Target family: CatSper and Two-Pore channels (TPC) (type: vgic)
Target: CatSper1

Ligand: Cd2+ (Inorganic)
Interaction type: Channel blocker
Action: Inhibition
Primary target: no
Median affinity: 3.700000047683716 pIC50
Reference (Journal): Whole-cell patch-clamp measurements of spermatozoa reveal an alkaline-activated Ca2+ channel.
Published in: Nature

Ligand: HC-056456 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 4.699999809265137 pIC50
Reference (Journal): Pharmacological targeting of native CatSper channels reveals a required role in maintenance of sperm hyperactivation.
Published in: PLoS ONE

Ligand: mibefradil (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1997)
Primary target: no
Median affinity:  pIC50
Reference (Journal): The CatSper channel mediates progesterone-induced Ca2+ influx in human sperm.
Published in: Nature

Ligand: Ni2+ (Inorganic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 3.5 pIC50
Reference (Journal): Whole-cell patch-clamp measurements of spermatozoa reveal an alkaline-activated Ca2+ channel.
Published in: Nature

Ligand: NNC55-0396 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Median affinity: 5.6 pIC50
Reference (Journal): Progesterone activates the principal Ca2+ channel of human sperm.
Published in: Nature

Ligand: NNC55-0396 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.699999809265137 pIC50
Reference (Journal): Progesterone activates the principal Ca2+ channel of human sperm.
Published in: Nature

Ligand: NNC55-0396 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.699999809265137 pIC50
Reference (Journal): The CatSper channel mediates progesterone-induced Ca2+ influx in human sperm.
Published in: Nature

Ligand: PGE1 (Metabolite)
Interaction type: Activator
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1981)
Median affinity: 6.3 pEC50
Reference (Journal): Progesterone activates the principal Ca2+ channel of human sperm.
Published in: Nature

Ligand: PGE2 (Metabolite)
Interaction type: Activator
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1977)
Median affinity: 6.3 pEC50
Reference (Journal): Progesterone activates the principal Ca2+ channel of human sperm.
Published in: Nature

Ligand: PGF1α (Metabolite)
Interaction type: Activator
Action: Full agonist
Ligand approved: no
Median affinity: 6.3 pEC50
Reference (Journal): Progesterone activates the principal Ca2+ channel of human sperm.
Published in: Nature

Ligand: progesterone (Metabolite)
Interaction type: Activator
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1959)
Primary target: no
Median affinity:  pEC50
Reference (Journal): Progesterone activates the principal Ca2+ channel of human sperm.
Published in: Nature

Ligand: progesterone (Metabolite)
Interaction type: Activator
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1959)
Primary target: no
Median affinity:  pEC50
Reference (Journal): The CatSper channel mediates progesterone-induced Ca2+ influx in human sperm.
Published in: Nature

Ligand: ruthenium red (Inorganic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5 pIC50
Reference (Journal): Whole-cell patch-clamp measurements of spermatozoa reveal an alkaline-activated Ca2+ channel.
Published in: Nature