TUG-469 is a selective free fatty acid receptor 1 (FFA1/GPR40) agonist with an EC50 value of 19 nM. TUG-469 is >200-fold selective for FFA1 over FFA4. TUG-469 significantly improves glucose tolerance in pre-diabetic mice. TUG-469 can be used for the research of diabetes.

TUG-499 is a selective free fatty acid receptor 1 (FFAR1 or GPR40) (Free Fatty Acid Receptor) agonist with a pEC50 of 7.39. TUG-499 exhibits >100-fold selectivity over the related receptors FFA2, FFA3, and the nuclear receptor PPARγ and other diverse receptors, ion channels, and transporters. TUG-499 can be used for the research of type 2 diabetes.

(R,S)-3,5-DHPG hydrochloride (DHPG, Dihydroxy phenylglycine) is a salt of free amino acid dihydroxy phenylglycine (DHPG) which acts as a selective and potent agonist of group I metabotropic glutamate receptors (mGluR) (mGluR 1 and mGluR 5).

CP-135807 is an orally active and selective 5-HT1D agonist (IC50=3.1 nM), bovine). CP-135807 mediates central psychoactivity and can be used in antidepressant research.

RS-102221 is a selective 5-HT2C receptor antagonist (Ki=10 nM). RS-102221 shows nearly 100-fold selectivity for the 5-HT2C receptor as compared to the 5-HT2A and 5-HT2B receptors. RS-102221 can promote the differentiation of new nerve cells. RS-102221 increases food-intake and weight-gain in rats.

3-AQC, a piperazinylquinoxaline derivative, is a potent and competitive 5-HT3 receptor antagonist.

SB699551 is a potent, selective 5-HT5A receptor antagonist with pKi of 8.3, >100-fold selectivity over 5-HT1B/D, 5-HT2A, 5-HT2C, 5-HT1A and 5-HT7 receptors. SB699551 also is a novel PSMD4/Rpn10 inhibitor, decreases cell viability in MM cell lines.

PSB11 hydrochloride is an antagonist with reverse excitatory activity for human A3 Adenosine Receptor with high affinity (Ki=2.3 nM).

Butaxamine (Butoxamin) is a potent, selective and orally active β2-adrenoceptor antagonist. Butaxamine shows antiosteoporotic activity.

LAS190792 (AZD8999) is a potent muscarinic antagonist and β2-adrenoceptor agonist with pIC50 8.9, 8.8, 8.8, 9.2, 8.2, 7.5, 9.1, 5.6 for M1, M2, M3, M4, M5, β1, β2, β3, respectively. LAS190792 can be used as a bronchodilator.

Abanoquil (U-K52046), an potent and selective α-1 adrenoceptor antagonist, is an anti-arrhythmic agent. Abanoquil can be used for erectile dysfunction research.

L-796568 is a β(3)-adrenergic receptor agonist. L-796568 can be used for the research of obesity.

GW 833972A is a selective CB2 receptor agonist. GW 833972A inhibits induced nerve depolarization and citric acid-induced cough in animal models.

Pirnabine is a cannabinoid receptor ligand. Pirnabine can be used for the research of glaucoma.

PD 168568 is a orally active and potent dopamine receptor D4 (DRD4) antagonist. PD 168568 contains an isoindolinone and is selective for the D4 receptor versus D2 and D3, with Ki values of 8.8, 1842, and 2682 nM, respectively. PD 168568 can be used for glioblastoma (GBM) research.

PAOPA, an analog of L-proline-l-leucine-glycine amide (PLG) peptide, is an allosteric modulator of Dopamine D2 Receptor. PAOPA can effectively reduce behavioral abnormalities in rodent models of schizophrenia. PAOPA increases the high affinity dopamine D2 receptor and promotes its binding to agonists.

LP-471756 is a potent GPR139 antagonist with an IC50 value of 640 nM. LP-471756 inhibits LP-360924-stimulated cAMP production.

Immepip is a H3 agonist. Immepip can reduce cortical histamine release. Immepip can be used for the research of neurological diseases.

ST-1006 is a potent histamine H4 receptor agonist with a pKi value of 7.94. ST-1006 has anti-inflammatory effect.

PTAC oxalate is a selective muscarinic receptor ligand. PTAC oxalate is an partial agonist of M2 and M4 but antagonist of M1, M3, and M5 (Ki values of 0.2-2.8 nM for hM1-5 in CHO cells). PTAC oxalate alleviates the mechanical allodynia on the neuropathic pain and has antidepression effects.

Afacifenacin (SMP-986) is a potent and orally active muscarinic receptor antagonist. Afacifenacin inhibits the bladder afferent pathway through the sodium-channel blockade, increasing volume, and reducing the frequency of urination and incontinence. Afacifenacin has the potential for the research of overactive bladder (OAB).

Eucatropine is a potent muscarinic acetylcholine receptor (mAChR) inhibitor with an IC50 value of 0.583 μM. Eucatropine is an anticholinergic agent.

L-CCG-I is an extended isomer of conformationally restricted glutamate analog. L-CCG-I also is a potent agonist for mGluR2 with an EC50 value of 0.3 nM. L-CCG-I can be used for the research of mGluR family.

MTEP is a potent, non-competitive and highly selective mGluR5 antagonist, with an IC50 of 5 nM and a Ki of 16 nM. MTEP shows antidepressant and anxiolytic-like effects. MTEP can be used for Parkinson's disease research.

(S,S)-J-113397 is an isomer of J-113397. J-113397 is an Opioid Receptor antagonist.

Naloxonazine is a potent and selective opiate mu-1 antagonist that can also affect leishmania by regulating host coding function.

(Rac)-SNC80 is a racemate of SNC80. SNC80 (NIH 10815) is a potent, highly selective and non-peptide δ-opioid receptor agonist with a Ki of 1.78 nM and an IC50 of 2.73 nM. SNC80 shows antinociceptive, antihyperalgesic and antidepressant‐like effects. SNC80 has the potential for multiple headache disorders treatment.

SC 51089 free base is a selective antagonist of prostaglandin E2 EP1 receptor, with Kis of 1.3, 11.2, 17.5, and 61.1 μM for EP1, TP, EP3, and FP receptors, respectively. SC 51089 free base exhibits neuroprotective activity.

Thromboxane A2 (TXA2) is a prostanoid mediator produced by the metabolism of Arachidonic acid through the cyclooxygenase pathway. Thromboxane A2 activates the thromboxane-prostanoid (TP) receptors. Thromboxane A2 is a potent vasoconstrictor eicosanoid. Thromboxane A2 (TXA2) leads to potent vasoconstriction by stimulation of smooth muscle cells. Thromboxane A2 acts as s tonic immunoregulator to regulate adaptive immune responses.

AS604872 is an orally active, potent and selective prostaglandin F2α receptor (FP) antagonist with a Ki of 35 nM in humans, 158 nM in rats and 323 nM in mice. AS604872 inhibits contractions and delays labour.

AL-3138 (11-Deoxy-16-fluoro PGF2α) is a prostaglandin F2 alpha (PGF2alpha) analogue that antagonises FP prostaglandin receptor-mediated inositol phosphate production.

I-SAP is a radioiodinated TXA2/PGH2 receptor antagonist. The bind between I-SAP and the receptors, is inhibited by the histidine modifying reagent diethyl-pyrocarbonate (DEPC).

Fingolimod phosphate (FTY720 phosphate) is an orally active sphingosine 1-phosphate (S1P) receptor agonist. Fingolimod phosphate can promote the neuroprotective effects of microglia. Fingolimod phosphate can be used for the research of multiple sclerosis and neurologic diseases.

ONO-0740556 is a potent Gi-coupled human lysophosphatidic acid receptor 1 (LPA1) agonist with an EC50 value of 0.26 nM.

Evocalcet (KHK7580) is an novel oral calcimimetic agent which acts via allosteric activation of the calcium sensing receptor (CaSR). Evocalcet (0, 20 and 60 nM) dose-dependently increases cytoplasmic [Ca2+] concentrations with an EC50 value of 92.7 nM in hCaR-HEK293 cells.

PF-07054894 is a potent CCR6 antagonist. PF-07054894 targets G protein-coupled receptor (GPCR). PF-07054894 can be used in research of inflammatory bowel disease.

UCM1306 is a potent and orally active human dopamine D1 receptor allosteric modulator (PAM). UCM-1306 increases the endogenous dopamine (DA) maximal effect both in human and mouse D1 receptors. UCM-1306 is not only for improving motor symptoms but also for addressing the key comorbid cognitive impairment associated with long-term Parkinson’s disease (PD).

Macimorelin (EP-1572) acetate, a GH secretagogue, is an orally active GHSR agonist. Macimorelin acetate stimulates GH release. Macimorelin acetate can be used in the research of adult growth hormone deficiency (AGHD), and Cancer anorexia-cachexia syndrome (CACS).

Muscarine ((+)-Muscarine) is a toxin that can stimulate the parasympathetic nervous system. Muscarine is an agonist of muscarinic acetylcholine receptor (mAChR).

FR 113680 is a tripeptide substance P antagonist that interacts selectively with the NK1 neurokinin receptor.

JNJ-40411813 is a novel potent positive allosteric modulator of mGlu2 with EC50 of 147 nM. JNJ-40411813 displays >30-fold selectivity over mGlu1 and mGlu3-8, 10-fold over 5-HT2A. JNJ-40411813 displays an optimal interplay between potency, selectivity, favorable ADMET/PK and cardiovascular safety profile, and central EEG activity; has been investigated in the clinic for schizophrenia and anxious depression disorders.

Norepinephrine (Levarterenol; L-Noradrenaline) hydrochloride is a potent agonist of adrenergic receptor (AR). Norepinephrine activates α1, α2, β1 receptors.

MEN 11270, a cyclic decapeptide, is a B2 kinin receptor antagonist. MEN 11270 bound with high-affinity to the B2 kinin receptor constitutively expressed by WI38 human fibroblasts, inhibiting 3H-bradykinin (BK) with pKi of 10.3.

MR120 (CCR6 antagonist 1b) is a potent, selective CCR6 antagonist, disrupts the CCL20-induced chemotaxis of CCR6+CD4+ T cells.

CB-25 is a ligand of CB1 cannabinoid receptors, acting as a partial agonist. CB-25 enhances Forskolin-induced cAMP formation in cancer cells but not hCB1-CHO cells.

25B-NBOMe is a highly selective 5-HT2A receptor agonist with Ki of 0.05 nM, 100-fold selective over 5-HT2C (Ki=4.6 nM).

AS2030680 is a potent, selective and brain-penetrating 5-HT5A receptor antagonist with Ki of 0.58, 1.1 and 2.6 nM against human, rat, mouse 5-HT5A receptors, respectively.

AS2674723 is a potent, selective and brain-penetrating 5-HT5A receptor antagonist with Ki of 0.75, 0.67 and 1.9 nM against human, rat, mouse 5-HT5A receptors, respectively.

AS5736 is a potent, selective and brain-penetrating 5-HT5A receptor antagonist with Ki of 3.6, 1.7 and 4.4 nM against human, rat, mouse 5-HT5A receptors, respectively.

CSTI-300 (SMP-100) is a potent, selective 5-HT3 receptor partial agonist with high affinity for human and rat 5-HT3 receptor (Ki=2.0 nM).

E-6801 is a potent, selective 5-HT6 receptor partial agonist of 5-HT6 receptor with pKi of 8.46, cAMP formation EC50 of 8.02.

NH300094 is a potent antagonist of 5-HT receptors and dopamine receptors with IC50 of 0.47 nM, 1.04 nM, 11.71 nM and 31.55 nM for 5-HT2A, D2L, D2S and D3 receptors, respectively.

NU-1223 is a β carboline analog of alstonine and serotonin 5-HT2C receptor agonist, blocks phencyclidine and amphetamine-induced hyperactivity in subchronic phencyclidine mice.

PZ-1922 is a potent, triple-acting 5-HT6R/5-HT3R antagonist and MAO-B reversible inhibitor with Ki of 17/0.45 nM (5-HT6R/5-HT3R), and pIC50 of 8.93 for MAO-B.

TZB-30878 is a potent, selective, orally bioavailable 5-HT1A agonist and 5-HT3 antagonist, selectively binds to human 5-HT1A and 5-HT) receptors with Kd values of 0.68 and 8.90 nM, respectively.

VU6047534 is a selective, peripherally restricted 5-HT2B partial agonist with IC50 of 480 nM in radioligand binding assays.

BnOCPA is a potent and powerful analgesic and a highly selective and potent, full agonist at human adenosine A1 receptors (A1Rs) with pEC50 of 7.23 in a NanoBRET agonist binding assay.

I-ABOPX (BW-A522) is a potent, selective A3 adenosine receptor antagonist with high affinity for both the ovine (Ki=3 nM) and human (Ki=19 nM) A3 receptors.

KF-26777 (KF26777) is a potent and selective adenosine A3 receptor antagonist with Ki of 0.2 nM (human A3 receptor).

MRS7935 is a potent, selective positive allosteric modulator (PAM) of A1 adenosine receptor (A1AR) with EC50 of 1.43 uM.

OT-7999 (OT7999) is a potent and selective adenosine A3 receptor antagonist with Ki of 0.61 nM (human A3 receptor) in radioligand binding assays.

QAF-805 (QAF805) is a potent, dual adenosine-A2B receptor and adenosine-A3 receptor antagonist with Ki of 3.4 nM (A2B).

TRR469 is a potent, selective adenosine A1 receptor (A1AR) positive allosteric modulator with pKb of 5.36, exhibits anti-nociceptive properties in acute and neuropathic pain models in mice.

AS408 is a negative allosteric modulator of the β2-adrenergic receptor (β2AR) for both G-protein activation and arrestin recruitment (pKB=6.8, [35S]GTPγS binding assays), binds to a pocket formed by the membrane-facing surface of TM3 and TM5.

Difluorophenyl Quinazoline (DFPQ, AP-06-202) is a selective, biased, negative allosteric modulator of β-arrestin recruitment to the β2AR, without effect on on β2AR coupling to Gs.

L-771688 (L-771,688, SNAP 6383) is a potent and selective alpha1A (α1A)-adrenoceptor antagonist with binding Ki of 0.13 nM to α1-adrenoceptors in human prostate tissue.

A potent, highly selective α2-adrenoceptor agonist with Ki of 1.08 nM.

Tasipimidine is a potent, selective and orally active human α2A-adrenoceptor agonist with pEC50 of 7.57, >100-fold selectivity over α2B-and α2C-adrenoceptors and the rodent α2D-adrenoceptor.

ZD7114 (ICI D7114) is a potent, selective beta-adrenoceptor agonist, selectively stimulates brown fat and increases whole-body oxygen consumption.

Forasartan (SC-52458) is a potent, specific, competitive and reversible angiotensin II receptor (AT1 receptor) antagonist with binding Ki value of 2.9 nM.

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.

Protokylol hydrochloride(Caytine hydrochloride, JB-251 hydrochloride) is a salt form of protokylol and is an agonist of β-adrenergic receptor. Protokylol hydrochloride is also used as a bronchodilator.