DSO-5a (Dimethyl shikonin oxime 5a) is a potent, selective agonist pf bombesin receptor subtype-3 (BB3, BRS-3) with pEC50 of 8.4 (IP-1 accumulation in hBB3-H1299 cells).

(S)-AC-265347 is a potent, selective CaSR agonist and positive allosteric modulator (ago-PAM), 10- to 20-fold more potent than (R)-AC-265347.

AM6527 is a highly potent, selective cannabinoid CB1 receptor antagonist with binding Ki of 4.88 nM, 100-fold selective over CB2 receptors.

JM-00266 is a novel non-brain penetrant cannabinoid receptor 1 (CB1R) inverse agonist.

JWH133 (JWH-133) is a potent and selective CB2 agonist with Ki of 3.4 nM, 200-fold selective over CB1 receptors, inhibits glioma growth in vivo.

LEI-102 (LEI 102) is a potent, selective cannabinoid CB2 receptor agonist with binding pKi of 8.0, 1000-fold selectivity over CB1R.

URB447 (URB-447) is a peripherally restricted CB(1) antagonist/CB(2) agonist with IC50 of 313 nM (rat CB1) and 41 nM (human CB2).

BMS-694153 is a potent, selective calcitonin gene-related peptide (CGRP) receptor antagonist with Ki of 0.013 nM for hCGRP (inhibition of 125I-CGRP binding in SK-N-MC cell membranes).

ACT-672125 (ACT672125) is a potent, selective CXCR3 antagonist with IC50 of 239 nM in human blood.

alpha-NETA (α-NETA) is a small molecule antagonist of chemerin receptor chemokine-like receptor 1 (CMKLR1), inhibits chemerin-stimulated β-arrestin2 association with CMKLR1 with IC50 of 4.9 uM.

AZ12436092 (AZ 12436092) is a potent, selective CCR3 antagonist with binding pKi value of 9.2.

AZD3778 (AZD-3778) is a dual CCR3 and H1-receptor antagonistwith Ki of 54 nM for guinea-pig H1-receptor, inhibits binding of CR3 radioligand 125I-eotaxin to human CCR3-receptor expressed on CHO-cells with IC50 of 8 nM.

BPRCX714 (BPRCX 714) is a highly selective and potent CXCR4 antagonist with binding IC50 of 34.2 nM, effectively inhibits CXCL12-induced movement of CCRF-CEM cells with EC50 of 13.7 nM.

BPRCX807 (BPRCX-807) is a highly selective and potent CXCR4 antagonist with binding IC50 of 40.4 nM and EC50 of 48.1 nM for cell-mobility activity in the chemotaxis assays, inhibits CXCL12-mediated cell signaling pathway.

A potent and specific CCR6 antagonist.

DF2755A is a selective, allosteric, orally acting inhibitor of CXCR1/2 (Kd=2.24/0.94 nM), inhibits human PMN (hPMN) migration induced by CXCL8 and CXCL1 with IC50 of 4.2 and 2.1 nM, respectively.

GW782415W (GW782415) is a potent, specific CCR3 antagonist, inhibits chemotaxis of human and murine eosinophils pKi of 8.08 and 7.85, respectively.

Ki19003 (Ki 19003) is a potent, specific CCR3 antagonist, inhibits the CCL11-induced migration of CCR3-expressing L1.2 cells with IC50 of 20 nM.

LN6023 (LN-6023) a potent, selective and first-in-class inhibitor of the atypical chemokine receptor 3 (ACKR3, CXCR7) with β-arrestin EC50 of 3.5 uM.

NUCC-390 dihydrochloride (NUCC390) is a small molecule agonist of CXCR4, recapitulates the activity of CXCL12α.

RAP-103 is an orally active, stabilized pentapeptide analog of DAPTA (D-ala-peptide T-amide), and multi-chemokine receptor antagonist.

SCH-479833 is a potent, specific and orally active CXCR1 and CXCR2 antagonist with Ki of 0.17 and 7 nM, respectively.

UCB35625 is a potent, selective inhibitor of CCR1 and CCR3, inhibits MIP-1α-induced chemotaxis in CCR1 transfectants and eotaxin-induced chemotaxis in CCR3 transfectants with IC50 of 9.57 and 93.8 nM respectively.

UCUF-965 (UCUF965) is a potent partial agonist and positive allosteric modulator of CXCR4 with EC50 of 0.02 uM, Emax=44% for CXCR4/CXCL12 signaling for β-arrestin-2 recruitment.

VUF15485 is a small-molecule agonist of the atypical chemokine receptor ACKR3 with binding pIC50 of 8.3, and pEC50 of 7.6 in BRET-based β-arrestin2 recruitment assay.

YM-344031 is a potent, selective, brain-penetrable CCR3 antagonist with binding IC50 of 3.0 nM, inhibits ligand-induced Ca(2+) flux with IC50 of 5.4 nM.

YM-344484 (YM344484) is a potent, selective dual antagonist of chemokine CCR3 receptor and histamine H1 receptor, potently inhibits both the CCL11-induced Ca2+ influx in human CCR3-expressing cells (Kb=1.8 nM) and histamine-induced Ca2+ influx in histamin

YM-355179 is a potent selective, and orally available antagonist of CC chemokine receptor 3 (CCR3) with binding IC50 of 7.6 nM (CCL5).

BMK-C205 (BMK-C 205) is a potent, selective corticotropin-releasing hormone receptor 1 (CRF1R) antagonist with IC50 of 74 nM in calcium mobilization assays, blocks hypothalamus-pituitary-adrenal (HPA) axis activation.

NBI-27914 is a potent, selective antagonist of corticotropin-releasing factor 1 (CRF1) receptor with Ki of 1.7 nM, shows no activity at CRF2 receptors.

NBI-35965 is a potent, selective antagonist of corticotropin-releasing factor 1 (CRF1) receptor with Ki of 4 nM, >1000-fold selective over CRF2.

GSK598809 (GSK-598809) is a potent, selective dopamine D(3) receptor antagonist with Ki value of 6.2 nM, >100-fold selectivity over D2 receptor.

(±)VK4-40 is a highly selective and metabolically stable D3 partial agonist, shows high affinity for D3 receptor (Ki=0.35 nM) and high selectivity for D3 over the D2 receptor.

(R)-ABS01-113 is a potent, selective dopamine D3 receptor (D3R) antagonist with IC50 of 11.4 nM, binds with high affinity to D3R with Ki value of 0.34 nM.

(S)-ABS01-113 is a potent, highly selective and efficacious dopamine D3 receptor (D3R) partial agonist with EC50 of 7.6 nM, binds with high affinity to D3R with Ki value of 0.84 nM, >1,000-fold selectivity over D2R.

(±)-ABS01-113 is a structural analog of the D3R partial agonist, (±)-VK4-40.

AG-0029 is a highly potent agonist of dopamine D2/D3 receptor (EC50=0.08 nM) and a moderate affinity antagonis of H3 receptor (IC50=111 nM).

ASP4345 (ASP-4345) is a potent, selective positive allosteric modulator of the dopamine type 1 (D1) receptor that selectively binds to, and enhances the activity of, D1 receptors.

BAK4-54 is a high affinity dopamine D3 receptor (D3R) antagonist/partial agonist withIC50 of 8.0 nM as full D3R antagonist, EC50 of 140 nM as partial D3R agonist.

CAB-01-019 is potent, selective dopamine D4 receptor (D4R) full antagonist with binding Ki of 2.2 nM, >500-fold selectivity over D2R and D3R.

CAB2-015 is a high affinity dopamine D3 receptor (D3R) antagonist/partial agonist withIC50 of 7.4 nM, Ki of 0.351 nM, 45-fold selectivity over D2R.

CJB 090 (CJB090) is a selective partial agonist of dopamine D3 receptor with binding Ki of 0.6 nM, CJB 090 is 97-fold selective for D3 receptors over D2.

F17464 is a dopamine D3 receptor preferential antagonist exhibiting high affinity for human dopamine receptor subtype 3 (hD3) (Ki=0.17 nM) and 5-HT1a (Ki=0.16 nM) and a >50 fold lower affinity for the human dopamine receptor subtype 2 short and long form (hD2s/l) (Ki=8.9 and 12.1 nM, respectively). F17464 is a D3 receptor antagonist, 5-HT1a receptor partial agonist. F17464 blocks ketamine induced morphological changes, an effect D3 receptor mediated, in human dopaminergic neurons. F17464 increases dopamine release in the rat prefrontal cortex and mouse lateral forebrain-dorsal striatum and seems to reduce the effect of MK801 on % c-fos mRNA medium expressing neurons in cortical and subcortical regions. F17464 also rescues valproate induced impairment in a rat social interaction model of autism, with dose range 0.32-2.5 mg/kg i.p. in both rats and mice

GR-103691 is a potent, selective dopamine D3 receptor antagonist with binding Ki of 0.4 nM, >100-fold selectivity over D1 and D4 receptors.

ML321, CAS 1596117-75-7, ML 321, D2R antagonist. ML321 is a selective small molecule dopamine D2 receptor (D2R) antagonist with binding Ki of 120 nM, exhibits an excellent D2 versus D1, D3, D4 and D5 receptor selectivity.

PG01037 is a potent selective dopamine D3 receptor antagonist with binding Ki of 0.7 nM, displays 133- and 540-fold selectivity over D2 and D4 receptors, respectively.

R-VK4-40 is a highly selective, potent and orally available dopamine D3 receptor (D3R) antagonist with Ki of 6.8 nM, >1500-dold selectivity over D2R.

ZINC621433144 is a Gi-biased, high-affinity full agonist of dopamine D4 receptor with Ki of 4.3 nM and cAMP EC50 of 0.18 nM.

2CTAP is a small molecule inverse agonist of FFA2 receptor signalling, inhibits constitutive Ca2+ levels, antagonised acetate-induced pERK1/2 and prevents damage following IRI, has no effect on cAMP.

AZ13595491 (AZ491) is a potent, selective G-protein-coupled receptor GPR120 (FFAR4) agonist with IC50 of 0.74/1.0 uM for huamn/mouse GPR120, respectively.

AZ423 (AZ13595423, AZ-423) is a potent, selective G-protein-coupled receptor GPR120 (FFAR4) agonist with IC50 of 0.36/0.51 uM for huamn/mouse GPR120, respectively.

CPL207280 (CPL 207280) is a novel potent, selective GPR40/FFA1 agonist with EC50 of 80 nM in a Ca2+ influx assay, shows greater potency than fasiglifam (EC50=270 nM).

MK-2305 (MK2305) is a potent and selective partial GPR40 (FFAR1) agonist with EC50 of 6 nM (rat GPR40), stimulates glucose stimulated insulin secretion (GSIS).

Phenylacetamide 2 (FFA2 allosteric agonist 2) is a potent, specific and allosteric agonist of FFA2 (GPR43) with cAMP IC50 of 0.48 and 0.66 uM for hFFA2 and mFFA2, respectively.

TUG-2304 (TUG2304) is a highly potent FFA2 (GPR43) antagonist with IC50 of 3-4 nM in both cAMP and GTPγS assays.

Merigolix is a potent, selective gonadotrophin releasing hormone (GnRH) antagonist.

SCH900271 is a potent nicotinic acid receptor GPR109A agonist with EC50 of 2 nM in hu-GPR109a assays.

AS1535907 is a potent GPR119 agonist with EC50 of 4.8 uM in HEK293 cells stably expressing human GPR119.

AS1907417 is a potent, selective GPR119 agonist with cAMP EC50 of 1.1 uM (human GPR119).

HBK001 (HBK-001) is a dual-target DPP4 inhibitor and GPR119 agonist with IC50 of 66 nM for DPP4 and EC50 of 30 nM for GPR119 transactivation activity.

JTP-109192 (JTP109192) is a potent GPR119 agonist with EC50 of 3.6. 4.5 and 5.2 nM for human, rat and mouse GPR119 respectively (increased intracellular cAMP levels).

ZB-16 (ZB40-0016) is a potent, selective GPR119 agonist, increase intracellular cAMP with EC50 of 7.25 nM, stimulates incretin secretion.

CID1792197 is a potent, selective GPR55 agonist with EC50 of 110 nM in the β-arrestin trafficking assay,100-fold selectivity for GPR55 over GPR35, CB1 and CB2.

OX04528 is a highly potent, selective, G-protein pathway biased and orally bioavailable GPR84 agonist with EC50 of 5.98 pM for inhibition of FSK (25 uM)-induced cAMP production in CHO-hGPR84 cells.

OX04529 is a highly potent, selective, G-protein pathway biased and orally bioavailable GPR84 agonist with EC50 of 18.5 pM for inhibition of FSK (25 uM)-induced cAMP production in CHO-hGPR84 cells.

RTI-122 (RTI 122) is a highly potent, selective and brain permeable GPR88 agonist with cAMP EC50 of 11 nM (hGPR88 CHO).

RGH-235 is a potent, selective, and orally active H3 receptor antagonist/inverse agonist with high affinity (Ki=3.0-9.2 nM, depending on species), without affinity to H1, H2 or H4 receptors.

UR-MB-69 is a potent agonist of histamine H2 receptor (H2R) dopamine receptor D3R with pKi of 8.69 and 8.06, respectively.

LY290154 is a leukotriene LTD4/E4 antagonist.

ACT-1016-0707 is a potent, selective, and orally active lysophosphatidic acid receptor subtype 1 receptor (LPA1 receptor, LPAR1) antagonist with IC50 of 3.1 nM, highly selective over LPAR2 or LPAR3.

ASP1126 is a potent, selective and orally active sphingosine-1-phosphate (S1P) agonist with EC50 of 7.12 and 517 nM for hS1P1 and hS1P3 in GTPgS-binding assays, respectively.

IMMH002 is a potent, selective and orally active S1P1 agonist, IMMH002 can be transformed to IMMH002-P in vivo, IMMH002-P activates S1P1, S1P4, and S1P5 with 12.4, 19.8 and 29.4 nM respectively.

JTE-013 (JTE013) is a potent, specific S1P2 receptor (Edg-5) antagonist with IC50 of 17 nM and 22 nM for human and rat S1P2, respectively.

NXC736 hydrochloride (SLB736) is a selective functional antagonist for type 4 sphingosine-1-phosphate receptor (S1PR4), has immunomodulatory and anti-fibrotic effects.

SLB1122168 is a potent, specific inhibitor of S1P transporter spinster homologue 2 (Spns2), inhibits Spns2-mediated S1P release with IC50 of 94 nM.

SLB1122168 hydrochloride is a potent, specific inhibitor of S1P transporter spinster homologue 2 (Spns2), inhibits Spns2-mediated S1P release with IC50 of 94 nM.

TP0541640 (TP 0541640) is a novel potent LPA1 antagonist with IC50 of 1.6 nM, shows potential for the treatment of lung and skin fibrosis.

UCM-14216 (UCM14216) is a potent and selective antagonist of type 2 lysophosphatidic acid receptor (LPA2) with KD value of 1.3 nM and IC50 of 1.9 uM.

VU0405645 is a potent, biased M1 receptor-positive allosteric modulator, potentiates Ca2+ mobilization in CHO cells stably expressing the M1 receptor with EC50 of 340 nM.

CRN04894 is a highly potent, selective, orally available melanocortin 2 receptor (MC2R antagonist) antagonist with Ki of 2.1 nM.

SNT-207707 (SNT207707) is a potent, selective, BBB-penetrating, and orally active melanocortin-4 (MC-4) receptor antagonist with binding/fuaction IC50 of 8/5 nM, respectively.

SNT-207858 (SNT207858) is a potent, selective, BBB-penetrating, and orally active melanocortin-4 (MC-4) receptor antagonist with binding/fuaction IC50 of 22/11 nM, respectively.

TCMCB07 is a synthetic, cyclic nonapeptide peptide antagonist of the melanocortin-4 receptor (MC4R), ameliorates cancer- and chronic kidney disease-associated cachexia.

CVN636 is a potent, selective, CNS penetrant and allosteric agonist of mGluR7 with EC50 of 7 and 2 nM for human and mouse mGluR7, respectively.

MK-8768 (MK8768) is a potent, selective mGluR2 negative allosteric modulator (NAM) with IC50 of 9.6 nM, shows no activity against mGluR 1,3,4,5,6,8.

ML353 (VU0478006) is a highly potent, selective, MPEP-site silent allosteric modulator of mGlu5 receptor with with sub-100 nM affinity.

VU6046980 is a potent, selective and in vivo active mGlu7 positive allosteric modulator (PAM) with EC50 of 0.15 uM (rat mGlu7).

VU0506013 is a high-affinity, selective positive allosteric modulator (PAM) of neuropeptide Y4 receptor (Y4R) with EC50 of 125 nM.

ML301 is a selective full (79-93%) neurotensin-1 (NTR1) receptor agonist with EC50 of 2.0-4.1 uM, good selectivity relative to NTR2 and GPR35.

AT-039 is a potent, selective agonist of nociceptin opioid peptide (NOP) receptor, AT-039 is useful for treatment of hypertension and/or volume overload/hyponatraemic states.

LY2817412 is a potent, selective andorally active nociceptin/orphanin FQ (NOP) receptor antagonist with Ki of 0.176 nM, Kb of 0.273 nM in functional assay of receptor-mediated G-protein activation using [35S]-GTPγS binding.

MP135 is a potent, μ-δ opioid receptor heteromer-selective agonist with EC50 of 0.8 nM in GTPγS assays, shows functional selectivity for μ-δ heteromers over homomeric μOR and δOR and low β-arrestin2 recruitment activity.

A potent, competitive antagonist for μ, κ, δ, and σ-opioid receptors with Ki of 0.0825 nM, 0.509 nM, and 8.02 nM, for MOR, KOR, and DOR, respectively.

PIPE-3297 is a fully efficacious and selective kappa opioid receptor (KOR) agonist with functional GTPγS EC50 of 1.1 nM, Emax=91%, does not elicit β-arrestin-2 recruitment functional response.

PN6047 is an orally bioavailable, G protein-biased and selective δ opioid agonist with pKi of 7.25, fully engages G protein signaling but is a partial agonist in both the arrestin recruitment and internalization assays.

ZYKR1 is a potent, and peripherally restricted kappa opioid receptor (KOR)-selective agonist with EC50 of 0.061 nM in cAMP assays, highly selective over the mu and delta opioid receptors (EC50>10 μM).

(R)-YNT-3708 is a potent, selective orexin 1 receptor (OX1R) agonist with EC50 of 7.48 nM and Emax 101%, 22-fold selectivity over OX2R (IC50=168 nM).

CVN45502 (CVN 45502) is a potent, orally bioavailable, highly selective orexin 1 receptor (Hcrtr1, OX1R) antagonist with binding affinity (pKi) of 7.86 (human Hcrtr1), significantly reduces feeding and body weight in diet-induced obese (DIO).

CVN766 (CVN 766) is a potent, exquisitely selective orexin 1 receptor (OX1R) antagonist with IC50 of 8 nM, 1000-fold selective over OX2R.

OBPt-9 is a potent, postivie allosteric potentiator of orexin receptor-mediated signaling, similarly potentiates the response of OXR1 and OXR2 to orexin A.

MRS4833 is a potent, selective antagonist of Gi protein-coupled P2Y14 receptor (P2Y14R, GPR105) with IC50 of 5.9 nM, Ki of 3.44 nM (human P2Y14R).

MRS4853 is a selective P2Y6 receptor (P2Y6R) antagonist with IC50 of 0.46 uM (hP2Y6R), displays weak affinity for mP2Y6R (IC50=6.15 uM).

ACT-774312 (ACT774312) is a potent and selective CRTH2 receptor antagonist with IC50 of 3 nM, 150-fold more potent than setipiprant in inhibiting PGD2-induced eosinophil cell shape change.

AGN 225660 is a second-generation prostanoid receptor antagonist acting at multiple receptor subtypes with IC50 of 220/70/2900/7100/70/180/1100/5 nM for DP1/EP1/EP2/EP3/EP4/FP/IP/TP receptors, respectively.

AMX12006 (AMX-12006) is a potent, selective, orally active antagonist of prostaglandin E2 (PGE2) receptor 4 (EP4) with IC50 of 4.3 nM in cAMP assays, shows no activity against EP1, EP2, EP3 receptors.

CR6086 sodium (CR-6086) is a potent, selective prostaglandin E2 receptor 4 (EP4) antagonist with Ki of 16.6 nM (hEP4 receptor), inhibits PGE2-stimulated cAMP production with IC50 of 22 nM.

L001 is a potent and selective EP4 antagonist with cAMP IC50 of 7.29 nM, impairs pancreatic cancer migration and invasion.

LY3127760 is a potent, selective prostaglandin E4 (EP4) receptor antagonist with binding Ki of 58 nM (hEP4) and cAMP IC50 of 5.6 nM.

ONO-4578 (BMS-986310) is a potent, highly selective EP4 antagonist, potently inhibits the PGE2-induced cAMP production in CHO cells expressing mouse and human EP4 receptors with single-digit nM IC50.

TG11-77 is a potent, selective, brain-permeable and orally available antagonist of the prostaglandin E2 (PGE2) receptor subtype EP2 with KB value of 9.7 nM.

1-Piperidine Propionic Acid (1-PPA) is an allosteric Inhibitor of protease activated receptor-2 (PAR2) with IC50 of 2.3 uM.

NRD-21 is a potent, selective, reversible, negative allosteric modulator of PAR1 with IC50 of 0.37 uM in calcium mobilization assays.

TFLLRN-NH2 is a potent, PAR1-selective agonist peptide with EC50 of 1.9 uM.

Ogremorphin (OGM, OGM8345) is a highly specific, first-in-class small-molecule inhibitor of GPR68 with IC50 of 0.71 uM.

Ogremorphin-1 (OGM1) is a highly specific, first-in-class small-molecule inhibitor of GPR68 with IC50 of 0.16 uM.

DC591053 (DC 591053) is a selective small molecule agonist of relaxin family peptide receptor 4 (RXFP4) with pEC50  of 7.24  and pKi  of  6.95, shows no activity against RXFP3.

AZ-66 is a highly potent S1R/S2R antagonist with Ki of 0.31/1.76 nM, respectively.

CM-304 is a potent, selective sigma-1 receptor (S1R) antagonist with Ki of 3.41 nM, 100-fold selective over S2R.

GM310 is a small molecule inhibitor of glycolysis, proteotoxicity, inflammation, and impairments in animal models of Alzheime's, Huntington's, and stroke by activation of the Sigma-1 receptor.

JR1-157 is a potent selective sigma 2 receptor (σ2R) ligand with Ki value of 47 nM, >10-fold selectivity over σ1R.

MAM03055A is a novel bivalent sigma-2 receptor/TMEM97 ligand with cytotoxic activity, exhibits high affinity and strong preference for sigma-2 receptor with Ki of 55.9 nM.

RC-752 is a potent, seletive sigma-1 receptor (S1R) antagonist with Ki of 6.2 nM, 50-fold selective over S2R, shows antinociceptive activity.

WLB-89462 (WLB89462) is a potent, highly selective sigma-2 receptor (σ2R) ligand with Ki of 13 nM, >100-fold selective over σ1R (Ki=1777 nM).

CRN02481 is a potent and selective SST5 receptor agonist with EC50 of 0.37 nM (human SST5), with excellent selectivity against SST1, SST2, SST3 and SST4 receptors.

S6821 (S 6821) is a potent and selective bitter taste receptor TAS2R8 with IC50 of 21 nM.

Org 274179-0 is a highly potent, allosteric antagonist of the thyroid-stimulating hormone receptor (TSH receptor), inhibits bTSH-, hTSH- and M22-mediated CRE-luciferase transactivation in the CHO cell line.

SYD5115 (SYD-5115) is a potent, selective and orally bioavailable thyrotropin receptor (TSH-R) antagonist with IC50 of 48 and 62 nM for rTSHR and hTSHR, respectively.

OPC-61815 is a water-soluble phosphate ester pro-drug of Tolvaptan (Cat# PC-45125), which is an orally active vasopressin V2 receptor antagonist.

RGH-122 is a potent, selective, and orally bioavailable V1a receptor antagonist with Ki/IC50 of 0.3/0.9 nM (hV1a) respectively, >100-fold selectiive over V2 receptor.

CMP-1611 is a small molecule inhibitor of protease of the complement classical pathway, C1r, directly inhibits classical pathway-specific complement activation in a dose-dependent manner.

DF3016A (DF 3016A) is a potent and selective C5aR inhibitor with IC50 of 50 nM (C5a-induced human PMN migration and IC50 of 45 and 37 nM against rat and mouse C5aR, respectively.

T-ALZ01 (CMP-1696) is a small molecule inhibitor of complement component C1r.

Peptide WWGKKYRASKLGLAR is a super agonist of complement factor C3aR, 12-15 times more active than natural C3a.

MK-886 (L-663,536) is a potent, selective and orally active inhibitor of 5-lipoxygenase-activating protein (FLAP) with IC50 of 30 nM.

Rytvela (Peptide 101.10) is a potent, selective, allosteric negative modulator (antagonist) of IL-1 receptor I (IL-1RI), inhibits dose-dependently IL-1-induced PGE2 formation (IC50= 0.5 nM) and IL-1-induced human thymocyte (TF-1 cell) proliferation (IC50=

KME-2780 (KME2780) is a potent and selective dual IRAK1 and IRAK4 (IRAK1/4) inhibitor with IC50 of 19 and 0.5 nM, respectively.

KME-3859 is a potent, selective IRAK4 inhibitor with IC50 of 5 nM, 100-fold selective over IRAK1.

TJ-M2010-2 is a small molecule inhibitor of MyD88 homodimerization, interacts with MyD88 TIR domain.

PCC-0105002 is a novel small molecule inhibitor of PSD95-nNOS protein-protein interaction with IC50 of 1.4 uM.

T1059 is a selective inhibitor of eNOS/iNOS with a long-term vasoconstrictive effect in vivo.

ADS032 (ADS-032) is the first, reversible and stable dual NLRP1 and NLRP3 inflammasome inhibitor, inhibits nigericin-induced NLRP3-induced IL-1β secretion from LPS-primed iBMDMs with IC50 of 30 uM.

DFV890 (IFM-2427) is apotent, selective and orally active inhibitor of NLRP3 inflammasome, directly binds to NLRP3 and locks the protein in an inactive conformation,prevents NLRP3 inflammasome assembly in response to sterile danger signals.

FK156 is an immunoactive peptide and a nucleotide-binding oligomerization domain (Nod)-1 ligand agonist.

FK565 is an immunoactive peptide and a nucleotide-binding oligomerization domain (Nod)-1 ligand agonist.

JC2-11 is an anti-inflammasome compound and a pan-inhibitor of the NLRP3, NLRC4, and AIM2 inflammasomes.

JT001 (JT-001) is a potent, highly specific NLRP3 inhibitor, inhibits NLRP3 inflammasome assembly.

JT002 is a potent and selective inhibitor of NLRP3 inflammasome with IC50 of 6 nM (IL-1β production from hPBMCs), inhibits NLRP3 mediated cytokine production and pyroptosis.

ML146 (ML-146, Pubmed CID-1088438) is a selective small molecule NOD1 inhibitor with IC50 of 1.5 uM in NOD1 agonist-stimulated NF-κB reporter assay in HEK293T cells.

NDT-19795 is the carboxylic acid metabolite of selective NLRP3 inhibitor NT-0796, suppresses release of IL-1β in LPS-activated human PBMCs with IC50 of 47 nM.

NLRP3-inhibitory compound 7 (NIC7) is a small-molecule inhibitor of Nod-like receptor family pyrin domain-containing 3 (NLRP3), inhibits NLRP3-mediated activation of caspase 1 along with the secretion of IL-1β, IL-18, and lactate dehydrogenase.

NP3-146 is a small molecule NLRP3 inflammasome inhibitor and an analog of MCC950.

ZYIL1 is an oral small molecule NLRP3 inflammasome inhibitor, exhibits potent (IC50 in nanomolar range) in human whole blood and supresses inflammation caused by the NLRP3 inflammasome.

BMS135 is a small molecule h-PD1/h-PD-L1 interaction inhibitor with IC50 of 79.1 nM, bind specifically to hPD-L1 through a unique mode of action, induces the dimerization of hPD-L1.

BMS136 is a small molecule h-PD1/h-PD-L1 interaction inhibitor with IC50 of 96.7 nM, bind specifically to hPD-L1 through a unique mode of action, induces the dimerization of hPD-L1.

IMMH-010 (YPD-30) is an ester prodrug of YPD-29B, a high potent PD-L1 inhibitor (IC50=0.08 pM), YPD-30 is a potent PD-L1 inhibitor with IC50 of 45.2 nM in HTRF assays.

IMMH-010 maleate (YPD-30) is an ester prodrug of YPD-29B, a high potent PD-L1 inhibitor (IC50=0.08 pM), YPD-30 is a potent PD-L1 inhibitor with IC50 of 45.2 nM in HTRF assays.

MAX10181 (MAX-10181) is an orally active small molecule PD-L1 inhibitor, shows similar efficacy as Durvalumab in the head to head test of human PD-L1 knock-in MC38 cell line in human PD-1 knock-in mice.

YPD-29B is a potent, specific programmed cell death ligand 1 (PD-L1) inhibitor, effectively blocks the binding of PD-1 and PD-L1 with IC50 of 0.08 pM in HTRF protein-protein interaction assays.

LY3023703 is a potent, highly selective microsomal prostaglandin E synthase 1 (mPGES1) inhibitor, dose-dependently inhibits PGE2 production in human whole blood ex vivo.

MPO-0144 (MPO 0144) is a potent, selective mPGES-1 inhibitor (PGE2 IC50=41.77 nM, mPGES-1 IC50=1.16 nM), exhibits potent neuroprotection (ED50=3.0 nM) against 6-OHDA-induced in PC12 cells without significant neurotoxicity (IC50>10 uM).

SZ0232 is a small molecule mPGES-2 (microsomal prostaglandin E synthase-2) inhibitor with IC50 of <1 uM, exhibits beneficial effects on modulating β-cell function and glucose metabolism both in vitro and in vivo.

TAS-204 (TAS204) is a potent, specific hematopoietic prostaglandin D synthase (H-PGDS) inhibitor, inhibits recombinant human H-PGDS with IC50 of 24.0 nM.

TAS-205 (Pizuglanstat, TAS205) is a potent, specific hematopoietic prostaglandin D synthase (H-PGDS) inhibitor with IC50 of 55.8 nM, does not inhibit LPGDS at 100 uM.

UT-11 is a potent microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor, inhibits PGE2 production from human SK-N-AS and murine BV2 cells induced by LPS with IC50 of 0.1 and 2.0 uM, respectively.

HWG-35D is a potent, selective sphingosine kinase 2 (SphK2, SK2) with IC50 of 41 nM, 100-fold selectivity for SK2 over SK1.

SLL3071511 is a novel potent inhibitor of Chikungunya virus (CHIKV) infection with EC50 of 2.91 uM, inhibits sphingosine kinase SK1 and SK2 with Ki values of 0.27 and 0.66 uM, respectively.

SLP9101555 is a potent, selective sphingosine kinase SphK2 with Ki of 90 nM (hSphK2), 200-fold selectivity over SphK1.

ChX710 (ChX0306710) is a small molecule that primes the type I interferon response to cytosolic DNA, which is dependent on the adaptor MAVS and IRF1, but not the IRF3.

DWL-4-140 is a small molecule inhibitor of cyclized nucleotide-binding domain (CBD) of STING, selectively inhibits DNA-mediated IFNβ responses with IC50 of 617 nM.

HB3089 (HB-3089) is a novel potent, highly specific STING agonist, dose-dependently activates interferon-stimulated gene (ISG) signaling in THP1-Dual reporter cells with EC50 of 1-10 uM.

LB244 (LB-244) is a highly potent, selective and irreversible STING antagonist, blocks STING oligomerization and inhibits STING signaling THP1 dual cells with IC50 of 0.8 uM.

MK-1454 (Ulevostinag) is a novel cyclic dinucleotide STING agonist with robust tumor cytokine upregulation and effective antitumor activity.

SB24011 (SB 24011) is a selective small molecule inhibitor of the STING-TRIM29 interaction with IC50 of 3.85 uM in luciferase complementation assays, enhances cGAMP-mediated STING immunity.

SHR1032 is a novel small molecule non-cyclic di-nucleotide STING agonist, exhibits significantly high affinity binding to STING and cellular reporter assay (EC50=30 nM).

AZD8848 (AZD 8848) is a potent, selective TLR7 agonist with EC50 of 4 nM for induction of IFNα from human PBMCs and an IC50 of 0.2-1.0 nM for inhibition of IL-5.

Diprovocim-X is a potent human and murine TLR1/TLR2 agonist with EC50 of 0.14 nM (hTLR1/TLR2) and 0.75 nM (m TLR1/TLR2), respectively.

E014 is a potent, selective TLR7 agonist with EC50 of 69 nM in Ramos Blue reporter assays, >500-fold selective for TLR7 over TLR8.

E567 is a small moleculeTLR2 signaling inhibitor with anti-viral activity, efficiently inhibits both LCMV and HSV-1 induced cytokine responses in both human and mouse cell cultures.

E6742 (E6742) is a potent, selective, dual TLR7/8 inhibitor with binding Kd of 1.7 uM/37 nM in ITC assays, respectively, inhibits TLR7/8 agonist CL097 induced reporter activation with IC50 values of 22, 68, and 3.0 nM for hTLR7, mTLR7, and hTLR8, respecti

MHV370 (MHV-370) is a potent, selective, orally bioavailable inhibitor of Toll-like receptors 7 and 8 (TLR7/8) with IC50 of 1.1 and 4.5 nM in cell-based assays.

SZU101 is a small molecule TLR7 agonist that directly activates, induces reporter activity (23-fold) in a TLR7-NF-kB reporter system expressed in HEK-293 cells TLR7 signalling.

SZU-106 is a small molecule TLR7 agonist, selectively activates TLR7 and increases the expression of SEAP by activating the NF-κB pathway.

ABBV-712 is a potent, selective inhibitor of tyrosine kinase 2 (TYK2) with EC50 of 0.01 uM, binds and stabilizes the pseudokinase (JH2) domain of TYK2.

ABT-317 (ABT317) is a potent, selective JAK1 inhibitor, inhibits IL-6-stimulated pSTAT3 (TF-1 cells, IC50=16 nM) and IL-2-stimulated pSTAT5 (T-blasts, IC50=30 nM).

ATI-1777 is a potent, selective and ATP-competitive JAK1/3 inhibitor with IC50 of 1.5/3.6/7.1/19.0 nM for JAK1/JAK2/JAK3/TYK2, respectively.

AZD0449 (AZD-0449) is a potent and highly selective JAK1 inhibitor with IC50 of 2.4 nM, displays >50-fold selectivity over TYK2 and JAK2, and no inhibition against JAK3.

CPL409116 (CPL 409116) is a potent, competitive, dual JAK and ROCK inhibitor with IC50 of 0.95/5.36//0.87/110.6/106.7 nM for JAK1/JAK2/JAK3/ROCK1/ROCK2, respectively.

MMT3-72 is a gastrointestinal locally-activating Janus kinase (JAK) inhibitor, readily converted to MMT3-72-M2 in the colon contents (JAK1 IC50=10.8 nM, JAK2 IC50=26.3 nM and TYK2 IC50=91.6 nM).

QL-1200186 is a potent, highly selective allosteric inhibitor of tyrosine kinase 2 (TYK2) with IC50 of 0.06 nM, targets pseudokinase regulatory domain (Janus homology 2, JH2) of the TYK2 protein.

A potent, selective, orally active JAK1/JAK2 inhibitor with IC50 of 3.3/2.8 nM, respectively.

YLIU-4-105-1 is a novel type II JAK2 inhibitor, binds to JAK2 kinase domain (JH1), show potential for overcoming acquired resistance to ruxolitinib.

Z583 is a potent, highly selective JAK3 inhibitor with IC50 of 0.1 nM, 4500-fold selectivity over other JAK subtypes.

DR-1-55 (DR-155) is a selective STAT3 inhibitor that covalently modifies a cysteine in the SH2 domain of STAT3.

K1836 is a small molecule Stattic analog inhibitor of STAT3 signalling.

LLL12B is a selective STAT3 inhibitor that suppresses Th17 development, specifically inhibits STAT3 and suppresses Th17 differentiation and expansion.

MC0704 (MC-0704) is a novel synthetic STAT3 pathway inhibitor, exhibits potential antitumor activity in vitro and in vivo models in docetaxel-resistant TNBC cells.

MNS1-Leu is a novel pyrazole-based small molecular inhibitor of STAT3 pathway, potently inhibit IL-6-induced STAT3 phosphorylation at 10 μM in dBT114 cells.

MNS1-MV is a novel pyrazole-based small molecular inhibitor of STAT3 pathway, potently inhibit IL-6-induced STAT3 phosphorylation at 10 μM in dBT114 cells.

ODZ10117 is a small molecule inhibitor of STAT3, effectively inhibits the level of tyrosine phosphorylated STAT3 in various cancer cell lines.

SF-1-088 is a small molecule STAT5-SH2 domain inhibitor with Ki of 8.3 uM (Stat5b), shows no affinity for Stat1 and Stat3 (Ki>25 uM).