Home > Inhibitors & Agonists > GPCR
Cat. No. Product name CAS No.
DC11104 Tildacerfont Featured

corticotropin releasing factor (CRF) antagonist.

1014983-00-6
DC10528 CP 376395 Featured

CP 376395 is a potent and selective CRF1 receptor antagonist (Ki values are 12 and >10000 nM for CRF1 and CRF2 receptors respectively).

175140-00-8
DC9303 Taprenepag(CP-544326) Featured

CP-544326 is a selective prostaglandin EP(2) agonist on intraocular pressure in preclinical models of glaucoma.

752187-80-7
DC9317 CP-809101 (hydrochloride)

CP-809101 Hcl is a potent and selective 5-HT2C receptor agonist with pEC50 of 9.96/7.19/6.81 for human 5-HT2C/5-HT2B/5-HT2A receptors respectively.

1215721-40-6
DC10527 Ciforadenant (CPI-444) Featured

CPI-444 is an orally administered antagonist of the adenosine A2A receptor. It is designed to block the action of adenosine that is produced by tumors.

1202402-40-1
DC9508 CPPHA Featured

CPPHA is a selective positive allosteric modulator of mGluR5 receptor.

693288-97-0
DC11154 CR6086

CR6086 (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.

DC11980 CX 4338

CX 4338 (CX4338, CX-4338) is a potent, selective CXCR2 inhibitor that selectively inhibits CXCR2-mediated recruitment of β-arrestin-2 with IC50 of 6.3 uM.

41609-06-7
DC10203 CXCR2-IN-1

CXCR2-IN-1 is a central nervous system penetrant CXCR2 antagonists with a pIC50 of 9.3.

1873376-49-8
DC8088 CYM5442 Featured

CYM-5442 is a highly-selective S1P1 (Spingosine 1-Phosphate Receptor 1) agonist.

1094042-01-9
DCAPI1536 Cyproheptadine Hydrochloride

Cyproheptadine hydrochloride is a migraine prophylactic and Non-selective SR-2A (5HT2) antagonist. Cyproheptadine hydrochloride is an inhibitor of Histamine H1 Receptor and SR-2C.

41354-29-4
DC11124 D-520

D-520 is a potent, multifunctional D2/D3 agonist with Ki of 41.8 /0.35 nM, modulates aggregation of alpha-synuclein (αSN) and reduces toxicity of preformed aggregates of αSN.

1619269-47-4
DC9689 Danirixin (GSK1325756) Featured

Danirixin(GSK1325756) is a selective CXCR2 antagonist.

954126-98-8
DC12498 S-Darusentan Featured

Darusentan is a potent inhibitor of endothelin signaling and function in both large and small arteries.

171714-84-4
DC7790 CB1-IN-1(BPRCB1184) Featured

CB1-IN-1 (BPRCB1184) is a peripherally restricted CB1R antagonist, with Ki of 0.3 nM and 21 nM for CB1R (EC50 = 3 nM) and CB2R, respectively. IC50 value: 0.3 nM (Ki, CB1R) 21 nM (Ki, CB2R) Target: CB1R in vivo: CB1-IN-1 is a novel peripherally restricted cannabinoid 1 receptor antagonist with significant weight-loss efficacy in diet-induced obese mice. CB1-IN-1 has great potential to ameliorate this related metabolic syndrome.

1429239-98-4
DC10554 DC260126 Featured

DC260126, a small-molecule antagonist of GPR40.

346692-04-4
DC9057 Desloratadine

Desloratadine(Sch34117) is a potent antagonist for human histamine H1 receptor used to treat allergies.

100643-71-8
DC8097 Detomidine hydrochloride

Detomidine hydrochloride produce dose-dependent sedative and analgesic effects, is a nonnarcotic, synthetic α2-adrenergic agonist

90038-01-0
DC4240 Dexmedetomidine hydrochloride Featured

Dexmedetomidine Hydrochloride is an agonist of adrenergic alpha-2 receptor, which is used in veterinary medicine for its analgesic and sedative properties.

145108-58-3
DC4161 Dimebon dihydrochloride

Dimebon is an antihistamine drug.

97657-92-6
DC9863 Dinoprost Featured

Dinoprost(Prostaglandin F2α) is a naturally occurring prostaglandin used in medicine to induce labor and as an abortifacient.

551-11-1
DCAPI1702 Diphemanil methylsulfate Featured

Diphemanil Methylsulfate is a quaternary ammonium anticholinergic, it binds muscarinic acetycholine receptors (mAchR).

62-97-5
DC10683 DL 071-IT hydrochloride

DL 071-IT is a potent non-selective beta-adrenoceptor antagonist.

55104-39-7
DC9323 Dalasetron (Mesylate hydrate)

Dolasetron(MDL-73147) is a serotonin 5-HT3 receptor antagonist used to treat nausea and vomiting following chemotherapy.

878143-33-0
DC11103 Tavapadon Featured

Tavapadon is a potent, orally-bioavailable, selective partial agonist of the dopamine D1 and D5 receptors.

1643489-24-0
DC9109 Doxylamine succinate

Doxylamine is a first generation antihistamine; can be used by itself as a short-term sedative and in combination with other drugs to provide night-time allergy and cold relief.

562-10-7
DC10039 DREADD Agonist 21 Featured

DREADD agonist 21 is a potent muscarinic hM3Dq DREADD agonist (EC50 = 1.7 nM). Highly selective for hM3Dq DREADDs over endogenous hM3 receptors.

56296-18-5
DC11233 DS-8500a

DS-8500a (DS8500a) is a novel potent, selective, orally available GPR119 agonist with EC50 of 51.5 nM in human GPR119-expressing CHO-K1 cells, displays no significant effect on 66 receptors, channels, or transporters.

1371591-51-3
DC8533 E5555 hydrobromide

E5555 shows potent inhibitory effects on human platelet aggregation induced by thrombin and TRAP with IC values of 0.064 and 0.031 μM respectively.

474550-69-1
DC10563 E-7046 Featured

E7046 is an orally bioavailable and specific EP4 antagonist, with IC50 of 13.5 nM and Ki of 23.14 nM, exhibiting anti-tumor activities.

1369489-71-3
DC8323 Eletriptan HBr Featured

Eletriptan HBr is an orally active, selective 5-HT1B/1D receptor agonist.

177834-92-3
DC7772 Elinogrel

Elinogrel is a reversible P2Y12 receptor antagonist for the treatment of acute coronary syndrome and prevention of secondary thrombotic events.

936500-94-6
DC8626 Eluxadoline Featured

Eluxadoline is an orally active mixed μ opioid receptor (μOR) agonist δ opioid receptor (δOR) antagonist.

864821-90-9
DC10869 Olodanrigan(EMA401) Featured

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

1316755-16-4
DC11028 EMD-281014 hydrochloride

EMD-281014 hydrochloride is a potent, highly selective 5-HT2A antagonist with Ki of 0.87 nM, displays little to no affinity for 5-HT2C receptors (Ki=557 nM), human D2 receptors and IKr channels.

443144-27-2
DC11027 EMD-281014

EMD-281014 is a potent, highly selective 5-HT2A antagonist with Ki of 0.87 nM, displays little to no affinity for 5-HT2C receptors (Ki=557 nM), human D2 receptors and IKr channels.

443144-26-1
DC9467 Epinastine Featured

Epinastine(WAL801) is an antihistamine and mast cell stabilizer that is used in eye drops to treat allergic conjunctivitis.

80012-43-7
DC9260 Eptapirone Featured

Eptapirone (F-11,440) is a very potent and highly selective 5-HT1A receptor full agonist of the azapirone family.

179756-58-2
DC9016 Etamsylate

Ethamsylate is a haemostatic drug, also inhibits biosynthesis and action of those prostaglandins.

2624-44-4
DC10040 Etrasimod(APD334) Featured

Etrasimod (APD334) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1(S1P1) receptor with an IC50 value of 1.88 nM in CHO cells.

1206123-37-6
DC9685 Evatanepag (CP-533536) Featured

Evatanepag (CP-533536) is an EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation with EC50 of 0.3 nM.

223488-57-1
DC9073 Famotidine

Famotidine is a competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.

76824-35-6
DC8912 Fesoterodine fumarate Featured

Fesoterodine Fumarate is an antimuscarinic agent and is rapidly de-esterified to its active metabolite 5-hydroxymethyl tolterodine that is a muscarinic receptor antagonist.

286930-03-8
DC11278 Fevipiprant Featured

Fevipiprant(QAW039) is a selective, potent, reversible competitive CRTh2 antagonist with an in vitro dissociation constant KD value of 1.1nM at the CRTh2 receptor and an IC50 value of 0.44 nM for inhibition of PGD2-induced eosinophil shape change.

872365-14-5
DC9175 Fexofenadine Hydrochloride Featured

Fexofenadine is a third-generation antihistamine pharmaceutical drug used in the treatment of allergy symptoms, such as hay fever, nasal congestion, and urticaria.

153439-40-8
DC8936 Fingolimod

Fingolimod(FTY720 free base) is a S1P antagonist with IC50 of 0.033 nM.

162359-55-9
DC9164 Flupenthixol dihydrochloride Featured

Flupenthixol dihydrochloride is a typical antipsychotic of the thioxanthene class that acts as an antagonist at dopamine D2 receptors (Ki = 0.38 nM) and an inverse agonist at serotonin 5-HT2A receptors (Ki = 7 nM).1 It has also been identified as an inhib

51529-01-2
DC7016 JNJ40411813 Featured

For the detailed information of JNJ40411813, the solubility of JNJ40411813 in water, the solubility of JNJ40411813 in DMSO, the solubility of JNJ40411813 in PBS buffer, the animal experiment (test) of JNJ40411813, the cell expriment (test) of JNJ40411813, the in vivo, in vitro and clinical trial test of JNJ40411813, the EC50, IC50,and Affinity of JNJ40411813, Please contact DC Chemicals..

1127498-03-6
DCAPI1596 Metroprolol succinate

For the detailed information of Metroprolol succinate, the solubility of Metroprolol succinate in water, the solubility of Metroprolol succinate in DMSO, the solubility of Metroprolol succinate in PBS buffer, the animal experiment (test) of Metroprolol succinate, the cell expriment (test) of Metroprolol succinate, the in vivo, in vitro and clinical trial test of Metroprolol succinate, the EC50, IC50,and Affinity of Metroprolol succinate, Please contact DC Chemicals..

98418-47-4
DC9333 Formoterol (Fumarate) Featured

Formoterol fumarate(Foradil) is a potent, selective and long-acting β2-adrenoceptor agonist.

43229-80-7
DCAPI1094 Fosaprepitant

Fosaprepitant (MK-0517, L-758,298) is a water-soluble phosphoryl prodrug for Aprepitant which is a NK1 antagonist.

172673-20-0
DC4201 Fosaprepitant dimeglumine Featured

Fosaprepitant (MK-0517, L-758,298) is a water-soluble phosphoryl prodrug for Aprepitant which is a NK1 antagonist.

265121-04-8
DC10814 G-15 Featured

G-15 is a cell-permeable non-steroidal antagonist of GPER (Ki = 20 nM).

1161002-05-6
DC10816 G-36 Featured

G-36 is a cell-permeable non-steroidal antagonist of GPER, inhibiting activation by either 17β-estradiol or the GPER-selective agonist G-1(IC50 = 112 and 165 nM, respectively).

1392487-51-2
DC11122 GAT-100

GAT-100 (GAT100) is a potent, selective CB1R negative allosteric modulator (NAM) with cAMP EC50 and β-arr EC50 of 174 nM and 2.1 nM, does not exhibit inverse agonism.

1663564-42-8
DC11119 GAT-211

GAT-211 (GAT211) is a selective cannabinoid 1 receptor (CB1R) positive allosteric modulator with pKb of 7.26, Arrestin2 EC50 of 775 nM.

102704-40-5
DC11741 GB-110

GB-110 is a potent, non-peptidic agonist of PAR2 that selectively induces PAR2-mediated intracellular Ca(2+) release in HT29 cells with EC50 of 0.28 uM.

1252806-70-4
DC11740 GB-88

GB-88 is a selective, orally available PAR2 antagonist that inhibits PAR2 activated Ca(2+) release with IC50 of 2 uM.

1416435-96-5
DC12342 Gemilukast (ONO-6950)

Gemilukast is an orally active and potent dual cysteinyl leukotriene 1 and 2 receptors (CysLT1 and CysLT2) antagonist, with IC50s of 1.7, 25 nM for human CysLT1 and CysLT2, respectively.

1232861-58-3
DC11246 Ghrelin agonist HM01 Featured

Ghrelin agonist HM01 is a novel potent, orally available ghrelin (GHS-R) agonist with Ki of 1.42 nM (human GHS-R1a), induces potent activation of intracellular calcium signaling with EC50 of 1.25 nM.

1394860-28-6
DC10003 PF-06291874(glucagon receptor antagonists-4) Featured

glucagon receptor antagonists-4 is a highly potent glucagon receptor antagonist.

1393124-08-7
DC8779 Glycopyrrolate Featured

Glycopyrrolate(Glycopyrronium Br) is a muscarinic competitive antagonist used as an antispasmodic.

596-51-0
DC8593 GPR120 Compound A Featured

GPR120 compound A is an orally available, high-affinity agonist of GPR120 (EC50 = ~0.35 µm) that demonstrates potent selectivity over another lipid-sensing G-protein, GPR40 (FFAR1).

1599477-75-4
DC8206 GPR39-C3 Featured

GPR39-C3 is the first potent, selective and orally bioavailable GPR39 agonist with an EC50 ~0.8 nM for human GPR39 and ~0.4 nM for rodent GPR39.

1621175-65-2
DC11143 GPR40 AgoPAM AP5

GPR40 AgoPAM AP5 is a potent, selective GPR40 AgoPAM (full agonist with positive allosteric modulation) with hIP1 EC50 of 0.8 nM, high selectivity over the GPR120 receptor (EC50>30 uM).

1623194-37-5
DC9299 GRA Ex-25 Featured

GRA Ex-25 is an orally active human glucagon receptor antagonist in a transgenic murine pharmacodynamic model at 10 and 30 mpk.

307983-31-9
DC9080 Granisetron HCl

Granisetron Hcl(BRL 43694A) is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.

107007-99-8
DC7422 GSK1292263 Featured

GSK1292263 is a novel GPR119 receptor agonist used for the treatment of type 2 diabetes.

1032823-75-8
DC8577 FFA4 (GPR120) agonist GSK137647A Featured

GSK-137647 is a potent and selective FFA4 (GPR120) agonist (pEC50 values are 6.3, 6.2 and 6.1 at the human, mouse and rat receptor, respectively). Exhibits ≥100-fold selectivity against a panel of 61 targets including FFA1, FFA2 and FFA3.

349085-82-1
DC9705 GSK163090 Featured

GSK163090 is a potent, selective, and orally active 5-HT1A/B/D receptor antagonist with pKi of  9.4/8.5/9.7, and 6.3/6.7 for 5-HT1A/B/D, and dopamine D2/D3, respectively.

844903-58-8
DC10102 GSK189254A Featured

GSK189254A (GSK189254) is a novel, potent and selective histamine H3 receptor antagonist with pKi values of 9.59-9.90 and 8.51-9.17 for human and rat H3, respectively.

720690-73-3
DC10391 EBI2 inhibitor GS682753A

GSK682753A is a selective and highly potent inverse agonist of the epstein-barr virus-induced receptor 2 (EBI2) with an IC50 of 53.6 nM.

1334294-76-6
DC10233 Guanfacine Hydrochloride

Guanfacine Hydrochloride is a selective α2A-adrenoceptor agonist with anti-hypertensive effect.

29110-48-3
DC9819 Guanoclor Featured

Guanoclor is a sympatholytic drug. It is known to bind to non-adrenergic sites in pig kidney membranes.

5001-32-1
DC9458 GW-1100

GW 1100 is a selective antagonist of GPR40-mediated Ca2+ elevations in HEK293 cells stimulated by GW 9508 (an agonist of both GPR40 and GPR120, another GPCR activated by long chain fatty acids) or linoleic acid with a pIC50 value equal to 5.99.

306974-70-9
DC8266 GW-627368X Featured

GW 627368X is a selective prostanoid EP4 receptor competitive antagonist with additional affinity at TP receptors (pKi values are 7.0 and 6.8 in competition radioligand bioassays).

439288-66-1
DC12266 H4 Receptor antagonist 1

H4 Receptor antagonist 1 is a potent and selective histamine H4 receptor inverse agonist, with an IC50 of 19 nM.

848217-00-5
DC10935 HAMI3379

HAMI3379 (HAMI-3379) is a potent and selective antagonist of cysteinyl leukotriene 2 (CysLT(2)) receptor, inhibits LTD4- and LTC4-induced intracellular calcium mobilization withIC50 of 3.8 nM and 4.4 nM respectively.

1245653-57-9
DC12493 HT-2157(SNAP37889) Featured

HT-2157 (SNAP 37889) is a selective, high-affinity, competitive antagonists of galanin-3 receptor (Gal3).

303149-14-6
DC11328 Hydroxyzine

Hydroxyzine is a histamine H1 receptor antagonist (Ki = 1.9 nM).

68-88-2
DC7020 Ibutamoren mesylate Featured

Ibutamoren mesylate (MK-0677) is an orally active nonpeptide growth hormone (GH) secretagogue.

159752-10-0
DC3115 ICI-118551 Featured

ICI-118,551 is a selective beta-2 (β2) adrenergic receptor antagonist.ICI binds to the β2 subtype with at least 100 times greater affinity than β1 or β3, the two other known subtypes of the beta adrenoceptor.

72795-01-8
DCAPI1055 Iloperidone (Fanapt)

Iloperidone (Fanapt)

133454-47-4
DC9389 INCB3344

INCB3344 is a novel, potent and selective small molecule antagonist of the mouse CCR2 receptor; inhibits the binding of CCL2 to mouse monocytes with nanomolar potency (IC50 = 10 nM).

1262238-11-8
DC7429 INCB 8761 Featured

INCB8761(PF-4136309) is a potent, Selective, and orally bioavailable CCR2 antagonist.

1341224-83-6
DCAPI1701 Indacaterol Maleate

Indacaterol is an ultra-long-acting β-adrenoceptor agonist with pKi of 7.36.

753498-25-8
DC8914 Indacaterol

Indacaterol(Onbrez; Arcapta) is an ultra-long-acting β-adrenoceptor agonist.

312753-06-3
DC7197 ML 161 Featured

Inhibitor of protease-activated receptor 1 (PAR1)-mediated platelet activation (IC50 = 0.26 μM for the inhibition of platelet P-selectin expression on human platelets). Thought to act allosterically. Also inhibits thrombin-induced platelet activation.

423735-93-7
DC8996 Isoprenaline HCl

Isoprenaline Hydrochloride is a non-selective beta-adrenergic agonist and structurally similar to adrenaline.

51-30-9
DCAPI1080 Istradefylline (KW-6002) Featured

Istradefylline(KW6002) is a very potent, selective and orally active adenosine A2A receptor antagonist(Ki=2.2 nM) in experimental models of Parkinson's disease.

155270-99-8
DC8304 Isoxazole 9(ISX9) Featured

ISX-9 is a small molecule inducer of adult neural stem cell differentiation both in vitro and in vivo.

832115-62-5
DC10283 IT1t dihydrochloride Featured

IT1t dihydrochloride is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM.

1092776-63-0
DC10306 IT1t

IT1t is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM.

864677-55-4
DC10095 JD5037 Featured

JD5037 is an inverse agonist of peripheral cannabinoid 1 (CB1) receptors (Ki = 0.35 nM).

1392116-14-1
DC9524 JDTic (dihydrochloride)

JDTic 2Hcl is a highly selective antagonist for the κ-opioid receptor; without affecting the μ- or δ-opioid receptors.

785835-79-2
DC10971 JMS-17-2 Featured

JMS-17-2 is a potent and selective antagonist of CX3CR1 with IC50 of 0.32 nM, displays significant selectivity for CX3CR1 over other chemokine receptors such CXCR2, CXCR1, and CXCR4 (IC50>1 uM).

1380392-05-1
DC7843 JNJ 42153605 Featured

JNJ 42153605 is a positive allosteric modulator of the metabotropic glutamate 2 receptor.

1254977-87-1
DC12374 JNJ-10229570 Featured

JNJ-10229570 (JNJ10229570) is a novel potent, selective melanocortin receptor MC1R and MC5R antagonist with binding IC50 of 270 nM and 200 nM, respectively.

524923-88-4
DC8140 JNJ31020028 Featured

JNJ-31020028 is a selective brain penetrant antagonist of neuropeptide Y2 receptor with high affinity(pIC50=8.07, human; pIC50=8.22 rat); >100-fold selective versus human Y1/Y4/Y5 receptors.

1094873-14-9
DC12166 JNJ-5207852 Featured

JNJ-5207852 is a selective and potent histamine H3 receptor (H3R) antagonist, with pKis of 8.9, 9.24 for rat and human H3R, respectively.

398473-34-2
DC9271 JNJ-63533054 Featured

JNJ-63533054 is a potent and selective agonist of hGPR139 with an EC50 = 16 nM.

1802326-66-4
DC8773 JNJ-7777120 Featured

JNJ-7777120 is a selective H4R antagonist with Ki of 4 ±1 nM, exhibits >1000-fold selectivity over the other histamin receptors.

459168-41-3
DC9132 Ketotifen fumarate

Ketotifen (fumarate) is a second-generation noncompetitive H1-antihistamine and mast cell stabilizer, which is used to prevent asthma attacks.

34580-14-8
DC8889 Ki16198 Featured

Ki16198 is the methyl ester of Ki16425, which is a LPA antagonist and inhibits LPA1- and LPA3-induced inositol phosphate production with Ki of 0.34 μM and 0.93 μM, respectively, shows weaker inhibition for LPA2, no activity at LPA4, LPA5, LPA6.

355025-13-7
DC7179 Ki16425 Featured

Ki16425 is a competitive, potent and reversible antagonist to LPA1, LPA2 and LPA3 with Ki of 0.34 μM, 6.5 μM and 0.93 μM, respectively, shows no activity at LPA4, LPA5, LPA6.

355025-24-0
DC8987 L-Methyldopa

L-(-)-α-Methyldopa hydrate is an alpha-adrenergic agonist (selective for α2-adrenergic receptors) psychoactive drug used as a sympatholytic or antihypertensive.

41372-08-1
DC11377 L-826,266

L-826,266 is a potent and selective competitive antagonist of the prostaglandin E2 receptor subtype EP3 (Ki = 0.8 nM).

244101-03-9
DC9006 Lamotrigine

Lamotrigine(BW430C) is a novel anticonvulsant drug for inhibition of 5-HT and sodium channel.

84057-84-1
DC7710 Lasmiditan (COL-144; LY573144) Featured

Lasmiditan (COL-144; LY573144) is a high-affinity, highly selective 5-HT1F receptor agonist(Ki=2.1 nM), compared with Ki of 1043 nM and 1357 nM at the 5-HT(1B) and 5-HT(1D) receptors, respectively.

439239-90-4
DC8635 Latanoprost Featured

Latanoprost is a prodrug (isopropyl ester) of 17-phenyl-13,14-dihydro prostaglandin F2α.

130209-82-4
DC8173 Lemborexant(E2006) Featured

Lemborexant (E-2006) is a dual antagonist of the orexin OX1 and OX2 receptors which is under development for treatment of insomnia.

1369764-02-2
DC8714 Levobetaxolol hydrochloride Featured

Levobetaxolol hydrochloride is a beta-adrenergic receptor inhibitor (beta blocker), used to lower the pressure in the eye in treating conditions such as glaucoma.

116209-55-3
DC8675 Levodropropizine

Levodropropizine is a histamine receptor inhibitor, Levodropropizine is an effective and very well tolerated peripheral antitussive drug.

99291-25-5
DC10278 LGD-6972 Featured

LGD-6972 is a selective and orally active glucagon receptor antagonist. LGD-6972 has the potential for type 2 diabetes research.

1207989-09-0
DC11148 LMD-A

LMD-A (CCR8 antagonist LMD-A) is a highly potent, small molecule antagonist of chemokine receptor CCR8 with EC50 of 2.5 nM.

850330-77-7
DC9104 Loratadine

Loratadine(SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM.

79794-75-5
DCAPI1419 Losartan

Losartan is a potent, non peptide antagonist of the angiotensin II receptor type 1. This receptor initiates a signal cascade that causes vasoconstriction. Antagonism of this receptor in turn causes vasodilation by blocking the signal from angiotensin II.

114798-26-4
DC9153 Losartan Potassium Featured

Losartan is an angiotensin II receptor antagonist, competes with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM.

124750-99-8
DC7583 Idalopirdine(Lu-AE-58054) Featured

Lu AE58054 is an in-vitro potency and selectivity, in-vivo binding affinity and effect of the 5-HT(6)R antagonist with a Ki value of 0.83 nM.

467459-31-0
DC11422 Lumateperone Tosylate Featured

Lumateperone Tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a SERT blocker (Ki = 61 nM).

1187020-80-9
DC3173 Lurasidone HCl Featured

Lurasidone is an atypical antipsychotic, inhibits Dopamine D2, 5-HT2A, 5-HT7, 5-HT1A and noradrenaline α2C with IC50 of 1.68 nM, 2.03 nM, 0.495 nM, 6.75 nM and 10.8 nM, respectively.

367514-88-3
DC3174 lurasidone

Lurasidone is a novel psychotropic agent that has been shown in studies of cloned human receptors to be an antagonist at the 5-HT2A receptor.

367514-87-2
DC8435 LY2119620 Featured

LY2119620 is a specific, and allosteric agonist of human M2 and M4 muscarinic acetylcholine receptors.

886047-22-9
DC10782 LY2510924 Featured

LY2510924 is an inhibitor of CXC chemokine receptor 4 (CXCR4), with potential antineoplastic activity.

1088715-84-7
DC12081 LY2828360 Featured

LY2828360 is a slowly acting but efficacious G protein-biased cannabinoid (CB2) agonist, inhibiting cAMP accumulation and activating ERK1/2 signaling.

1231220-79-3
DC11681 LY2922470

LY2922470 (LY-2922470) is a potent, selective, orally available GPR40 agonist with EC50 of 7 nM.

1423018-12-5
DC7884 LY310762 Featured

LY310762 is a 5-HT1D receptor antagonist with Ki of 249 nM, having a weaker affinity for 5-HT1B receptor.

192927-92-7
DC11330 LY320135 Featured

LY320135 is a selective cannabinoid (CB) receptor 1 antagonist (Kis = 224 and >10,000 nM for CB1 and CB2, respectively, in vitro).

176977-56-3
DC10712 LY334370 Featured

LY334370 is a selective 5-HT1F receptor agonist with a Ki of 1.6 nM.

182563-08-2
DC9314 LY 344864

LY344864 is a selective receptor agonist with an affinity of 6 nM (Ki) at the recently cloned 5-HT1F receptor.

186544-26-3
DC11323 LY354740

LY354740 is an agonist of the group II metabotropic glutamate receptor (mGluR) subtypes mGluR2 and mGluR3 (Kis = 99 and 94 nM, respectively).

176199-48-7
DC7192 LY-404039 Featured

LY404039 is an inhibitor for mGluR1(Ki=149 nM) and mGluR2(Ki= 92 nM), which can also inhibit dopamine receptor.

635318-11-5
DC1012 Macitentan (Actelion-1,ACT-064992) Featured

macitentan (Actelion-1, ACT-064992) is an orally active, non-peptide dual endothelin (ET)A/B receptor antagonist with IC50 of 0.5 nM/391 nM.

441798-33-0
DC9519 Maropitant

Maropitant is a neurokinin (NK1) receptor antagonist.

147116-67-4
DC7681 Mavoglurant (AFQ 056) Featured

Mavoglurant (AFQ056) is an experimental drug candidate for the treatment of fragile X syndrome.It exerts its effect as an antagonist of the metabotropic glutamate receptor 5 (mGLU5).

543906-09-8
DC9297 MDK-5220(Orexin-2 receptor agonist) Featured

MDK-5220(Orexin-2 receptor agonist) is the first selective nonpeptidic orexin 2 receptor (OX2R) agonist (OX2R EC50 = 0.023 μM, Emax = 98%; OX1R EC50 = 1.616 μM, Emax = 100%)

1796565-52-0
DC7757 (R)-Meclizine

Meclizine is a histamine H1 receptor antagonist used to treat nausea and motion sickness.

189298-48-4
DCAPI1580 Medetomidine

Medetomidine hydrochloride is a potent and highly selective α2-AR adrenoceptor agonist (Ki values are 1.08 and 1750 nM for α2- and α1-adrenoceptors respectively). Shows greater selectivity over α1-adrenoceptors than clonidine and UK 14,304 (1620-, 220- an

86347-14-0
DC11083 Dersimelagon Featured

Dersimelagon, also known as MT-7117 and WHO 10832, is a novel, orally-administered, small molecule, selective melanocortin-1 receptor (MC1R) agonist that increases skin melanin without sun exposure and is being developed to increase light tolerance in EPP/XLP patients. Dersimelagon significantly boosted sunlight tolerance in patients with erythropoietic protoporphyria in a multicenter, phase 2, randomized trial.

1835256-48-8
DC9526 Meptazinol (hydrochloride) Featured

Meptazinol Hcl(WY-22811 Hcl) is a unique centrally active opioid analgesic.

59263-76-2
DC10407 Mequitazine

Mequitazine is a potent, nonsedative and long-acting histamine H1 antagonist.

29216-28-2
DC9527 Methylnaltrexone (Bromide) Featured

Methylnaltrexone Bromide is a pheriphally-acting μ-opioid antagonist that acts on the gastrointestinal tract to decrease opioid-induced constipation.

73232-52-7
DC9191 Metoprolol tartrate

Metoprolol is a cardioselective β1-adrenergic blocking agent.

56392-17-7
DC8249 MF498

MF498 is a novel and selective E prostanoid receptor 4 (EP4) inhibitor, relieves joint inflammation and pain in rodent models of rheumatoid and osteoarthritis.

915191-42-3
DC11902 Minesapride

Minesapride (DSP-6952) is a novel potent, selective, orally active 5-HT4 receptor partial agonist with Ki of 50-100 nM for human 5-HT4a/4b/4c.

1184662-54-1
DC3172 Mirabegron Featured

Mirabegron is a selective β3-adrenoceptor agonist with EC50 of 22.4 nM.

223673-61-8
DC9468 Mizolastine

Mizolastine is a histamine H1-receptor antagonist with IC50 of 47 nM used in the treatment of hay fever (seasonal allergic rhinitis), hives and other allergic reactions.

108612-45-9
DC1009 Laropiprant Featured

MK 0524 is a potent, selective DP1 receptor antagonist with Ki values of 0.57 nM and 0.75 µM for the DP1 and DP2 receptors, respectively.

571170-77-9
DC9456 MK-0354

MK-0354 is a partial agonist of GPR109a receptor, for hGPR109a/ mGPR109a with EC50 of 1.65/1.08 μM, showed no activation of GPR109b.

851776-28-8
DC10045 MK-0557 Featured

MK-0557 is a highly selective, orally administered neuropeptide NPY5R antagonist, could limit weight regain after very-low-calorie diet (VLCD)-induced weight loss.

328232-95-7
DC3167 MK0812

MK-0812 is chemokine receptor CCR-2 antagonist

624733-88-6
DC9398 MK-0974

MK-0974(Telcagepant) is a highly potent, selective, and orally bioavailable CGRP receptor antagonist with Ki values of 0.77 nM and 1.2 nM for human and rhesus CGRP receptors respectively; displays >1500-fold lower affinity for the canine and rat receptors

781649-09-0
DC9966 MK-1064 Featured

MK-1064 is a selective orexin 2 receptor antagonist (2-SORA) for the research of insomnia.

1207253-08-4
DC9607 MK-2894

MK-2894 is a highly potent and selective second generation EP4 antagonist.

1006036-87-8
DC9397 MK-3207 (Hydrochloride)

MK-3207 is a potent and orally bioavailable CGRP receptor antagonist (IC50= 0.12 nM; Ki value= 0.024 nM); highly selective versus human AM1, AM2, CTR, and AMY3.

957116-20-0
DC7646 MK3697

MK-3697 is a third insomnia drug, currently being developed by Merck. MK-3697 is a potent and selective Orexin receptor antagonist with Ki = 0.95 nM.

1224846-01-8
DC9279 MK-571 Featured

MK-571 is a selective, orally active CysLT1 receptor antagonist.

115103-85-0
DC9455 MK-6892

MK-6892 is a highly potential GPR109A agonist with Ki value of 4.0 nM.

917910-45-3
DC10785 MK-7246 Featured

MK-7246 is a potent and selective CRTH2 antagonist with a Ki of 2.5±0.5 nM.

1218918-62-7
DC11142 MK-8318

MK-8318 (MK8318) is a potent, selective, orally available CRTh2 receptor antagonist with Ki of 5 nM, shows nM potency in functional assay (cAMP IC50=8 nM, β-Arrestin IC50=3.5 nM.

1416581-40-2
DC12333 ML-109 Featured

ML-109 is a potent and full thyroid stimulating hormone receptor (TSHR) agonist, with an EC50 of 40 nM.

1186649-91-1
DC7781 ML-224 Featured

ML-224 (ANTAG3) is a selective TSH receptor antagonist inhibits stimulation of thyroid function in female mice.

1338824-21-7
DC10221 MLR-1023

MLR-1023 is a chemical compound which inhibits acid secretion in animal models and also acts as a bronchodilator in histamine-challenged animals.

41964-07-2
DC11165 MLS6585

MLS6585 is a novel positive allosteric modulator of the D1 dopamine receptor, potentiatse dopamine-stimulated G-protein- and β-arrestin-mediated signaling and increase the affinity of dopamine for the D1 receptor with low micromolar potencies..

389080-71-1
DC3160 Montelukast Sodium Featured

Montelukast belongs to a group of medications known as leukotriene receptor antagonists.

151767-02-1
DC10326 Mozavaptan

Mozavaptan (OPC31260) is a orally effective, nonpeptide vasopressin V2 receptor antagonist with an IC50 of 14 nM.

137975-06-5
DC10437 MRE-269 Featured

MRE-269 is an active metabolite of selexipag, and acts as a selective IP receptor agonist.

475085-57-5
DC12258 MRS1186

MRS1186 is a potent and selective human Adenosine A3 receptor (hA3AR) antagonist, with a Ki of 7.66 nM.

183721-03-1
DC7203 MRS 2578 Featured

MRS2578 is a potent P2Y6 receptor antagonist with IC50 of 37 nM, exhibits insignificant activity at P2Y1, P2Y2, P2Y4,and P2Y11 receptors.

711019-86-2
DC8822 MSX-122 Featured

MSX-122 is a n orally bioavailable inhibitor of CXCR4 with potential antineoplastic and antiviral activities.

897657-95-3
DC11270 MSX-130 Featured

MSX-130 is CXCR4 Antagonist.

4051-59-6
DC9507 MTEP (hydrochloride)

MTEP Hcl is a potent, selective and non-competitive mGlu5 antagonist with IC50 and Ki of 5 nM and 16 nM, respectively.

1186195-60-7
DCAPI1550 Naftopidil

Naftopidil is an α-1-Adrenergic receptor antagonist and an antihypertensive.

57149-07-2
DC10455 NE-100 Featured

NE100 hydrochloride is a potent and selective σ1 receptor antagonist (Ki = 0.86 nM) that displays > 55-fold selectivity over σ2 receptors and > 6000-fold selectivity over D1,

149409-57-4
DCAPI1592 Nebivolol hydrochloride

Nebivolol hydrochloride is a highly selective β1-adrenoceptor antagonist

152520-56-4
DC7472 Nedocromil

Nedocromil is an inhaled anti-inflammatory agent for the preventive management of asthma.

69049-73-6
DC11469 APD125(Nelotanserin) Featured

Nelotanserin is a potent 5-HT2A inverse agonist, a moderately potent 5-HT2C partial inverse agonist and a weak 5-HT2B inverse agonist, with IC50s of 1.7, 79, 791 nM in IP accumulation assays, respectively.

839713-36-9
DC11550 Netazepide

Netazepide (YF476, Sograzepide) is a potent, selective and orally active gastrin/CCK-2 antagonist with IC50 of 0.1 nM.

155488-25-8
DC11171 NFEPP

NFEPP is a novel potent, selective pH-dependent μ-opioid receptor (MOR) agonist with a low pKa, shows significantly lower affinity compared with fentanyl at pH 7.4.

1422952-82-6
DC8836 NIBR189 Featured

NIBR 189 is a potent and selective EBI2 (GPR183) receptor antagonist (IC50 values are 11 and 15 nM for human and mouse EBI2 receptors respectively).

1599432-08-2
DC10114 Nifenalol Featured

Nifenalol is a beta-adrenoceptor antagonist.

5704-60-9
DC9520 NKP608

NKP608 is a non-peptidic derivative of 4-aminopiperidine which acts as a selective, specific and potent antagonist at the neurokinin-1 (NK-1) receptor both in vitro(IC50=2.6 nM) and in vivo.

177707-12-9
DC12351 NMI 8739

NMI 8739 is a dopamine D2 autoreceptor agonist, which is an amine conjugate of the DHA carrier and the neurotransmitter dopamine.

129024-87-9
DC11386 NNZ-2591 Featured

NNZ2591 (cyclo-L-glycyl-L-2-allylproline)1 is an investigational synthetic analog of cyclic glycine-proline (cGP), a breakdown product of human insulin-like growth factor 1 (IGF-1), that has been chemically modified to increase its half-life, stability, and oral bioavailability.

1821796-28-4
DC12198 N-Oleoyl glycine

N-Oleoyl glycine is a lipoamino acid, which stimulates adipogenesis associated with activation of CB1 receptor and Akt signaling pathway in 3T3-L1 adipocyte.

2601-90-3
DC8583 Asenapine Maleate Featured

Novel psychopharmacologic agent. Displays antagonist activity at 5-HT, dopamine, noradrenalin and histamine receptor subtypes (pKi values are 8.60, 8.40, 10.15, 9.75, 10.46, 8.84, 9.60, 9.94, 8.85, 8.90, 8.84, 9.38, 8.95, 8.93, 8.9, 9.49, 8.91, 9.00 and 8

85650-56-2
DC4136 NPS-2143 HCL

NPS 2143 hydrochloride is a selective CaSR (Ca2+-sensing receptor) inhibitor and antagonist, shown to block increases in cytoplasmic Ca2+ concentrations elicited by human Ca2+ receptors expressed in HEK293 cells with an IC50 of 43 nM. NPS 2143 hydrochlori

324523-20-8
DC7214 NPS-2143(SB 262470A )

NPS-2143(SB 262470A ) is a selective potent calcium ion-sensing receptor antagonist with IC50 of 43 and 41 nM for cytoplasmic Ca2+ concentrations and parathyroid hormone secretion, respectively.

284035-33-2
DC11269 MSX-127(NSC23026) Featured

NSC-23026, also known as MSX-127, is a CXCR4 receptor modulator.

6616-56-4
DC7701 NVP-QAV680

NVP-QAV680 is a potent and selective CRTh2 receptor antagonist suitable for clinical testing in allergic diseases.

872365-16-7
DC12298 Octreotide acetate (SMS 201-995 (acetate)) Featured

Octreotide acetate, a long-acting synthetic analog of native somatostatin, inhibits growth hormone, glucagon, and insulin more potently.

79517-01-4
DC9059 Olanzapine Featured

Olanzapine(LY170053) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist.

132539-06-1
DC10370 Olcegepant hydrochloride

Olcegepant hydrochloride is the first potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC50 of 0.03 nM and with a Ki of 14.4 pM for human CGRP.

586368-06-1
DC9396 Olcegepant Featured

Olcegepant(BIBN 4096; BIBN 4096BS) is the first potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor(IC50= 0.03 nM).

204697-65-4
DCAPI1464 Olmesartan

Olmesartan Acid is an angiotensin II receptor antagonist that prevents the binding of angiotensin II, thus preventing vasoconstriction.

144689-24-7
DC9179 Olmesartan MedoxoMil

Olmesartan medoxomil(Olmetec; Benicar; CS 866) is an angiotensin II receptor antagonist which is used as an anti-hypertensive.

144689-63-4
DC10384 Olodaterol Featured

Olodaterol (BI1744) is a long acting β2-adrenoceptor agonist with an EC50 of 1.4±0.08 nM.

868049-49-4
DC9248 Olodaterol(BI-1744) hydrochloride Featured

Olodaterol is a novel, long-acting beta2-adrenergic agonist (LABA) that exerts its pharmacological effect by binding and activating beta2-adrenergic receptors located primarily in the lungs.

869477-96-3
DC11043 Omidenepag Featured

Omidenepag is a potent, selective agonist human EP2 receptor with binding IC50/EC50 of 10/1.7 nM, >500-fold selectivity over EP1, EP3 and EP4 receptors; Omidenepag is the active form of Omidenepag Isopropyl (OMDI).

1187451-41-7
DC11044 Omidenepag Isopropyl Featured

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.

1187451-19-9
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