Natural/Endogenous Targets
Target 5-HT3A CaS receptor VRAC

Cofactor in Enzyme Reactions
Enzyme Reference mevalonate kinase 6,12,22 phosphomevalonate kinase 4,11 diphosphomevalonate decarboxylase 15,28 geranylgeranyl diphosphate synthase 13,29,33 farnesyl diphosphate synthase 1,5,24 squalene synthase 25 isopentenyl-diphosphate Δ-isomerase 1 10 isopentenyl-diphosphate Δ-isomerase 2 10,34 sphingosine kinase 1 sphingosine kinase 2

Transporters Moving this Compound Across a Lipid Membrane
Transporter EC number Reaction Reference Solute carrier family 41 member 1 8 Solute carrier family 41 member 2 9

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 Rn Agonist Partial agonist 2.4 pKd - 2,23 ⤷ pKd 2.4 [2,23]

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 - - 1x10-3 - 1x10-2 16 ⤷ Conc range: 1x10-3 - 1x10-2 M Decrease in agonist apparent affinity. [16] 5-HT3A Mm Allosteric modulator Negative - - 1x10-3 - 1x10-2 7,19 ⤷ Conc range: 1x10-3 - 1x10-2 M decrease in agonist apparent affinity. [7,19] Kir2.3 Hs Channel blocker (Intracellular Mg2+) Antagonist 5.0 pKd - 14 ⤷ pKd 5.0 (Kd 1x10-5 M) [14] Voltage: 50.0 mV Kir2.1 Mm Channel blocker (Intracellular Mg2+) Antagonist 4.8 pKd - 31 ⤷ pKd 4.8 (Kd 1.71x10-5 M) [31] Voltage: 40.0 mV Kir1.1 Rn Channel blocker (Extracellular Mg2+) - 2.2 – 2.3 pKi 1x10-3 - 3x10-3 18,32 ⤷ pKi 2.3 (Ki 5x10-3 M) Conc range: 1x10-3 - 3x10-3 M [18,32] Voltage: 0.0 mV pKi 2.2 (Ki 6x10-3 M) Conc range: 1x10-3 - 3x10-3 M [32] Voltage: 0.0 mV TRPM6 Hs Channel blocker - 5.5 – 6.0 pIC50 - ⤷ pIC50 5.5 – 6.0 (IC50 3.4x10-6 – 1.1x10-6 M) inward current mediated by monovalent cations is blocked Kir2.2 Hs Inhibitor (Intracellular Mg2+) - 5.0 pIC50 - 30 ⤷ pIC50 5.0 (IC50 1.1x10-5 M) [30] Voltage: 40.0 mV TRPC5 Rn Channel blocker Inhibition 3.3 pIC50 - 21 ⤷ pIC50 3.3 Internal magnesium [21] HCN1 Mm Channel blocker - 3.3 pIC50 - 26 ⤷ pIC50 3.3 [26] Voltage: 50.0 mV TRPM6 Hs Channel blocker Antagonist 3.3 pIC50 - 27 ⤷ pIC50 3.3 [27] Voltage: 80.0 mV HCN2 Mm Channel blocker - 3.2 pIC50 - 26 ⤷ pIC50 3.2 [26] Voltage: 50.0 mV TRPM7 Mm Channel blocker Antagonist 2.5 pIC50 - 17 ⤷ pIC50 2.5 (IC50 3.2x10-3 M) Reversible inhibition [17] Voltage: 80.0 mV TRPM3 Mm Channel blocker Antagonist 2.0 pIC50 - 20 ⤷ pIC50 2.0 [20] Kir2.4 Hs Inhibitor (Intracellular Mg2+) - - - - ⤷ GluN2A Hs Channel blocker - - - - ⤷ GluN2A = GluN2B > GluN2C = GluN2D GluN2B Hs Channel blocker - - - - ⤷ GluN2A = GluN2B > GluN2C = GluN2D GluN2C Hs Channel blocker - - - - ⤷ GluN2A = GluN2B > GluN2C = GluN2D GluN2D Hs Channel blocker - - - - ⤷ GluN2A = GluN2B > GluN2C = GluN2D TRPM6 Hs Activator (intracellular Mg2+) - - - - ⤷ TRPV5 Hs Channel blocker - - - - ⤷ TRPV6 Hs Channel blocker - - - - ⤷ VRAC Hs Channel blocker (intracellular Mg2+) - - - - ⤷ RyR1 Hs Antagonist (cytosolic Mg2+) Antagonist - - - ⤷ mM range RyR2 Hs Antagonist (cytosolic Mg2+) Antagonist - - - ⤷ mM range RyR3 Hs Antagonist (cytosolic Mg2+) Antagonist - - - ⤷ mM 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+	3

Ligand mentioned in the following text fields
Ionotropic glutamate receptors comments