Omidenepag Isopropyl (DE-117, OMDI) is the prodrug of Omidenepag, which is a potent, selective agonist human EP2 receptor; demonstrates excellent IOP-lowering activities following ocular administration in ocular normotensive monkeys, Omidenepag Isopropyl (OMDI) is a clinical candidate for the treatment of glaucoma.

Ondansetron is a serotonin 5-HT3 receptor antagonist used mainly as anantiemetic (to treat nausea and vomiting), often following chemotherapy.

ONO-7300243 is a novel, potent LPA1(Lysophosphatidic Acid Receptor) antagonist with an IC50 of 160 nM.

ONO-AE3-208(AE 3-208) is an EP4 antagonist; suppresses cell invasion, migration, and metastasis of prostate cancer.

Orally active and specific inhibitor of human hematopoietic prostaglandin D synthase (H-PGDS) (IC50 = 6 μM). Antiallergic and anti-inflammatory.

Org 27569 is an allosteric modulator of cannabinoid CB1 receptor, induces a CB1 receptor state that is characterized by enhanced agonist affinity and decreased inverse agonist affinity.

Otenabant (CP945598) is a recently discovered selective, high affinity, competitive CB1 receptor antagonist with Ki of 0.7 nM.

Ozanimod (RPC1063) is a selective S1P1R modulator

Paliperidone (9-hydroxyrisperidone) is a dopamine antagonist of the atypical antipsychotic class of medications.

A serotonin 5-HT3 receptor antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV). It is an antiemetic.

Palosuran (ACT-058362) is a new potent and specific antagonist of the human UT receptor with an IC50 of 3.6±0.2 nM.

Pardoprunox hydrochloride is a novel partial dopamine D2 and D3 receptor agonist and serotonin 5-HT1A receptor agonist, D2 (pKi = 8.1) and D3 receptor (pKi = 8.6) partial agonist and 5-HT1A receptor (pKi = 8.5) full agonist.

Pardoprunox(SLV-308) is a novel partial dopamine D2 and D3 receptor agonist and serotonin 5-HT1A receptor agonist; D2 (pKi = 8.1) and D3 receptor (pKi = 8.6) partial agonist (IA = 50% and 67%, respectively) and 5-HT1A receptor (pKi = 8.5) full agonist (IA

PBI-4050 (Setogepram, PBI4050) is a synthetic analog of a medium-chain fatty acid that displays agonist and antagonist ligand affinity toward GPR40 and GPR84, respectively.

PBI-4050 (Setogepram, PBI4050) is a synthetic analog of a medium-chain fatty acid that displays agonist and antagonist ligand affinity toward GPR40 and GPR84, respectively.

PCC0104005 (PCC-0104005) is a novel modulator of serotonin, dopamine, and noradrenaline receptors, including partial agonism at dopamine D2, D3, D4, serotonin 5-HT1A, and 5-HT2A receptors and antagonism at 5-HT2B, 5-HT6, and 5-HT7 receptors.

PCO371 is a novel, orally active small molecule that acts as a full agonist of PTHR1.

PD 123319 is a potent, selective AT2 angiotensin II receptor antagonist with IC50 of 34 nM.

PD-168077 maleate is a selective dopamine D4 receptor agonist, with a Ki of 9 nM.

Pemirolast Potassium (BMY 26517) is a histamine H1 antagonist and mast cell stabilizer that acts as an antiallergic agent.

PF-00446687 hydrochloride (PF-446687) is a potent, selective melanocortin-4 receptor (MC4R) agonist with EC50 of 12 nM.

PF-00446687(PF-446687) is a potent, selective melanocortin-4 receptor (MC4R) agonist with EC50 of 12 nM.

PF-04418948 is an orally active, potent, and selective EP2 receptor antagonist (IC50 = 16 nM).

PF-04995274 is a 5-HT4 receptor partial agonist. It thought to act centrally as a pro-cognitive agent that being developed for the treatment of Alzheimer's disease (AD).

PF-06764427 (PF06764427) is a potent, selective M1 muscarinic acetylcholine receptor (mAChR) positive allosteric modulator with EC50 of 55 nM, has no measurable agonist or PAM activity at the M2-M5 receptors at 10 uM.

PF-06827443 (PF06827443) is a potent, orally bioavailable, and CNS-penetrant M1-selective positive allosteric modulator (PAM) with EC50 of 47 nM, shows no activity against M2-M5 at 10 uM.

PF-3274167 is a high-affinity nonpeptide oxytocin receptor (OTR) antagonist, with Ki of 9.5 nM.

PHCCC is a Group I metabotropic glutamate receptor antagonist (IC50 ~ 3 μM).

Pheniramine Maleate ia an antihistamine and vasoconstrictor.

Phentolamine Mesylate is a nonselective alpha-adrenergic antagonist.

Phenylbiguanide is a 5-HT3 receptor selective agonist with an EC50 of 3.0±0.1 μM.

Piboserod (SB 207266) is a selective 5-HT(4) receptor antagonist.

Pimavanserin(ACP-103) is a potent and selective 5-HT2A receptor inverse agonist with mean pIC50 of with 8.7 in the cell-based functional assay.

Piperoxan hydrochloride is an α2 adrenoceptor antagonist.

Pirmenol hydrochloride inhibits IK.ACh by blocking muscarinic receptors. The IC50 of Pirmenol for inhibition of Carbachol-induced IK.ACh is 0.1 μM.

Pitolisant Hcl(BF2.649;Ciproxidine ) is a novel, potent, and selective nonimidazole inverse agonist at the recombinant human H3 receptor (Ki=0.16 nM).

Plerixafor is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM, respectively.

Plerixafor octahydrochloride(AMD3100 8HCL) is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM, respectively.

Ponesimod(ACT-128800) is an orally active, selective sphingosine-1-phosphate receptor 1 (S1P1) immunomodulator with EC50 of 5.7 nM.

Potent and selective 5-HT6 receptor antagonist (pKi = 8.6).

Potent, selective CB1 cannabinoid receptor antagonist/inverse agonist (Ki values are 12 and 4200 nM for CB1 and CB2 receptors respectively). Increases locomotor activity following systemic administration in vivo. Analog of SR141716A (Ki = 14 nM).

Pramipexole is a dopamine agonist of the non-ergoline class indicated for treating Parkinson's disease (PD) and restless legs syndrome (RLS).

Pramipexole is a partial/full D2S, D2L, D3, D4, receptor agonist with a Ki of 3.9, 2.2, 0.5, 5.1 nM.

Pravadoline is a cannabimimetic aminoalkylindole agonist of the cannabinoid receptors and an inhibitor of Cox-1 and Cox-2, demonstrating powerful analgesic effects through the combination of these actions.

PRE-084 hydrochloride is a high affinity, selective σ1 agonist (Ki values are 2.2 and 13091 nM for σ1 and σ2 receptors respectively).

Preladenant(SCH 420814) is a potent and selective antagonist at the adenosine A2A receptor.

PrNMI is a peripherally restricted cannabinoid 1 receptor (CB1R) agonist, significantly alleviates spontaneous pain behaviors in the animals.

Prochlorperazine is a dopamine (D2) receptor antagonist that belongs to the phenothiazine class of antipsychotic agents. It is also a highly potent typical antipsychotic.

Prostaglandin E2 is a hormone-like substance that participate in a wide range of body functions such as the contraction and relaxation of smooth muscle, the dilation and constriction of blood vessels, control of blood pressure, and modulation of inflammation.

Prucalopride is a selective, high affinity 5-HT receptor agonistfor 5-HT4a and 5-HT4b with Ki of 2.5 nM and 8 nM, respectively.

Prucalopride succinate is a selective, high affinity 5-HT4 receptor agonist with pKi of 8.6/8.1 for 5-HT4a/4b.

PRX-08066 is a selective 5-hydroxytryptamine receptor 2B (5-HT2BR, IC50= 3.4 nM) antagonist that causes selective vasodilation of pulmonary arteries.

PZM21 is a potent and selective μ opioid receptor agonist with an EC50 of 1.8 nM.

R15A inhibitor.

Ramelteon is a novel melatonin receptor agonist for human MT1 and MT2 receptors and chick forebrain melatonin receptors with Ki of 14 pM, 112 pM and 23.1 pM, respectively.

Ramosetron Hydrochloride(YM060 Hydrochloride) is a serotonin 5-HT3 receptor antagonist for the treatment of nausea and vomiting.

Reparixin(DF 1681Y) is an inhibitor of CXCL8 receptor, also inhibit CXCR1 and CXCR2 activation, which has been shown to attenuate inflammatory responses in various injury models.

RG7090(CTEP Derivative,Basimglurant, RO4917523) is a negative modulator of metabotropic glutamate receptor subtype 5 (mGluR5; GRM5).

Rimonabant Hcl(SR141716A) is a selective central cannabinoid (CB1) receptor inverse agonist with Ki of 1.8 nM.

Rimonabant(SR141716) is a selective central cannabinoid (CB1) receptor inverse agonist with Ki of 1.8 nM.

Risperidone(R 64 766) is a serotonin 5-HT2 receptor blocker(Ki= 0.16 nM) and a potent dopamine D2 receptor antagonist(Ki= 1.4 nM).

Rizatriptan Benzoate is a selective serotonin 5-HTID receptor agonist which is structurally derived from tryptamine.

Ro 46-2005 is a novel synthetic non-peptide endothelin receptor antagonist, inhibits the specific binding of 125I-ET-1 to human vascular smooth muscle cells (ETA receptor) with IC50 of 220 nM.

RO5028442 is a highly potent and selective Brain-Penetrant Vasopressin 1a (V1a) receptor antagonist with Kis of 1 nM (hV1a) and 39 nM (mV1a).

Rotigotine is dopamine D2 and D3 receptor agonist. Ki values are 13 and 0.71 nM for D2 and D3 respectively. Rotigotine also has significant affinity for 5-HT1A and adrenergic α2B receptors. Rotigotine exhibits antiparkinsonian acitivity.

Roxatidine Acetate Hydrochloride is a histamine H2-receptor antagonist used in ulcer treatment. This compound has been found to inhibit platelet function in vitro.

RS 102895 hydrochloride is a chemokine receptor CCR2 antagonist.

RS 17053 hydrochloride is a potent and selective α1A adrenoceptor antagonist, with a pKi value of 9.1 in native cell membrane and a pA2 value of 9.8 in functional assays.

RS-127445 is a potent and selective antagonist at the serotonin 5-HT2B receptor, with around 1000x selectivity over the closely related 5-HT2A and 5-HT2C receptors.

RTI-13951-33 is a potent, selective, brain-penetrant agonist of the orphan receptor GPR88 with EC50 of 25 nM in in vitro cAMP functional assay.

Rupatadine is a dual histamine H1 and PAF antagonist

S 38093 is a novel brain-penetrant antagonist/inverse agonist of H3 receptors.

S1p receptor agonist 1 is an S1P receptor agonist extracted from patent WO 2015039587 A1, compound example 2.

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

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

Salbutamol is an agonist of the β2-adrenergic receptor (β2-AR; Kd = 759 nM in a radioligand binding assay using CHO cells expressing the human receptor).

Salmeterol Xinafoate is a long-acting β2-adrenergic receptor agonist with anti-inflammatory effects, used in the treatment of asthma symptoms and chronic obstructive pulmonary disease (COPD) symptoms.

Salmeterol Xinafoate is a long-acting β2-adrenergic receptor agonist with anti-inflammatory effects, used in the treatment of asthma symptoms and chronic obstructive pulmonary disease (COPD) symptoms.

SAR-100842 (SAR100842) is a potent, selective, orally available antagonist of the Lysophosphatidic Acid 1 Receptor (LPA1 receptor) with IC50 of 31 nM in β-arrestin assays.

Sarpogrelate(MCI-9042) hydrochloride, a selective 5-HT2 antagonist, has been widely used as an anti-platelet agent for the treatment of PAD.

SB 222200 is a selective, reversible and competitive antagonist of human NK-3 receptor(Ki=4.4 nM) that effectively crosses the blood-brain barrier.

SB 242084 is a potent and selective antagonist of 5-HT2C receptor.

SB225002 is a potent, and selective CXCR2 antagonist with IC50 of 22 nM for inhibiting interleukin IL-8 binding to CXCR2, > 150-fold selectivity over the other 7-TMRs tested.

SB269970 is a potent and selective 5-HT7 receptor antagonist.

SB271046 Hcl is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 8.9.

SB-334867 is a selective non-peptide orexin OX1 receptor antagonist with a pKb value of 7.2.

SB-334867 is a selective orexin-1 (OX1) receptor antagonist.

Potent, brain penetrant, orally active 5-HT6 antagonist. Displays > 200-fold selectivity for 5-HT6 over other 5-HT receptors (pKi values are 9.11, 8.81 and 9.02 for human recombinant, native rat and native human 5-HT6 receptors respectively).

SB408124 is a non-peptide antagonist for OX1 receptor with Ki of 57 nM and 27 nM in both whole cell and membrane, respectively; exhibits 50-fold selectivity over OX2 receptor.

SB-674042 is a potent and selective non-peptide orexin OX1 receptor antagonist (Kd = 3.76 nM); exhibits 100-fold selectivity for OX1 over OX2 receptors.

SB-742457(RVT-101) is a selective 5-HT6 receptor antagonist with potential cognition, memory, and learning-enhancing effects.

SCH 23390 hydrochloride is a potent dopamine receptor D1 antagonist with Ki values of 0.2 and 0.3 nM for the D1 and D5.

SCH 546738 is a novel, potent and non-competitive small molecule CXCR3 antagonist with Ki of 0.4 nM .

SCH-527123 is a potent antagonist of both CXCR1 and CXCR2 with IC50 of 42 nM and 3 nM, respectively.

Seliforant (SENS-111, SENS111) is a novel potent, selective histamine H4 receptor antagonist..

Setipiprant is an orally available, selective CRTH2 antagonist. CRTH2 is a G protein-coupled receptor for PGD2.

Setiptiline is a serotonin receptor antagonist.

Setiptiline(Org-8282) is a serotonin receptor antagonist.

Silodosin(Rapaflo) is an α1-adrenoceptor antagonist with high uroselectivity. Silodosin causes practically no orthostatic hypotension (in contrast to other α1 blockers). Since Silodosin is a highly selective inhibitor of the α1A adrenergic receptor, it ca

Sitaxentan sodium (TBC-11251) is a selective endothelin receptor-A antagonist with IC50 and Ki of 1.4 nM and 0.43 nM, respectively.

SKF 38393 is a partial agonist of the dopamine D1-like receptors D1 and D5 (Kis = 1 and ~0.5 nM, respectively).

SKF 82958 hydrobromide is a D1/D5 receptor full agonist.

SKF38393 HCl is a selective dopamine D1/D5 receptor agonist.

SKI II is a highly selective and non ATP-competitive S1P receptor inhibitor with IC50 of 0.5 μM, while exhibits no inhibitory on other kinases including PI3K, PKCα and ERK2.

Sotalol Hydrochloride is an adrenergic beta-antagonist that is used in the treatment of life-threatening arrhythmias.

SR 48692 is a neurotensin antagonist; selective for NTS1 over NTS2 (apparent affinity, Ke, is 36 nM for NTS1). Competitively inhibits binding of [125I]-neurotensin to HT29 and N1E115 cell membranes (IC50 values are 15.3 and 20.4 nM respectively).

ST-836 Hcl is a dopamine receptor ligand; Antiparkinsonian agent.

Strontium Ranelate is a bone metabolism modulator that inhibits bone resorption while maintaining bone formation. Commonly used as an antiosteoporotic.

Substance P antagonists (SPA).

Substance P free acid is a Sensory neuropeptide and inflammatory mediator. Exerts excitatory effects on central and peripheral neurons, constricts bronchioles and is involved in pain transmission.

Substance P is a Sensory neuropeptide and inflammatory mediator. Exerts excitatory effects on central and peripheral neurons, constricts bronchioles and is involved in pain transmission.

Sufugolix(TAK-013) is a non-peptide, orally-active, selective antagonist of the gonadotropin-releasing hormone receptor (GnRHR) (IC50 = 0.1 and 0.06 nM for affinity and in vitro inhibition, respectively).

Suvorexant (MK-4305) is a potent, selective, and orally bioavailable antagonist of OX1R and OX2R currently under clinical investigation as a novel therapy for insomnia.Suvorexant is an analytical reference standard categorized as a diazepane sedative.Formulations containing suvorexant show abuse potential similar to zolpidem in recreational polydrug users with a history of sedative and psychedelic drug use.2 Suvorexant is regulated as a Schedule IV compound in the United States. This product is intended for use in analytical forensic applications.

TAK-071 is a novel, potent and highly selective muscarinic acetylcholine receptor 1 (M1R) positive allosteric modulator. EC50 of TAK-071 M1R agonist activities is 520 nM.

TAK-615 (TAK615) is a potent, selective, negative allosteric modulator (NAM) of the LPA1 receptor, partially inhibits the LPA response with IC50 of 91 nM (60% at 10 uM) in calcium mobilisation assays..

TAK-875 is a potent, selective and orally bioavailable GPR40 agonist with EC50 of 0.072 μM.

Taranabant is a highly selective cannabinoid-1 (CB1) receptor inverse agonist.

TBPB is an allosteric M1 mAChR agonist(EC50=289 nM) that regulates amyloid processing and produces antipsychotic-like activity in rats.

TCS 1102 is a potent, dual orexin receptor antagonist (Ki values are 0.2 and 3 nM for OX2 and OX1 receptors respectively).

TCS-OX2-29 is a potent and selective OX2 receptor antagonist with IC50 of 40 nM. Displays >250-fold selectivity for OX2 over OX1.

TD-4208 is a potent and selective inhaled muscarinic antagonist with functional lung selectivity and long duration of action in preclinical models of bronchoconstriction.

Tegaserod maleate is a partial agonist of the 5-HT4 receptor; stimulates the peristaltic reflex and accelerates gastrointestinal transit.

Terutroban is a thromboxane/prostaglandin endoperoxide receptor antagonist.

TG6-10-1 is a cell-permeable,highly potent, selective, and competitive antagonist of prostaglandin E2 receptor (EP2, Kb = 17.8 nM).

Thiothixene is a typical antipsychotic.1 It selectively binds to dopamine D2 over D1, D3, and D4 receptors (Kis = 0.417, 338, 186.2, and 363.1 nM, respectively).

Tianeptine is a selective facilitator of 5-HT uptake in vitro and in vivo.

Tianeptine sodium salt is a selective facilitator of 5-HT uptake in vitro and in vivo.

TIC10 isomer(ONC201 isomer) is an isomer of TIC10; TIC10 is a potent, orally active, and stable small molecule that transcriptionally induces TRAIL in a p53-independent manner and crosses the blood-brain barrier.

Ticagrelor is the first reversibly binding oral P2Y12 receptor antagonist, also inhibits CYP2C9 and 4-hydroxylation with IC50 of 10.5 μM and 8.2 μM respectively.

Tiotropium Bromide is a muscarinic acetylcholine receptor (mAChR M) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel. This stops signaling between neurons and leads to muscle relaxation.

TM30089 is a slective CRTH2 antagonist, displaying high antagonistic potency on mouse CRTH2 with low affinity to TP and many other prostanoid receptors including the related anaphylatoxin C3a and C5a receptors.

Tolterodine L-Tartrate is a muscarinic receptor antagonist that is active at all mAChR M subtypes. This compound blocks the opening of ion channels by acetylcholine, which in turn leads to muscle relaxation by blocking neuronal signaling.

Tolvaptan is a selective, competitive arginine vasopressin receptor 2 antagonist with an IC50 of 1.28μM for the inhibition of AVP-induced platelet aggregation.

Topiramate is an anticonvulsant that antagonizes GluR5 receptors and acts as a positive allosteric modulator of GABA receptor-mediated currents.

Tozadenant (SYN-115) is an adenosine A2A receptor antagonist.

TP455 (TP-455) is a highly potent, selective A2A adenosine receptor inverse agonist with IC50 of 1.9 nM in cyclic AMP assays in hA2A CHO cells.

Trifluoperazine Dihydrochloride is a potent dopamine D2 receptor inhibitor used as an antipsychotic and an antiemetic.

TUG-891 is a potent and selective agonist of GPR120 with pEC50 values of 7.36 and 7.77 for human and mouse GPR120, respectively.

U-92016A is an agonist of the serotonin (5-HT) receptor subtype 5-HT1A (Ki = 0.4 nM).

UK 14,304 is a full α2-adrenergic receptor (α2-AR) agonist.

Umeclidinium bromide(GSK573719A) is a muscarinic receptor antagonist which is useful in treatment of chronic obstructive pulmonary disease (COPD).

Vabicaserin hydrochloride is a 5-hydroxytryptamine 2C (5-HT2C) receptor-selective agonist with an EC50 of 8 nM.

Valsartan is a nonpeptide angiotensin II AT1-receptor antagonist with an IC50 ranging from 39.5 to 116 μM. This in turn causes blood vessel dilation.

VCE-004.3 (VCE004.3) is a novel semi-synthetic cannabidiol derivative behaving as a dual PPARγ/CB2 agonist and CB1 receptor modulator, binds and activates PPARγ (IC50=3.5 uM) and CB2 receptors (pKi=6.69) and antagonizes CB1 receptor (pKi=5.61).

Vicriviroc Malate is a potent CKR-5 (CCR5) antagonist with IC50 of 0.91 nM.

Vipadenant(BIIB-014) is an adenosine A2a antagonist with Ki of 1.3 nM; less potent for A1(Ki=69 nM).

Vortioxetine (Lu AA21004) is a multimodal serotonergic agent, inhibits 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT with IC50 of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.

Vortioxetine Hcl (Lu AA21004 Hcl) is a multimodal serotonergic agent, inhibits 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT with IC50 of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.

VU 0238429 is positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5), with an EC50 of 1.16 μM.

VU 0364770 is a positive allosteric modulator(PAM) of mGlu4 with EC50 of 1.1 μM, exhibits insignificant activity at 68 other receptors, including other mGlu subtypes.

VU 0365114 is a mAChR M5 positive allosteric modulator, with an EC50 of 2.7 μM.

VU0152100 is a potent and selective allosteric potentiator of M4 mAChR with an EC50 of 380 ± 93 nM.

VU0357017 hydrochloride is a highly selective M1 agonists that appear to act at an allosteric site to activate the receptor (EC50 = 477 ± 172 nM; pEC50 = 6.37 ± 0.15).

VU0418506 (VU 0418506) is a potent and selective mGlu4 positive allosteric modulator (PAM) with EC50 of 68 nM (hmGlu4).

VU0453595 (VU453595) is a potent, selective M1 positive allosteric modulator (PAM) with EC50 of 3.2 uM (rM1).

VU0467154 (VU 0467154) is a potent, selective M4 mAChR positive allosteric modulator with EC50 of 17.7 nM.

VU0652957 (VU2957, Valiglurax) is a potent, selective mGlu4 positive allosteric modulator (PAM) with EC50 of 64.6 nM in calcium mobilization human mGlu4/Gqi5 assays; showes excellent pharmacokinetics across species (low CLps, %F > 35%), an acceptable CYP profile (>30 uM vs. 3A4, 2D6 and 2C9, 12.5 uM vs. 2C19 and 1.5 uM vs. 1A2), no CYP induction or timedependent inhibition and excellent metabolite coverage across species; also shows attractive predicted human PK parameters (CLps 5-9 mL/min/kg, Vds 1-2 L/kg and t1/2 2-4 hours).

VU6004256 (VU 6004256) is a highly potent, selective M1 muscarinic acetylcholine receptor (mAChR) positive allosteric modulator with EC50 of 155 nM (mouse M1), significant selectivity over M2-M5 (EC50>30 uM).

VU6005649 is a dual mGlu7/8 positive allosteric modulator with EC50s of 649 nM and 2.6 μM for mGlu7 and mGlu8, respectively.

VUF10460 is a non-imidazole histamine H4 receptor agonist; binds to rat H4 receptor with a pKi of 7.46.

VUF11207 is a highly potent CXCR7 agonist. VUF11207 induces recruitment of β-arrestin2 to the CXCR7 followed by internalization of the receptor.

WAY-181187 is a potent and selective 5-HT6 receptor agonist. WAY-181187 possesses high affinity binding (2.2 and 4.8 nM, respectively) at the human 5-HT6 receptor and profile as full receptor agonists (WAY-181187: EC50=6.6 nM, Emax=93%).

WIN 55212-2 (mesylate) is a potent aminoalkylindole cannabinoid (CB) receptor agonist with a Ki of 62.3 and 3.3 nM for human recombinant CB1 and CB2 receptors, respectively.

WZ811 is a novel small molecular and potency CXCR4 antagonist with EC50 of 0.3 nM.

Xanomeline(LY246708) is a selective M1 muscarinic receptor agonist.

XL-001 (XL001) is a novel specific CB2 inverse agonist with Ki of 0.5 nM.

Xylazine Hydrochloride is α2 class of adrenergic receptor agonist.

YL-0919 is a novel synthetic compound with combined high affinity and selectivity for serotonin transporter and 5-HT1A receptors.

Zafirlukast(Accolate)

Zibotentan (ZD4054) is an orally administered, potent and specific ETA-receptor (endothelin A receptor) antagonist (IC50 = 21 nM).

Ziprasidone HCl

ZM 241385 is a Potent A2 adenosine receptor antagonist, with approx 50-fold selectivity for A2A receptors.

Zotepine is a SR-2A and D2DR inhibitor (Ki values are 0.69 and 2.3 nM respectively). Zotepine is also a potent histamine H1 receptor antagonist (IC50 = 8.0 nM).

Mosapride citrate is a gastroprokinetic agent that acts as a selective 5HT4 agonist.

SCH 58261 is a potent and selective A2a adenosine receptor antagonist with Ki of 2.3 nM and 2 nM for rat A2a and bovine A2a, respectively. Cas: 160098-96-4

Desmopressin(DDAVP) acetate is the synthetic analogue of the antidiuretic hormone arginine vasopressin.

Motixafortide (BKT140 4-fluorobenzoyl) is a novel CXCR4 antagonist with an IC50 vakue of ～1 nM.

Carbetocin (Lonactene; Duratocin) is an obstetric drug used to control postpartum hemorrhage and bleeding after giving birth; an agonist at peripheral oxytocin receptors.

CYM5541 is a selective sphingosine-1-phosphate receptor 3 (S1P3) allosteric agonist (EC50 = 72-132 nM).

Oxytocin (α-Hypophamine) acetate is a mammalian neurohypophysial hormone; its actions are mediated by specific, high-affinity oxytocin receptors; ligand of oxytocin receptor.

Vorapaxar (SCH 530348) is a potent and orally active thrombin receptor (PAR-1) antagonist with Ki of 8.1 nM.

Rolapitant (SCH619734) is a potent, selective and orally active neurokinin NK1 receptor antagonist with a Ki of 0.66 nM.

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

Selective dopamine D1-like receptor partial agonist (IC50 values are 19.7 and 2425 nM for binding to D1-like and D2-like receptors respectively). Centrally active following systemic administration in vivo.

Azilsartan medoxomil(TAK 491) is an orally administered angiotensin II receptor type 1 antagonist with IC50 of  0.62 nM, which used in the treatment of adults with essential hypertension.

Ceralifimod is selective, high potent agonist for sphingosine 1-phosphate receptors 1 and 5, with EC50s of 27.3, 334 pM for human S1P receptor 1 and 5, respectively.

BAF312 is a potent and selective agonist of S1P with EC50 value of 0.39nM for S1P1 receptors and 0.98nM for S1P5 receptors, respectively

GSK-2018682 is a sphingosine 1 phosphate receptor (S1PR)-1 agonist potentially for the treatment of multiple sclerosis.

JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist with IC50 of 94 nM, weakly inhibits receptors δ, κ, and μ.

CP-945598 HCl is a potent and selective cannabinoid type 1 receptor antagonist with Ki of 0.7 nM.

AB928 is an orally bioavailable, selective dual adenosine receptor (A2aR/A2bR) antagonist with immunomodulatory activity.

4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol. 4-Hydroxypropranolol hydrochlorid is of comparable potency to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA2 values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties.

Hydroxybupropion is the major active metabolite of Bupropion. Hydroxybupropion is metabolized by CYP2B6.Bupropion is an atypical antidepressant and smoking-cessation agent. Hydroxybupropion inhibits norepinephrine uptake with an IC50 value of 1.7 μM. Hydroxybupropion is also a nACh receptor antagonis tis more potent than Bupropion .

Desmethyl cariprazine is an active metabolite of Cariprazine. Cariprazine, an antipsychotic drug candidate, exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (2.6 nM).

Didesmethyl cariprazine is a metabolite of Cariprazine and acts as the predominant circulating active moiety. Didesmethyl cariprazine has a long half-life of 1-3 weeks. Cariprazine is a antipsychotic drug candidate that exhibits high affinity for the D3 and D2 receptors, and moderate affinity for the 5-HT1A receptor.

Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole. Dehydroaripiprazole has with antipsychotic activity equivalent to Aripiprazole.