: no
Median affinity: 8.5 pIC50
Reference (Journal): Lower Affinity of Isradipine for L-Type Ca<sup>2+</sup> Channels during Substantia Nigra Dopamine Neuron-Like Activity: Implications for Neuroprotection in Parkinson's Disease.
Published in: J Neurosci

Ligand: isradipine (Synthetic organic)
Interaction type: Gating inhibitor
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1990)
Primary target: no
Median affinity: 7.5 pIC50
Reference (Journal): Isoform-specific regulation of mood behavior and pancreatic beta cell and cardiovascular function by L-type Ca 2+ channels.
Published in: J Clin Invest

Ligand: mibefradil (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1997)
Median affinity: 4.9 pIC50
Reference (Journal): Mibefradil block of cloned T-type calcium channels.
Published in: J Pharmacol Exp Ther

Ligand: nifedipine (Synthetic organic)
Interaction type: Gating inhibitor
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1981)
Primary target: no
Median affinity:  pIC50
Reference (Journal): Vascular selectivity of seven prototype calcium antagonists: a study at the single cell level.
Published in: J Cardiovasc Pharmacol

Ligand: nifedipine (Synthetic organic)
Interaction type: Gating inhibitor
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1981)
Primary target: no
Median affinity:  pIC50
Reference (Journal): Characterization of nifedipine-resistant calcium current in neonatal rat ventricular cardiomyocytes.
Published in: Am J Physiol Heart Circ Physiol

Ligand: nimodipine (Synthetic organic)
Interaction type: Gating inhibitor
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1988)
Primary target: no
Median affinity: 6.800000190734863 pIC50
Reference (Journal): Neuronal Ca(V)1.3alpha(1) L-type channels activate at relatively hyperpolarized membrane potentials and are incompletely inhibited by dihydropyridines.
Published in: J Neurosci

Ligand: nisoldipine (Synthetic organic)
Interaction type: Gating inhibitor
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1995)
Primary target: no
Median affinity:  pIC50
Reference (Journal): Functional embryonic cardiomyocytes after disruption of the L-type alpha1C (Cav1.2) calcium channel gene in the mouse.
Published in: J Biol Chem

Ligand: nisoldipine (Synthetic organic)
Interaction type: Gating inhibitor
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1995)
Primary target: no
Median affinity: 7.099999904632568 pIC50
Reference (Journal): Ca(V)1.2 calcium channel dysfunction causes a multisystem disorder including arrhythmia and autism.
Published in: Cell

Ligand: nitrendipine (Synthetic organic)
Interaction type: Gating inhibitor
Action: Antagonist
Ligand approved: yes
Primary target: no
Median affinity: 9.399999618530273 pIC50
Reference (Journal): Nitrendipine block of cardiac calcium channels: high-affinity binding to the inactivated state.
Published in: Proc Natl Acad Sci USA

Ligand: Pb2+ (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Median affinity: 6.4 pIC50
Reference (Journal): Characteristics of block by Pb2+ of function of human neuronal L-, N-, and R-type Ca2+ channels transiently expressed in human embryonic kidney 293 cells.
Published in: Mol Pharmacol

Ligand: (-)-(S)-BayK8644 (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity: 7.760000228881836 pEC50

Ligand: [3H](-)devapamil (Synthetic organic)
Interaction type: Gating inhibitor
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Pharmacological, radioligand binding, and electrophysiological characteristics of FPL 64176, a novel nondihydropyridine Ca2+ channel activator, in cardiac and vascular preparations.
Published in: Mol Pharmacol

Ligand: [3H](-)devapamil (Synthetic organic)
Interaction type: Gating inhibitor
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): SR 33557, a novel calcium entry blocker. II. Interactions with 1,4-dihydropyridine, phenylalkylamine and benzothiazepine binding sites in rat heart sarcolemmal membranes.
Published in: J Pharmacol Exp Ther

Ligand: [3H](+)-cis-diltiazem (Synthetic organic)
Interaction type: Gating inhibitor
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.199999809265137 pKd
Reference (Journal): SR 33557, a novel calcium entry blocker. II. Interactions with 1,4-dihydropyridine, phenylalkylamine and benzothiazepine binding sites in rat heart sarcolemmal membranes.
Published in: J Pharmacol Exp Ther

Ligand: [3H](+)-isradipine (Synthetic organic)
Interaction type: Gating inhibitor
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 10.100000381469727 pKd
Reference (Journal): Isoform-specific regulation of mood behavior and pancreatic beta cell and cardiovascular function by L-type Ca 2+ channels.
Published in: J Clin Invest

Ligand: [3H](+)-isradipine (Synthetic organic)
Interaction type: Gating inhibitor
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Regional expression and functional characterization of the L-type Ca2+-channel in myocardium from patients with end-stage heart failure and in non-failing human hearts.
Published in: J Mol Cell Cardiol

Ligand: SZ(+)-(S)-202-791 (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: verapamil (Synthetic organic)
Interaction type: Gating inhibitor
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1981)
Primary target: no
Median affinity:  pIC50
Reference (Journal): Distinct effects of mutations in transmembrane segment IVS6 on block of L-type calcium channels by structurally similar phenylalkylamines.
Published in: Mol Pharmacol

Ligand: verapamil (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1981)
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Distinct effects of mutations in transmembrane segment IVS6 on block of L-type calcium channels by structurally similar phenylalkylamines.
Published in: Mol Pharmacol