DS-II-73 is a selective α2/3/5-containing GABAA receptor (GABAAR) potentiator with IC50 of 320 nM, 381 nM and 435 nM for α2β3γ2 α3β3γ2 α5β3γ2.

CGP 36742 (SGS-742) is a BBB-penetrant GABAB receptor antagonist, discretely up-regulates GABAB receptor binding sites.

Glutipyran is a small-molecule glucose transporter inhibitor, inhibits glycolytic activity and cell growth in human pancreatic cancer cells.

(R)-AS-1 is an orally bioavailable, selective positive allosteric modulator (PAM) of the glutamate transporter EAAT2 with EC50 of 11 nM and Emax of 251%, shows potent antiseizure activity in vivo.

GT951 (GT-951) is a potent, selective activator (positive allosteric modulator) of EAAT2 with EC50 of 0.8 nM in vitro glutamate uptake assays in COS cells overexpressing EAAT2.

GTS476 (GTS-476) is a potent, selective, orally active activator of EAAT2 with EC50 of 35.1 nM in vitro glutamate uptake assays in COS cells overexpressing EAAT2.

GTS511 (GTS-511) is a potent, selective, brain-permeable activator of EAAT2 with EC50 of 3.8 nM in vitro glutamate uptake assays in COS cells overexpressing EAAT2.

NV-6297 (NV6297) is a potent, selective mTORC1 pathway signaling inhibitor without inhibition on mTORC2, inhibits S6K1 phosphorylation (pS6K1 T389) in MCF7 cells with IC50 of 120 nM, directly and selectively targets GLUT-1.

NUCC-0200590 is a small-molecule inhibitor of the TRIP8b-HCN interaction with IC50 of 7.0 uM in AlphaScreen assays, effectively disrupts the TRIP8b-HCN interaction in vitro and in vivo.

Org 34167 HCl salt is a broad-spectrum inhibitor of HCN channels with IC50 of 23.4, 8.2 and 9.2 uM for HCN1, HCN2 and HCN4 channels, respectively, slowing activation and causing a hyperpolarising shift in voltage-dependence of activation.

RO-275 is a potent, selective HCN1 ion channel inhibitor with IC50 of 46 nM, displays 311/100/302-fold selectivity over HCN2/HCN3/HCN4.

(R)-OF-NB1 is a small molecule splice variant GluN2B-selective NMDAR antagonist with IC50 of 675 nM and 97 nM for F-NB1 for splice variant containing exon 5 and GluN1-1a in X. laevis oocytes.

(S)-(-)-DQP-997-74 is a potent, selective GluN2C- and GluN2D-containing NMDARs negative allosteric modulator with IC50 of 69 and 35 nM, respectively, exhibits >100- and >300-fold over GluN2A- and GluN2B-containing receptors.

DQP-997-74 is a potent, selective GluN2C- and GluN2D-containing NMDARs negative allosteric modulator with IC50 of 0.35 and 0.13 uM, respectively, exhibits >100-fold over GluN2A- and GluN2B-containing receptors.

FP802 is a potent neuroprotectant and small molecule inhibitor of TwinF interface, shows selective elimination of eNMDAR-mediated toxicity via disruption of the NMDAR/TRPM4 death signaling complex, while sparing the vital physiological functions of synapt

GluN2A PAM (R)-9 is a potent, brain penetrant, GluN2A-selective positive allosteric modulator with EC50 of 0.51 uM, Emax 350%.

Org 26576 (MK 8777.

PTC-174 is a selective, positive allosteric modulator of NMDA receptors containing GluN2C or GluN2D subunits with EC50 of 4.1 uM (GluN1/2C) and 5.7 uM (GluN1/2D).

UBP1700 is a subtype-selective competitive antagonist of GluN2C/2D-containing NMDA receptors with Ki of 7-9 nM, 50-fold selectivity over GluN2A and GluN2B.

UBP791 is a subtype-selective competitive antagonist of GluN2C/2D-containing NMDA receptors with Ki of 80-90 nM, 50-fold selectivity over GluN2A and GluN2B.

UBP792 is a novel negative allosteric modulator (antagonist) of NMDA receptors, displays partial subtype-selectivity by having a varied maximal inhibition of GluN2A-, GluN2B-, GluN2C-, and GluN2D-containing receptors (52%, 70%, 87%, 89%, respectively) wit

ZCAN155 is a small molecule that prevents AMPA-mediated excitotoxicity (IC50=35 nM) by targeting an allosteric binding site of AMPA glutamate receptor 2 (GluA2), restores neurological function and myelination.

ZCAN262 is a small molecule that prevents AMPA-mediated excitotoxicity (IC50=8.5 nM) by targeting an allosteric binding site of AMPA glutamate receptor 2 (GluA2).

(S)-CE-123 is a specific small molecule dopamine transporter (DAT) inhibitor, improves memory acquisition and memory retrieval.

CDTP-32476 is a potent slow-onset dopamine reuptake blocker with an affinity of 8.6 nM, CDTP-32476 is moderately selective (14-fold) versus NE reuptake blockade with little effect on the SERT.

D-578 is a potent, orally active triple monoamine reuptake inhibitor with Ki values of 16.2. 16.2, 3.23 nM, and 29.6, 20.6, 6.10 nM for the rat brain and cloned human dopamine, serotonin and norepinephrine transporters, respectively.

FFN200 is a vesicular monoamine transporter 2 (VMAT2) substrate, and the first probe to selectively trace monoamine exocytosis in both neuronal cell culture and brain tissue.

GZ-11608 is a potent and selective vesicular monoamine transporter-2 (VMAT2) inhibitor with Ki of 25 nM, GZ-11608 (EC50=620 nM) released vesicular dopamine 25-fold less potently than it inhibited VMAT2 dopamine uptake.

GZ-794A is a potent, selective inhibitor of vesicular monoamine transporter-2 (VMAT2) with Ki of 30 nM, inhibits methamphetamine-evoked endogenous dopamine release with IC50 of 0.4 uM, shows potential for treatment for methamphetamine abuse.

JJC8-016 is a potent, Modafinil-derived dopamine transporter (DAT) ligand with Ki of 116 nM, attenuates compulsive-like methamphetamine self-administration in rats.

JJC8-088 is a potent, Modafinil-derived dopamine transporter (DAT) ligand with Ki of 2.53 nM.

JJC8-091 is a potent, Modafinil-derived dopamine transporter (DAT) ligand with Ki of 16.7 nM, attenuates compulsive-like methamphetamine self-administration in rats.

LQFM215 (LQFM-215) is a synthetic L-proline transporter (PROT/SLC6A7) inhibitor, inhibits proline uptake in hippocampal synaptosome with IC50 of 20.4 uM, present neuroprotective potential.

Lu AF60097 is a high affinity, allosteric inhibitor of serotonin transporter (SERT) inhibitor with IC50 of 31 nM for inhibition of [3H]IMI dissociation, targets the extracellular vestibule (S2 site).

SRI-32743 is a novel allosteric modulator of dopamine transporter (DAT), attenuates HIV-1 Tat protein-induced inhibition of the dopamine transporter.

ZINC000006658090 (Compound 8090) is a highly potent, selective and non-competitive inhibitor of serotonin transporter (SERT) with Ki of 14 nM.

ZINC000443438219 (Compound 8219) is a highly potent, selective and non-competitive inhibitor of serotonin transporter (SERT) with Ki of 3 nM.

ABT-418 hydrochloride (ABT418) is an analog of (-)-nicotine and cholinergic ligand (activator) of nAChRs, a potent inhibitor of [3H]-cytisine binding to nAChR in rat brain with Ki of 2 nM.

Tebanicline dihydrochloride (ABT-594) is a potent, orally active neuronal nicotinic acetylcholine receptor (alpha 4 beta 2 nAChR) agonist with Ki of 37 pM (rat brain) and 55 pM (transfected human receptor).

AN317 is a functionally selective, partial agonist of α6β2-containing nicotinic acetylcholine receptor (nAChR) with pEC50 of 7.17 (α6/α3β2β3V9'S receptor) in cell-based assays, inhibits the effect of nicotine with IC50 of 1.1 uM.

AT1001 (AT-1001) is a high affinity and selective α3β4 nAChR antagonist with Ki value of 2.4 nM, >90-fold selectivity over the other major subtypes (α4β2 and α7 nAChR).

Cris-104 is a selective α4β2* neuronal nAChR agonist, demonstrates antinociceptive and antihypersensitivity in rodent acute/inflammatory and chronic pain models.

CVN417 (CVN-417) is a potent, selective and brain-penetrant α6-containing nicotinic acetylcholine receptor (α6 nAChR) antagonist with Ca2+ flux IC50 of 86 nM.

DM506 is a novel ibogamine derivative and inhibitor of α7 and α9α10 nicotinic acetylcholine receptors (nAChRs) with IC50 of 5.1 uM, 5.6 uM and 6.4 uM for α9α10, α7β2 and α7nAChR, respectively.

JWX-A0108 is a novel selective type I α7 nAChR positive allosteric modulator (PAM) with EC50 of 4.35 uM, shows no potentiation effect on α3β4 nAChR, α4β2 nAChR, or 5-HT3AR.

MK4334 is a potent, selective positive allosteric modulator (PAM) of the α7 nAChR with potential for treatment of Alzheimer's disease.

RGH-560 (RGH560) is a potent, selective α7 nAChR positive allosteric modulator (PAM) with EC50 of 190 nM (Ca2+-influx).

DT-0111 (DT0111) is a selective and effective, water-soluble antagonist at P2X2/3R, does not activate or block P2YR, inhibits ATP-induced current in nodose ganglionic cells with IC50 of 0.3 uM.

Filapixant (BAY1902607) is a potent, selective P2X3 receptor antagonist, shows a substantially higher in vitro selectivity for P2X3 over P2X2 when compared with Eliapixant (BAY1817080, Cat# PC-72754).

3hi2one-G4 is a highly selective small molecule activator targeting GIRK4 homomeric channels, does not activate GIRK2, GIRK1/2 or GIRK1/4 channels.

ACOU001 (ACOU 001) is a potent small-molecule agonist of Kv7.4 (KCNQ4) channel with potential effect against ge-related hearing loss (ARHL) and other hearing impairments related to compromised KV7.4 function.

ACOU085 (ACOU 085) is a potent small-molecule agonist of Kv7.4 (KCNQ4) channel with higher potency than ML-213 in the nanomolar range.

AUT00201 is a potent, selective Kv3 potassium channel modulator with potential for the treatment of rare epilepsy syndromes.

BK channel modulator BC5 is an allosteric modulator of BK type Ca2+-activated K+ channels, interacts with the CTD-VSD interface and specifically modulates the Ca2+ dependent activation mechanism.

C101248 is the first selective small-molecule inhibitor of tandem pore domain halothane-inhibited K+ channel 1 (THIK-1) with IC50 of 50 nM for both mouse and human THIK-1.

Ebio1 is a selective voltage-gated potassium channel KCNQ2 activator. Ebio1 activates KCNQ2 by generating an extended channel gate with greater conductance at a saturation voltage (+50 mV).

LAKI (Light Activated K+ channel Inhibitor) is a specific photoswitchable inhibitor of the pain-related two-pore-domain potassium (K2P) TREK and TRESK channels.

ML308 (ML 308) is a potent, selective inhibitor of two-pore domain potassium channel KCNK9 (TASK-3, K2P9.1) with IC50 of 130 nM in thallium influx fluorescent assays and 413 nM in automated electrophysiology assays, respectively.

NIP-142 (NIP142) is an anti-arrhythmic agent by targeting cardiac K+ channel Kv1.5 (Kv1.5) currents, inhibits the steady-state phase with IC50 of 4.75 uM.

NPBA is a potent, selective pharmacological activator for K2P channel TASK-3 with EC50 of 6.7 uM (TASK-3 whole-cell currents), shows good selectivity between TASK channels.

NPBA-4 is a potent selective TWIK2 channel inhibitor with IC50 of 8.41 uM. shows little to no effects on TWIK1 channel.

SCR2682 is a potent, selective neuronal voltage-gated potassium Kv7/KCNQ/M channel opener (activator) with EC50 of 9.8 nM (Kv7.2/Kv7.3), 100-fold more potency than retigabine.

Tamapin TFA salt is a venom peptide from the Indian red scorpion (Mesobuthus tamulus), potent and selective inhibitor of small conductance calcium-activated potassium channel 2 (SK2, KCNN2) with IC50 of 24 pM.

TTQC-1 is a potent activator of the large-conductance Ca2+-activated K+ channel (BKCa channel), directly and reversibly activates the macroscopic current of BKCa channels expressed in Xenopus oocytes from both sides of the cellular membrane, increases the

VU0542270 is the first selective inhibitor of vascular Kir6.1/SUR2B KATP channel with IC50 of 129 nM, >300-fold selective over other members of the Kir channel family.

VU0546110 (VU 0546110) is a potent, selective inhibitor of the sperm-specific potassium channel SLO3 with IC50 of 1.29 uM, impairs sperm function.

VU0935685 is a potent, selective inhibitor of SLACK potassium channels with IC50 of 0.32 uM in in whole-cell, voltage-clamp electrophysiology (EP) assays, demonstrates selectivity versus hERG.

ZVS-08 is a selective inhibitor of the voltage-gated potassium channel KV10.1 with IC50 of 3.7 uM.

Aneratrigine is a sodium channel protein type 9 subunit alpha blocker.

Benzocaine is a local anesthetic.

BW-031 chloride is a potent cationic sodium channel inhibitor, inhibited Nav 1.7 (IC50=9.5 uM) and Nav 1.1 channels with approximately sixfold greater potency than QX-314.

BW-031 iodide is a potent cationic sodium channel inhibitor, inhibited Nav 1.7 (IC50=9.5 uM) and Nav 1.1 channels with approximately sixfold greater potency than QX-314.

DS43260857 is a potent, selective NaV1.7 inhibitor with IC50 of 15 nM (hNaV1.7), shows 440-fold and 930-fold selectivity over hNaV1.1 and hNaV1.5, respectively.

LTGO-33 is a potent, selective inhibitor of voltage-gated sodium channel NaV1.8 with IC50 of 44 nM (hNaV1.8), 600-fold selectivity against NaV1.1-NaV1.7 and NaV1.9.

Tetrodotoxin (TTx) is a potent, highly selective sodium channel blocker with IC50 of 33 nM for Nav1.6.

UTX-143 is a potent, selective sodium-hydrogen exchange subtype 5 (NHE5) inhibitor with IC50 of 3.11 uM, 80-fold selective over NHE1.

XPC-5462 is a potent, selective dual inhibitor of NaV1.6 and NaV1.2 with IC50 of 10.9 nM and 10.3 nM, respectively.

XPC-7224 is a potent, selective NaV1.6 inhibitor with IC50 of 78 nM and 130 nM for human and mouse NaV1.6, respectively, interacts with the inactivated state of the channel.

AAL-149 is a non-phosphorylatable FTY720 analogue and novel TRPM7 inhibitor, inhibits IM7 in a dose-dependent manner with IC50 of 1.081 uM, shows potent anti-inflammatory effects in vivo.

AMG2504 (AMG 2504) is a selective small molecule TRPA1 inhibitor, inhibits AITC-induced increase in intracellular calcium mediated by TRPA1 in CHO cells with IC50 of 35 nM.

AZ465 (AZ-465) is a potent selective TRPA1 inhibitor, potently inhibitor Zn2+ (100 μM)- and O-chlorobenzylidene malononitrile (CS) (10 nM)-induced TRPA1 activation with IC50 of 85 nM and 20 nM, respectively.

GDC-6599 is a potent, selective transient receptor potential ankyrin 1 (TRPA1) antagonist with IC50 of 5.3 nM (hTRPA1), exhibits TRPA1 cell potency (IC50=20 nM) in the Ca2+ influx assay in CHO cells.

GNE551 is a potent, selective, non-covalent agonist of TRPA1 ion channel with EC50 of 254 nM in Ca2+ influx assays.

JNc-463 is a small-molecule that could increase the TRPV4-eNOS interaction, enhances vasodilation and exert antihypertensive effects in mice.

KS0365 (KS 0365) is a potent and selective activator of transient receptor potential vanilloid 3 (TRPV3) channel with EC50 of 5.08 uM.

Libvatrep (SAF312) is a potent, selective non-competitive inhibitor/antagonist of the transient receptor potential cation channel subfamily V member 1 (TRPV1), shows potential for treatment of ocular surface pain.

M085 (TRPC3/6/7 activator 4o) is a potent and selective TRPC3/6/7 activator with EC50 of 4.66 uM, also activates hTRPC6 with EC50 of 3.8 uM.

SAR7334 (SAR-7334 ) is a highly potent and selective inhibitor of TRPC6 channel, reduces TRPC6-mediated Ca2+ influx with IC50 of 9.5 nM.

Triphenylphosphine oxide (TPPO) is a selective and potent inhibitor of TRPM5 with IC50 of 12 and 30 uM for human and murine TRPM5 heterologously expressed in HEK293 cells.

Trpvicin is a potent and subtype-selective inhibitor of TRPV3 with IC50 of 0.41 and 0.22 uM for hTRPV3-WT and hTRPV3-G573S mutant, respectively.

VPC01091.4 is a non-phosphorylatable FTY720 analogue and novel TRPM7 inhibitor, inhibits IM7 in a dose-dependent manner with IC50 of 0.665 uM.

slCeMM1 is a potent, highly selective inhibitor of lactate transporter SLC16A3 (MCT4), inhibits intracellular lactate accumulation in SLC16A3 dependent cells (IC50=91 nM).

KC289 is a specific small-molecule agonist of PIEZO1 channel and Yoda1 analogue with EC50 of 150 nM in in calcium assays.

VP15 hydrochloride (VP-15 HCl) is a BBB-penetrant, orally active, multitarget directed ligand against acetylcholine and monoamine oxidase enzymes with IC50 of 0.04 and 0.37 uM for AChE and MAO-B, respectively, >600-fold selectivity over BuChE.

AD-5591 (AD5591) is a potent, selective, new generation small molecule ALDH2 activator, has the improved biological activities and pharmacological properties compared to Alda-1. AD-5591 (100  μM) significantly increases the enzymatic activity of recombinant WT and mutant human ALDH2 proteins. AD-5591 is the active form of AD-9308.

AD-9308 is a water-soluble, orally bioavailable, potent, and highly selective ALDH2 activator, AD-9308 is a valine ester prodrug of a potent and selective small molecule ALDH2 activator AD-5591.

ER-001135935 is a potent selective inhibitor of aldehyde dehydrogenase family 1 member A3 (ALDH1A3) with IC50 of 64 nM, Ki value of 106 nM.

KOTX1 is a potent, selective and reversible ALDH1A3 inhibitor with IC50 of 5.14 nM by Aldefluor assay in A375 cells.

LEI-945 (LEI 945) is a first-in-class probe that enables profiling retinaldehyde dehydrogenases (ALDHs) in cancer cells.

NCT-507 (NCT507) is a potent, selective, orally available ALDH1A1 inhibitor with IC50 of 7 nM (hALDH1A1), exhibits high specificity over other ALDH isozymes and unrelated dehydrogenases.

STA-55 is a broad-spectrum activity-based probe of aldehyde dehydrogenase family, can be used to identify therapy resistance biomarkers in cancer and to validate target engagement of ALDH drug candidates.

BAY1128688 is a potent, steroidal aldo-keto reductase 1C3 (AKR1C3) inhibitor with potential for endometriosis.

Imirestat (AL-1576) is a potent aldose reductase inhibitor with IC50 of 8.5 nM for rat lens aldose reductase, with similar IC50 value for the human placental enzyme, shows high affinity for AKR1A1 and AKR1B1 with Ki of 47 and 46 nM respectively.

DG013A (DG 013A) is tripeptide mimetic chemical probe (inhibitor) of ERAP1 with IC50 of 0.19 uM, 15-fold selectivity over ERAP2, potently inhibits aminopeptidase N (APN) with IC50 of 3.7 nM.

AZD0011 (AZD-0011) a novel peptidic boronic acid prodrug of AZD0011-PL, highly potent and orally available Arginase (ARG) inhibitor with IC50 of 404/308 nM for ARG1/2, respectively.

AZD0011-PL is a highly potent Arginase (ARG) inhibitor with IC50 of 7/15 nM for ARG1/2, respectively.

ALLM (Ac-Leu-Leu-Met-CHO) is a potent, cell-permeable calpain inhibitor with Ki of 0.6 and 100 nM for calpain L and calpain B, respectively.

NA-184 is a potent, selective calpain-2 inhibitor with Ki of 50 nM (human calpain-2) and IC50 of 134 nM (mouse calpain-2).

Dutacatib (AFG495) is potent, selective and non-covalent cathepsin K inhibitor with IC50 of 3-6 nM (human CatK), shows excellent selectivity profile versus human cathepsins L and S.

MK-1256 (MK1256) is a potent, selective cathepsin K (Cat K) inhibitor with IC50 of 0.62 nM, >1100-fold selectivity over Cat B, L, S, C, H, Z, and V, 110-fold over Cat F.

Z-Tyr-Ala-CHN2 is a potent cathepsin L inhibitor with EC50 of <50 nM, has broad-spectrum coronavirus antiviral activity.

BMS-737 (BMS737) is a potent, , selective, non-steroidal, reversible inhibitor of CYP17 lyase, 11-fold selectivity for CYP17 lyase over CYP17 hydroxylase.

DLCI-1 is a potent and selective CYP2A6 inhibitor with IC50 of 17 nM, 15-765-fold selectivity other major hepatic CYP enzymes.

DLCI-1 dihydrochloride is a potent and selective CYP2A6 inhibitor with IC50 of 17 nM, 15-765-fold selectivity other major hepatic CYP enzymes.

ODM-208 (ODM208) is a potent, selective, orally bioavailable CYP11A1 inhibitor, inhibits the biosynthesis of pregnenolone with IC50 of 15 nM in NCI-H295R cells.

ODM-209 (ODM209) is a potent, selective, orally bioavailable inhibitor of CYP11A1 (cholesterol side-chain cleavage enzyme) with potential antineoplastic activity, inhibits the biosynthesis of pregnenolone.

TPP-IOA is a specific inhibitor of cytochrome c (cyt c) peroxidase activity, inhibits peroxidase activity of cardiolipin-induced cytochrome c peroxidase activity with IC50 of 5 uM.

AZD7687 (AZD-7687) is a potent, selective DGAT1 inhibitor with IC50 of 80 nM (hDGAT1), >400-fold selectivity over hACAT1.

TP-020 is a potent, selective, orally active inhibitor of monoacylglycerol acyltransferase (MGAT2) with IC50 of 7.8 and 2.4 nM for human and mouse MGAT2, respectively.

AX8819 is a potent, specific DPP-2 inhibitor with IC50 of 0.88 nM, highly selective for DPP II over all of the other DPP enzymes.

ICeD-1 is a potent DPP9 inhibitor capable of killing HIV-1 infected peripheral blood mononuclear cells, activates the caspase recruitment domain family member 8 (CARD8) inflammasome.

TEI-8362 is a potent, selective inhibitor of human neutrophil elastase (HNE) with Ki value of 1.38 nM and IC50 of 1.9 nM.

ARN15381 is a potent, multitarget FAAH inhibitor/D3 partial agonist with low nanomolar range activity, decreases nicotine self-administration in male rats.

UCM1341 (UCM 1341) is a bivalent ligand with melatonin receptor agonist (hMT1/hMT2, pKi=9.11/8.77) and fatty acid amide hydrolase (FAAH) inhibitory activity (rFAAH IC5=0.85 nM).

Fasnall benzenesulfonate is a potent, selective fatty acid synthase (FASN) inhibitor with IC50 of 3.71 uM for purified human FASN isolated from the BT474 cell line.

FASstatin (FASNi-8) is an orally bioavailable small-molecule inhibitor of fatty acid synthase (FASN), directly binds FASN with SPR KD of 16 uM, potentiates TRIM56-mediated FASN ubiquitination.

NJNU-0069 is a specific small-molecule inducer of major histocompatibility complex class II (MHC-II), directly binds to the MAT domain of FASN (Kd=32.1 uM).

NJNU-0069-003 is a specific small-molecule inducer of major histocompatibility complex class II (MHC-II), directly binds to the MAT domain of FASN with Kd of 7.98 uM.

GKA23 is a potent, small molecule glucokinase (GK) activator with EC50 of 152 nM for glucokinase activation in 5 mM glucose, increases glucose uptake in primary rat hepatocytes with EC50 of 201 nM.

GKM-001 is a potent, liver-selective small molecule activator of glucokinase (GKA), demonstrates glucose lowering effect without hypoglycemia in normal and type II diabetes mellitus (T2DM).

TMG-123 (TMG123) is a potent small molecule activator of glucokinase (GK) with EC50 of 0.35 and 0.32 uM for human liver and pancreas GK, respectively.

MZ-101 is a potent, selective inhibitor of glycogen synthase 1 (GYS1) with IC50 of 41 nM (human GYS1), with no inhibition against GYS2.

SRK2128 (SRK 2128) is a highly potent HMG-CoA reductase degrader with EC50 of 84 nM, potently induce degradation of HMG-CoA reductase.

ADAM9i is a specific small molecule inhibitor of ADAM9 protein with binding KD of 5.9 uM and enzyme IC50 of 5.2 uM, promotes the selective degradation of KRAS and sensitizes pancreatic cancers to chemotherapy.

AZD1236 is a potent, selective MMP-9 and MMP-12 inhibitor with IC50 of 4.5 and 6.1 nM respectively, >10-fold selectivity to MMP-2 and MMP-13 and >350-fold selectivity to other MMPs.

BAY-9835 is the first orally bioavailable ADAMTS7 inhibitor with IC50 of 6 nM, which is selective against a range of off-targets and metalloproteases except for ADAMTS12.

CID 3117694 is a selective, non-competitive inhibitor of ADAM10 with IC50 of 1.1 uM, does not inhibit ADAM17.

IPR-179 (ACT-03) is a potent, BBB-permeable, selective gelatinase (MMP2 and MMP9) inhibitor with IC50 of 656 nM and 310 nM, respectively.

JTP-96193 (JTP96193) is a potent, selective TNF-α converting enzyme (TACE/ADAM17) inhibitor with IC50 of 5.4 nM, >1800-fold selectivity against ADAM10.

MMP118 is a potent, selective and orally bioavailable matrix metalloproteinase-12 (MMP-12) inhibitor with IC50 of 1.0 nM (hMMP-12), 1980- and 154-fold selectivity over MMP-13 and MMP-8 respectively.

MMP408 (MMP 408) is a potent, selective matrix metalloprotease 12 (MMP-12) inhibitor with IC50 of 2.0 nM (human MMP-12), 60-fold selectivity over MMP-13.

TAPI-0 is a potent, selective inhibitor of TNFalpha converting enzyme (TACE, ADAM7) with IC50 of 100 nM.

TP0628103 is a highly potent, selective matrix metalloproteinase-7 (MMP-7) inhibitor with IC50 of 0.17 nM and 4.1 nM for human and mouse MMP-7, respectively.

AKU-005 is a potent, dual MAGL/FAAH inhibitor with IC50 of 589 and 309 pM for MAGL in rat and mouse brain membrane respectively, inhibits rat and human FAAH with IC50 of 63 and 389 nM.

GLX481304 is a specific small molecule inhibitor of Nox2 and Nox4 with IC50 values of 1.25 uM, shows negligible effects on Nox1.

LMH001 is a small chemical compound blocking phosphorylated p47phox interaction with p22phox, inhibits effectively angiotensin II (AngII)-induced endothelial Nox2 activation and superoxide production (IC50=0.25 uM).

NCATS-SM7270 is a specific small molecule NADPH oxidase 2 (NOX2) inhibitor with IC50 of 2.1 uM (Polymorphonuclear leukocytes, PMN), inhibits NOX2 in primary human and mouse granulocytes.

TIPTP is a highly potent and selective inhibitor of p22phox, inhibits the p22phox-Rubicon interaction with IC50 of 0.1 uM, and suppresses ROS-mediated inflammation.

A4276 is a novel orally bioavailable NAMPT inhibitor with IC50 of 492 nM for inhibiting NAMPT enzymatic activity, shows high selectivity for NAPRT-deficient lung cancer cell lines.

MM201 is a novel potent nicotinamide phosphoribosyltransferase (NAMPT) inhibitor with IC50 of 74.3 nM in in vitro biochemical assays.

NAMPT activator (NAT) is a potent, small molecule activator of nicotinamide phosphoribosyltransferase (NAMPT) with ITC KD of 500 nM.

Dovramilast (CC-11050) is a potent and orally active phosphodiesterase 4 (PDE4) inhibitor, CC-11050 is a promising candidate for host directed therapy of patients with pulmonary TB.

CRD733 (ASP4901) is a potent, selective cGMP-specific PDE9 (phosphodiesterase 9) inhibitor.

Gemlapodect (NOE-105) is a potent, selective PDE10A inhibitor with a potential therapeutic effect for the treatment of COFD.

MCI-030 (ADT 061) is a potent, selective PDE10 inhibitor, inhibits recombinant PDE10 using cGMP as a substrate with IC50 of 0.3 uM.

ME3183 is a potent, selective phosphodiesterase 4 (PDE4) inhibitor with IC50 of 2.33, 1.28 and 1.63 nM for PDE4B1, PDE4A1A and PDE4D2 respectively.

A potent and selective PDE10A inhibitor with IC50 of 0.37 nM.

TOP-N53 is a dual-acting nitric oxide (NO) donor and selective PDE5 inhibitor, potently inhibits PDE5 with IC50 of 1.6 nM.

TPN171 (TPN-171) is a highly potent, selective phosphodiesterase type 5 (PDE5) inhibitor with IC50 of 0.62 nM, 32-fold selectivity over PDE6.

Yonkenafil is a potent, selective PDE5 inhibitor with IC50 of 2.0 nM.

ABD298 is a potent, selective ABHD13 inhibitor, inhibits HEK293T cells expressing recombinant mouse ABHD13 with IC50 of 0.98 uM.

KT-203 (KT203) is a potent, selective inhibitor of α/β-hydrolase domain 6 (ABHD6) with IC50 of 3.9 nM in 2-AG hydrolysis assays.

VU533 is a small molecule activator of N-acyl-phosphatidylethanolamine hydrolyzing phospholipase D (NAPE-PLD) with EC50 of 0.3 uM, enhances efferocytosis by macrophages.

VU534 is a small molecule activator of N-acyl-phosphatidylethanolamine hydrolyzing phospholipase D (NAPE-PLD) with EC50 of 0.3 uM, enhances efferocytosis by macrophages.

IPR3011 is a small-molecule uPAR-uPA protein-protein interaction inhibitor with Ki of 2.4 uM.

WX-293 is a highly selective small-molecule inhibitor of urokinase-type plasminogen activator (uPA) with Ki of 2.4 uM.

WX-340 is a highly specific and selective, peptidic cyclic competitive inhibitor of urokinase-type plasminogen activator (uPA) with Ki of 12 and 170 nM for human and mouse uPA, respectively, inhibit 10 Units of human uPA with IC50 of 90 nM.

GSK-199 is a potent, highly selective and reversible protein arginine deiminase PAD4 inhibitor with IC50 of 250 nM in FP binding assay (0.2 mM Ca), 200 nM in PAD4 NH3 release inhibition assay.

JBI-589 (JBI589) is potent, selective, orally active PAD4 small molecule inhibitor, reduces CXCR2 expression and blocks neutrophil chemotaxis.

ML325 (ML 325) is a potent, irreversible pan-protein arginine deiminase (PAD) inhibitor with IC50 of 70 nM, 200 nM 170 nM, and 240 nM for PAD1, 2, 3, and 4 in vitro respectively.

ATUX-1215 is a direct, orally active small molecule activator of protein phosphatase 2A (PP2A), suppresses bleomycin-induced fibrosis in vivo.

ATUX-792 is a small molecule activator of protein phosphatase 2A (PP2A), decreases survival, proliferation, and motility of neuroblastoma in vitro and tumor growth in vivo.

CNBCA is a selective, competitive inhibitor of Src homology phosphotyrosyl phosphatase 2 (SHP2) with IC50 of 0.87 uM, effectively suppresses breast cancer cell phenotypes.

DS-1211 (DS1211) is a potent, selecitve inhibitor of tissue-nonspecific alkaline phosphatase (TNAP) with IC50 of 3.4 nM.

HN252 is a potent protein phosphatase 1B (PPM1B) inhibitor with Ki of 0.52 uM and IC50 of 0.76 uM, shows no inhibition against topoisomerases in vitro.

JAB-3068 (JAB3068) is a potent, selective and orally bioavailable allosteric inhibitor of SHP2.

K161 is a potent, pan-SHIP1/2 inhibitor with IC50 of 1.5- 6 uM and 6.5-13 uM, respectively.

K306 is a specific, small molecule agonist of SH2-containing 5' inositol phosphatase 1 (SHIP1) with EC50 of 119 nM, 10-fold higher selectivity over SHIP2.

NGD61181 is a pyrazole-based SHIP2 inhibitor, has micromolar binding affinity and inhibitory activity, does not contain a phosphatase “warhead,” binds the active site of SHIP2.

NSC49L (NSC30049) is a small molecule agonist (activator) of protein phosphatase 2A (PP2A), specifically stimulates PP2A-Cα activity with Kact of 14 nM, downregulates the AKT1/mTOR/4EBP1-axis, and inhibits p21 translation.

NSC74429 is a CNS-active, small molecule PHLPP inhibitor with IC50 of <5 uM, shows neuroprotective activity in primary rat cortical neurons in STS assay.

SBI-221 is a small molecule inhihitor of SHP2-E76K mutant with IC50 of 2.1 uM and 7.4 uM for SHP2-E76K and SHP2-WT in isothermal CETSA assays, respectively.

SBI-668 is a selective inhihitor of SHP2-E76K mutant with IC50 of 2.1 uM in isothermal CETSA assays, 7-fold selectivity over SHP2-WT (IC50=15 uM).

Sanofi-14h is a selective inhibitor of the AGC family kinase SGK3, blocks DMXAA-stimulated IRF3-promoter activity with IC50 of 1.73 uM, inhibits IFNβ production under STING stimulation.

(R)-SW203668 (SCD inhibitor (R)-27) is a potent, tumor-specific, irreversible stearoyl CoA desaturase (SCD) inhibitor with high sensitity to H2122 cell (IC50=11 nM).

TPT-004 is a highly potent, selective tryptophan hydroxylase (TPH) with IC50 of 77 nM and 16 nM for TPH1 and TPH2, respectively.

MLT-827 is a potent and selective inhibitor of MALT1 paracaspase activity with IC50 of 5 nM.

MLT-943 is a potent and selective MALT1 protease inhibitor with IC50 of 40 nM in IL-2 reporter gene assay (Jurkat T cells), inhibits human PBMC IL-2 release with IC50 of 74 nM.

ET516 is a potent androgen receptor liquid-liquid phase separation (AR LLPS) inhibitor, specifically disrupts AR condensates, effectively suppresses AR transcriptional activity and inhibits the proliferation and tumor growth of prostate cancer cells expre

Faznolutamide is a potent, selective androgen receptor (AR) antagonist.

JJ-450 is a novel analogue of IMTPPE and direct and specific inhibitor of androgen receptor (AR) transcriptional activity, blocks AR recruitment to androgen-responsive elements and suppresses AR target gene expression.

M17-B15 is a potent, specific small molecule inhibitor of androgen receptor (AR) targeting the dimer interface pocket (DIP), inhibits AR transcriptional inhibition with IC50 of 0.03 uM.

A potent, selective androgen receptor modulator (SARM) with binding IC50 of 6.6 nM.

SC428 (SC-428) is a small molecule androgen receptor (AR) signaling inhibitor, directly binds to the AR N-terminal domain (NTD) and exhibits pan-AR inhibitory effect.

UT-105 is a small-molecule, irreversible, selective androgen receptor (AR) degrader (SARD) and irreversible inhibitor, binds to AR N-terminal domain (NTD) and inhibits both the AR and AR splice variants (AR-SVs).

UT-215 (UT215) is a small-molecule selective androgen receptor (AR) irreversible covalent antagonist, covalently and selectively bind to C406 and C327 in the AF-1 region of AR.

GDU-952 is a novel small molecule aryl hydrocarbon receptor (AhR) agonist, activates and induces nuclear translocation of AhR.

A endogenous ligand, potent aryl hydrocarbon receptor (AhR) agonist in vitro.

D089 is a selective small molecule stabilizer of the MYC G4-quadruplex, not only inhibits MYC expression in myeloma cell lines, but also selectively induces G1 arrest in MYC-driven cancer cell lines containing the MYC-G4 sequence.

Isopomiferin is a prenylated isoflavonoid, collapses the tumor checkpoint module (TCM) and suppresses both MYCN and TEAD4 in MYCN-amplified NBL cells.