Lipoic acid is a selective, small molecule large-conductance Ca(2+)-activated K(+) channel (BKCa, KCa1.1, MaxiK) positive modulator with EC50 of 11 uM. Lipoic acid shows a favorable selectivity profile on Nav, Cav, SK, and IK channels. Lipoic acid causes distinct activation from a concentration of 0.3 and 10 µM Lipoic acid left-shifted the voltage activation curve by 60 mV. Lipoic acid reduces spontaneous phasic contractions in guinea pig urinary bladder strips at 1 uM, while having only a modest effect on contractions evoked by electrical field stimulation (EFS) and no effect on high K+-induced contractions.

>98%,Standard References

A-1048400(A 1048400) is a novel potent, selective, orally active N-type and T-type calcium channel blocker with IC50 of 1.4 and 1.2 uM, respectively.

A-317567 (A317567) is a novel potent acid sensing ion channel (ASIC) blocker with IC50 of 2-30 uM.

A-740003 is potent, selective and competitive P2X7 receptor antagonist (IC50 values are 18 and 40 nM for rat and human receptors respectively).

ABT-639 is a novel, peripherally acting, selective T-type Ca2+ channel blocker. ABT-639 blocks recombinant human T-type (Cav3.2) Ca2+ channels in a voltage-dependent fashion (IC50 = 2 μM) and attenuates LVA currents in rat DRG neurons (IC50 = 8 μM).

ABX-1431 (ABX1431) is a highly potent, selective, orally available, CNS-penetrant monoacylglycerol lipase (MGLL) with IC50 of 14 nM (hMGLL).

ABX-1431 (ABX1431) is a highly potent, selective, orally available, CNS-penetrant monoacylglycerol lipase (MGLL) with IC50 of 14 nM (hMGLL).

Acetaminophen is a COX inhibitor for COX-1 and COX-2 with IC50 of 113.7 μM and 25.8 μM, respectively.

ADL5859 agonizes δ-opioid receptor with a 1000-fold selectivity than µ- or κ-opioid receptor with Ki of 32 nM and 37 nM, respectively.ADL5859 displays weak inhibitory activity at the hERG channel with an IC50 of 78 μM. The EC50 of ADL5859 against δ opioid

AMG9810 is a potent and selective, competitive vanilloid TRPV1 receptor antagonist (IC50 = 17 nM).

APD-371 (APD371, Olorinab) is a potent, selective and orally available CB2 agonist with EC50 of 6.2 nM; displays no activity against CB1 receptors (EC50>10 uM); exhibits activity in rat model of osteoarthritis pain.

BCTC is a potent and specific inhibitor of transient receptor potential cation channel subfamily M member 8 (TRPM8) in prostate cancer (PCa) DU145 cells.

BIA 10-2474 is an inhibitor of fatty acid amide hydrolase (FAAH) with IC50 values of 50 to 70mg/kg in various rat brain regions.

branopadol(GRT-6005) is a novel first in class compounds with potent agonist activity on ORL-1 (opioid receptor like -1) and the well established mu opioid receptor.

CNV1014802(GSK-1014802) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.

Difluprednate(Durezol) is a corticosteroid, approved difluprednate for the treatment of post-operative ocular inflammation and pain.

EMA401(Olodanrigan) is a highly selective AT2R antagonist, inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons.

Etodolac is a Cox-2 inhibitor with anti-inflammatory and analgesic activity. Etodolac is shown to inhibit growth and PCNA expression and induce cell cycle arrest in human hepatocellular carcinoma cell lines, in addition to suppressing the occurrence of ab

Flupirtine maleateis a non-opioid, centrally acting analgesia, muscle relaxation and neuroprotection. Currently under a clinical trial (recruiting phase) as a treatment for Multiple Sclerosis and has been used as an analgesic.

Flurbiprofen (Ansaid)

Ibuprofen (Motrin) is an anti-inflammatory inhibitor targeting COX-1 and COX-2, of which is used for pain relief, fever reduction and for reducing swelling.

Mavatrep is an orally bioavailable TRPV1 antagonist (Ki=6.5 nM), exhibits minimal effect on the enzymatic activity (IC50 > 25 μM) of CYP isoforms 3A4, 1A2, and 2D6.

Mirogabalin (DS-5565) is a novel, preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium-channel complexes in the CNS.

Mirogabalin (DS-5565) is a novel, preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium-channel complexes in the CNS.

Opiranserin (VVZ-149, VVZ-000149) is a potent, selective, mixed glycine GlyT2 transporter blocker (IC50= 0.86 uM), purine P2X3 receptor antagonist (IC50=0.87 uM) and serotonin 5-HT2A receptor antagonist (IC50=1.3 uM).

Parecoxib is a selective COX2 inhibitor.

PARECOXIB SODIUM

PF 05089771 is a Nav1.7 channel blocker extracted from patent WO/2010/079443 A1, compound example 788, has an IC50 of 8.6 nM.

PF-06273340 is a highly potent, kinases elective, well-tolerated pan-Trk inhibitor with IC50 values of 6, 4, 3 nM for TrkA, TrkB, Trk C, respectively.

S1RA(E-52862) is a potent and selective sigma-1 receptor(σ1R, Ki=17 nM), showed good selectivity against σ2R (Ki > 1000 nM).

S1RA(E-52862) is a potent and selective sigma-1 receptor(σ1R, Ki=17 nM), showed good selectivity against σ2R (Ki > 1000 nM).

SB-705498 is a potent, selective and orally bioavailable transient receptor potential vanilloid 1 (TRPV1) receptor antagonist with a pIC50 of 7.1.

Grapiprant is a selective EP4 receptor antagonist whose physiological ligand is prostaglandin E2 (PGE2)