Natural/Endogenous Targets
Target 5-HT3A CaCC CaS receptor Cx23 Cx25 Cx26 Cx30 Cx30.2 Cx30.3 Cx31 Cx31.1 Cx31.9 Cx32 Cx36 Cx37 Cx40 Cx40.1 Cx43 Cx45 Cx46 Cx47 Cx50 Cx59 Cx62 IP3R1 IP3R2 IP3R3

Cofactor in Enzyme Reactions
Enzyme Reference thyroid peroxidase

Selectivity at GPCRs
Key to terms and symbols		Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference CaS receptor Mm Agonist Full agonist 2.5 pKd - 35 ⤷ pKd 2.5 [35] CaS receptor Rn Agonist Full agonist 2.5 pKd - 36 ⤷ pKd 2.5 [36] CaS receptor Hs Agonist Full agonist 2.4 pKd - 28 ⤷ pKd 2.4 [28]

Selectivity at ion channels
Key to terms and symbols		Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference 5-HT3A Hs Allosteric modulator Negative - - 1x10-4 - 1x10-2 3,27 ⤷ Conc range: 1x10-4 - 1x10-2 M Decreased single channel conductance, increased channel activation rate, increased deactivation rate, increased desensitization rate, decrease in agonist apparent affinity. [3,27] 5-HT3A Mm Allosteric modulator Negative - - 1x10-4 - 1x10-2 9,16,29 ⤷ Conc range: 1x10-4 - 1x10-2 M Decreased single channel conductance, increased channel activation rate, increased deactivation rate, increased desensitization rate, decrease in agonist apparent affinity. [9,16,29] TRPP2 Hs Activator (Intracellular Ca2+) Agonist - - 5x10-3 5 ⤷ Conc range: 5x10-3 M [5] Voltage: -150.0 – 100.0 mV Conc range: 5x10-3 M [5] Voltage: -60.0 – -50.0 mV IP3R1 Hs Activator (cytosolic Ca2+) - - - < 7.5x10-4 ⤷ Conc range: < 7.5x10-4 M RyR1 Hs Antagonist (cytosolic Ca2+) Antagonist - - > 1x10-4 ⤷ Conc range: > 1x10-4 M KNa1.1 Rn Gating inhibitor Antagonist - - 0x100 - 3x10-6 20 ⤷ Conc range: 0x100 - 3x10-6 M [20] KCa3.1 Hs Activator Agonist 6.1 – 7.0 pEC50 - 10,17,21,26,37 ⤷ pEC50 6.1 – 7.0 [10,17,21,26,37] Voltage: -120.0 – 60.0 mV KCa2.1 Hs Activator Agonist 6.2 – 6.5 pEC50 - 22,43 ⤷ pEC50 6.2 – 6.5 (EC50 6x10-7 – 3x10-7 M) [22,43] Voltage: -80.0 mV KCa2.2 Hs Activator Agonist 6.2 – 6.5 pEC50 - 7,34,43 ⤷ pEC50 6.2 – 6.5 [7,34,43] KCa2.2 Rn Activator Agonist 6.1 – 6.4 pEC50 - 13,22 ⤷ pEC50 6.1 – 6.4 [13,22] KCa2.3 Hs Activator Agonist 6.0 – 6.5 pEC50 - 15,42-43 ⤷ pEC50 6.0 – 6.5 [15,42-43] KCa2.3 Rn Activator Agonist 6.2 pEC50 - 1 ⤷ pEC50 6.2 [1] TRPC5 Hs Activator (intracellular Ca2+) - 6.2 pEC50 - ⤷ pEC50 6.2 (EC50 6.35x10-7 M) at negative potentials TRPC5 Mm Activator Activation 6.0 pEC50 - 2,11 ⤷ pEC50 6.0 Internal calcium [2,11] TRPP1 Hs Activator (Intracellular Ca2+) - 6.0 pEC50 1x10-7 - 1x10-3 23 ⤷ pEC50 6.0 Conc range: 1x10-7 - 1x10-3 M [23] Voltage: -5.0 mV TRPM5 Mm Activator (intracellular Ca2+) Agonist 4.5 – 6.2 pEC50 - 14,25,41 ⤷ pEC50 4.5 – 6.2 (EC50 3x10-5 – 7x10-7 M) [14,25,41] Voltage: -80.0 – 80.0 mV TRPM4 Hs Activator (intracellular Ca2+) Agonist 3.9 – 6.3 pEC50 - 30-32,38 ⤷ pEC50 3.9 – 6.3 (EC50 1.4x10-4 – 5x10-7 M) [30-32,38] Voltage: -100.0 – 100.0 mV KNa1.1 Mm Gating inhibitor Antagonist 6.5 pIC50 - 33 ⤷ pIC50 6.5 [33] TRPM6 Hs Channel blocker - 5.3 – 5.3 pIC50 - ⤷ pIC50 5.3 – 5.3 (IC50 5.4x10-6 – 4.8x10-6 M) inward current mediated by monovalent cations is blocked ZAC Hs Antagonist Antagonist 2.0 pIC50 - 40 ⤷ pIC50 2.0 [40] TRPC2 N/A Activator (Intracellular Ca2+) - - - - ⤷ TRPM2 Hs Activator (intracellular Ca2+) - - - - ⤷ perhaps via calmodulin CaCC Hs Activator (intracellular Ca2+) - - - - ⤷ Cx23 Hs Inhibitor (extracellular Ca2+) - - - - ⤷ blocked by raising external Ca2+ Cx25 Hs Inhibitor (extracellular Ca2+) - - - - ⤷ blocked by raising external Ca2+ Cx26 Hs Inhibitor (extracellular Ca2+) - - - - ⤷ blocked by raising external Ca2+ Cx30 Hs Inhibitor (extracellular Ca2+) - - - - ⤷ blocked by raising external Ca2+ Cx30.2 Hs Inhibitor (extracellular Ca2+) - - - - ⤷ blocked by raising external Ca2+ Cx30.3 Hs Inhibitor (extracellular Ca2+) - - - - ⤷ blocked by raising external Ca2+ Cx31 Hs Inhibitor (extracellular Ca2+) - - - - ⤷ blocked by raising external Ca2+ Cx31.1 Hs Inhibitor (extracellular Ca2+) - - - - ⤷ blocked by raising external Ca2+ Cx31.9 Hs Inhibitor (extracellular Ca2+) - - - - ⤷ blocked by raising external Ca2+ Cx32 Hs Inhibitor (extracellular Ca2+) - - - - ⤷ blocked by raising external Ca2+ Cx36 Hs Inhibitor (extracellular Ca2+) - - - - ⤷ blocked by raising external Ca2+ Cx37 Hs Inhibitor (extracellular Ca2+) - - - - ⤷ blocked by raising external Ca2+ Cx40 Hs Inhibitor (extracellular Ca2+) - - - - ⤷ blocked by raising external Ca2+ Cx40.1 Hs Inhibitor (extracellular Ca2+) - - - - ⤷ blocked by raising external Ca2+ Cx43 Hs Inhibitor (extracellular Ca2+) - - - - ⤷ blocked by raising external Ca2+ Cx45 Hs Inhibitor (extracellular Ca2+) - - - - ⤷ blocked by raising external Ca2+ Cx46 Hs Inhibitor (extracellular Ca2+) - - - - ⤷ blocked by raising external Ca2+ Cx47 Hs Inhibitor (extracellular Ca2+) - - - - ⤷ blocked by raising external Ca2+ Cx50 Hs Inhibitor (extracellular Ca2+) - - - - ⤷ blocked by raising external Ca2+ Cx59 Hs Inhibitor (extracellular Ca2+) - - - - ⤷ blocked by raising external Ca2+ Cx62 Hs Inhibitor (extracellular Ca2+) - - - - ⤷ blocked by raising external Ca2+ IP3R2 Hs Activator (cytosolic Ca2+) - - - - ⤷ nM range IP3R3 Hs Activator (cytosolic Ca2+) - - - - ⤷ nM range RyR1 Hs Activator (luminal Ca2+) - - - - ⤷ endogenous endogenous; μM range

Additional information and targets (data relate to human unless otherwise stated)
Description	Data	Reference
Cation rank order of potency at CaS receptor	Gd3+ > Ca2+ > Mg2+	4
Endogenous inhibitors at adenylyl cyclase 6	Gαi, Ca2+, PKA-evoked phosphorylation, PKC-evoked phosphorylation, NO	6,12,24,39,44
Endogenous inhibitors at adenylyl cyclase 5	Gαi, Ca2+, PKA-evoked phosphorylation, Gβγ, NO	8,12,18-19,39

Ligand mentioned in the following text fields
Alpha subfamily overview
Glycine receptors overview
Protein kinase C (PKC) family overview
GABAB receptors comments
Glycine receptors comments