Home > Inhibitors & Agonists > GPCR
Cat. No. Product name CAS No.
DC5060 (+)PD 128907

(+)PD 128907 is a potent D3 dopamine receptor agonist (Ki = 2.3 nM). Displays 18 - 200-fold selectivity over other dopamine receptor subtypes.

300576-59-4
DCAPI1411 Bisoprolol Fumarate Featured

(±)-Bisoprolol hemifumarate is a selective β1-AR adrenergic antagonist. Possesses β1/β2 selectivity of approximately 100-fold and a Kd of 2-3 nM at the β1-AR (β1 receptor).

104344-23-2
DC10094 (±)-SLV319(Ibipinabant) Featured

(±)-SLV 319 is a potent and selective CB1 receptor antagonist (Ki = 7.8 nM). Exhibits 1000-fold selectivity for CB1 over CB2 receptors.

362519-49-1
DC10160 (1R,2S)-VU0155041

(1R,2S)-VU0155041, Cis regioisomer of VU0155041, is a partial mGluR4 agonist with an EC50 of 2.35 μM.

1263273-14-8
DC8964 Phenylephrine hydrochloride

(R)-(-)-Phenylephrine hydrochloride is a phenylephrine (PE) and an α1-adrenoceptor agonist

61-76-7
DC11364 Levocetirizine;(R)-Cetirizine (hydrochloride)

(R)-Cetirizine is the (R)-enantiomer of the histamine H1 receptor antagonist and second generation antihistamine cetirizine.

130018-87-0
DC9137 Timolol Maleate Featured

(S)-Timolol maleate, is a potent non-selective β-adrenergic receptor antagonist (Ki values are 1.97 and 2.0 nM for β1 and β2 receptor subtypes respectively).

26921-17-5
DCZ-156 UR-144

>98%,Standard References

1199943-44-6
DCZ-059 L-Stepholidine Featured

Stepholidine s a naturally occurring chemical compound found in the herb Stephania intermedia. Stepholidine is a dual D2 receptor antagonist and D1 receptor agonist, and has shown antipsychotic activity in animal studies.

16562-13-3
DC10090 4-P-PDOT Featured

4-P-PDOT is a slelctive MT2 melatonin receptor antagonist 300 fold selective for MT2 (MEL-1B-R) vs MT1 (MEL-1A-R) melatonin receptor subtype.

620170-78-7
DC10689 4P-PDOT Featured

4P-PDOT, also known as 4-phenyl-2- propionamidotetralin, is a MT2-receptor-specific antagonist. MT2 melatonin receptor may be a novel target for analgesic drug development.

134865-74-0
DC10877 5,3-AB-CHMFUPPYCA Featured

5,3-AB-CHMFUPPYCA is an analytical reference standard that is structurally classified as a synthetic cannabinoid.

DC7494 SB-242084 HCl Featured

5-HT2C receptor antagonist that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2Breceptors respectively. Also displays selectivity over a range of other 5-HT, dopamine and adrenergic receptors. Brain penetrant; exerts anxiolytic-like activity.

1049747-87-6
DC7925 GTPL-5846 (6-OAU) Featured

6-OAU(GTPL5846; 6-n-octylaminouracil) is a surrogate agonist of GPR84; activates human GPR84 in the presence of Gqi5 chimera in HEK293 cells with an EC50 of 105 nM in the PI assay.

83797-69-7
DC10537 8-OH-DPAT Featured

8-OH-DPAT is a research chemical of the aminotetralin chemical class and has been widely used to study the function of the 5-HT1A receptor.

78950-78-4
DC7289 Imiloxan

A moderately potent, but highly selective α2-adrenoceptor antagonist, the only reported selective antagonist at the α2B-adrenoceptor not having potent α1-adrenoceptor antagonist activity.

81167-16-0
DCAPI1496 Ambrisentan Featured

A nonpeptide endothelin ETA receptor antagonist. Antihypertensive.

177036-94-1
DC11523 Landipirdine

A novel 5-HT receptor antagonist for the treatment of Parkinson's disease..

1000308-25-7
DC11994 ZQ-16

A novel potent and selective agonist of GPR84 that induces calcium response with EC50 of 0.213 uM.

376616-73-8
DC11982 CX815

A novel potent, selective CXCR2 inhibitor with IC50 of 0.4 nM.

109628-27-5
DC11981 CX4152

A novel potent, selective CXCR2 inhibitor with IC50 of 7.6 nM.

333351-27-2
DC11605 ONO-0300302

A novel potent, slow tight binding LPA1 receptor antagonist with IC50 of 86 nM, Kd of 0.34 nM.

856689-51-5
DC11974 L 741742 hydrochloride

A potent and highly selective D4 dopamine receptor antagonist with Ki of 3.5 nM, >200-fold selectivity over D2 and D3 receptors.

874882-93-6
DC11743 BMS-681

A potent and orally bioavailable dual antagonist of CCR2 and CCR5 with binding IC50 of 0.7 nM and 2.4 nM, respectively.

847998-92-9
DC11705 GPR30 inhibitor G1 Featured

A potent and selective GPER/GPR30 agonist with Ki of 11 nM, EC50 of 2 nM.

881639-98-1
DC11699 VUF11403

A potent CXCR7 (ACKR3) agonist..

1378524-61-8
DC11976 SX-576

A potent, equipotent CXCR1 and CXCR2 antagonist with IC50 of 31 nM and 21 nM, respectively.

1240494-14-7
DC11903 NBUMP

A potent, highly selective 5-HT1A receptor partial agonist with Ki of 0.1 nM, displays 460- and 260-fold selectivity for 5-HT1A over the α1-adrenergic and D2 receptors, respectively..

1348755-27-0
DC11609 VU6010608

A potent, highly selective, CNS penetrant mGlu7 negative allosteric modulator with IC50 of 0.76 uM.

2165325-42-6
DC11758 PB 28 dihydrochloride Featured

A potent, mixed sigma2 agonist and sigma1 antagonist with Ki of 0.28 and 13.0 nM, respectively.

172907-03-8
DC11757 PB 28

A potent, mixed sigma2 agonist and sigma1 antagonist with Ki of 0.28 and 13.0 nM, respectively.

172906-90-0
DC11629 NK1-IN-9

A potent, orally active, dual NK1 receptor antagonist (IC50=0.5 nM) and SERT inhibitor (IC50=5.2 nM).

1100211-97-9
DC11697 AM-1638

A potent, orally bioavailable, full agonist of GPR40/FFA1 with EC50 of 0.16 uM.

1142214-62-7
DC11979 SB 332235

A potent, selective and competitive CXCR2 inhibitor that selectively inhibits CXCR2-mediated recruitment of β-arrestin-2 with pKi of 8.92.

276702-15-9
DC11755 L-732138 Featured

A potent, selective and competitive NK1 receptor antagonist with IC50 of 2.3 nM.

148451-96-1
DC11514 Atogepant

A potent, selective and orally available CGRP receptor antagonist for the prevention of migraine. Migraine.

1374248-81-3
DC11519 Ceclazepide

A potent, selective cholecystokinin receptor CCK2 antagonist for treatment of gastroesophageal reflux disease (GERD)..

1801749-44-9
DC12015 SKF 83566 hydrobromide

A potent, selective dopamine D1 receptor antagonist with Ki of 0.56 nM.

108179-91-5
DC11973 A-412997

A potent, selective dopamine D4 receptor agonist with Ki of 12.1 and 7.9 nM for rat and human D4 receptors, respectively.

1347744-96-0
DC11700 Chalcone 4 hydrate

A potent, selective inhibitor of CXCL12 binding to CXCR4 and CXCR7 with IC50 of 200 nM.

1202866-96-3
DC11560 SPM-242

A potent, selective S1P3 antagonist with Ki of 0.25 nM.

DC11561 SPM-242 racemate

A potent, selective S1P3 antagonist with Ki of 0.25 nM.

749263-43-2
DC11745 BMS-22

A potent, selective, allosteric CCR2 antagonist with binding IC50 of 5.1 nM.

445479-97-0
DC11744 CCR2-RA-[R]

A potent, selective, allosteric CCR2 antagonist with IC50 of 103 nM..

512177-83-2
DC11895 Foliglurax hydrochloride

A potent, selective, brain-penetrant and orally bioavailable mGluR4 positive allosteric modulator with EC50 of 79 nM.

2133294-96-7
DC11894 Foliglurax

A potent, selective, brain-penetrant and orally bioavailable mGluR4 positive allosteric modulator with EC50 of 79 nM.

1883329-51-8
DC11666 BMS-470539

A potent, selective, full agonist of human and murine MC1R with EC50 of 16.8 and 11.6 nM, respectively.

457893-92-4
DC11746 JNJ-27141491

A potent, selective, noncompetitive, orally active CCR2 antagonist with IC50 of 172 nM.

871313-59-6
DC11756 SR 140333

A potent, selective, non-peptide NK1 receptor antagonist with Ki of 0.74 nM, IC50 of 1.6 nM.

153050-21-6
DC11667 PF-592379

A potent, selective, orally active agonist of dopamine D3 receptor with EC50 of 21 nM.

710655-15-5
DC11683 LY2881835

A potent, selective, orally available GPR40 agonist with EC50 of 8 nM.

1292290-38-0
DC11682 LY2922083

A potent, selective, orally available GPR40 agonist with EC50 of 9 nM.

1309435-78-6
DC11680 LY3104607

A potent, selective, orally available GPR40 agonist with Ki of 15 nM, β-arrestin EC50 of 108 nM.

1795232-22-2
DC11623 GPR120 agonist 4x

A potent, selective, orally bioavailable GPR120 agonist with EC50 of 42 nM in calcium flux assays.

1628448-77-0
DC11748 LY2033298 Featured

LY2033298 is a robust allosteric potentiator that is highly selective for the human M4 muscarinic acetylcholine receptor subtype. LY2033298 enhances inhibition by oxotremorine of light-induced phase shifts in hamster circadian activity rhythms.

886047-13-8
DC11978 SB 265610 Featured

SB-265610 is a selective, competitive, nonpeptide and allosteric CXCR2 antagonist.

211096-49-0
DC11983 CX797

A potent, specfic CXCR2 antagonist that inhibits IL8 down-regulation of forskolin-induced cAMP with IC50 of 7.79 uM.

1611496-70-8
DC11977 SX-517

A potent, specific, noncompetitive dual CXCR1 and CXCR2 antagonist with IC50 of 38 nM (vs. CXCL1) and 36 nM (vs. CXCL8), respectively.

1240494-13-6
DC11972 PNU 96415E

A potential antipsychotic agent that binds selectively to D4 and 5-HT2A receptors with Ki of 3.0 and 5.8 nM, respectively.

170856-41-4
DC11545 IPAG Featured

IPAG is a prototypic selective inhibitor of sigma1 receptor that engages the unfolded protein response and induces autophagy in cancer cells.

193527-91-2
DC11698 α-NETA

A small molecule CMKLR1 antagonist that inhibits chemerin-stimulated β-arrestin2 association with CMKLR1 (EC50=9.7 nM).

31059-54-8
DC9867 prostaglandin D2(PGD2) inhibitor Featured

A small molecule compound of prostaglandin D2(PGD2) inhibitor.

885066-67-1
DC11686 (R)-CCX-777

A small-molecule partial agonist of CXCR7 (ACKR3)..

1257861-18-9
DC11687 (S)-CCX-777

A small-molecule partial agonist of CXCR7 (ACKR3)..

1257861-17-8
DC11685 CCX-777

A small-molecule partial agonist of CXCR7 (ACKR3)..

1226686-36-7
DC11525 Mocravimod

A synthetic immunosuppressant that functions as a S1P1 receptor agonist.

509092-16-4
DC8667 AB-MECA Featured

AB-MECA is a high affinity A3 adenosine receptor agonist, has high affinity for recombinant A1 and A3 receptors.

152918-26-8
DC10293 AC260584

AC260584 is an M1 muscarinic receptor allosteric agonist with a pEC50 of 7.6.

560083-42-3
DC10117 AC264613 Featured

AC264613 is a potent and selective protease-activated receptor 2 (PAR2) agonist (pEC50 = 7.5). Displays no activity at other PAR subtypes and exhibits no significant activity at over 30 other receptors implicated in nociception and inflammation.

1051487-82-1
DC10279 Acrivastine

Acrivastine (BW825C) is a short acting histamine 1 receptor antagonist for the treatment of allergic rhinitis.

87848-99-5
DC11209 ACT-246475

ACT-246475 (ACT246475) is a potent, selective, reversible P2Y12 receptor antagonist with binding IC50 of 1.0 nM.

1159500-34-1
DC11439 Nemorexant Featured

ACT-541468 is a dual orexin receptor antagonist.

1505484-82-1
DC8191 Sparsentan(PS433540) Featured

Sparsentan (RE-021) is a highly potent dual angiotensin II and endothelin A receptor antagonist with Kis of 0.8 and 9.3 nM, respectively[1].

254740-64-2
DC11754 AD 2900 Featured

AD 2900 (AD2900, AD-2900) is a novel potent, broad S1P receptor antagonist with IC50 of 3.8, 3.2, 6.2, 5.9 and 0.405 uM for S1P1, 2, 3, 4 and 5 respectively.

18360-29-7
DC7050 ADL5859 HCl Featured

ADL5859 agonizes δ-opioid receptor with a 1000-fold selectivity than µ- or κ-opioid receptor with Ki of 32 nM and 37 nM, respectively.ADL5859 displays weak inhibitory activity at the hERG channel with an IC50 of 78 μM. The EC50 of ADL5859 against δ opioid

850173-95-4
DC8087 ADX 47273 Featured

ADX-47273 is a novel, potent and selective metabotropic glutamate receptor 5 allosteric modulator with an EC50 of 170 nM.

851881-60-2
DC10465 ADX-88178 Featured

ADX-88178 is a novel potent, selective, and brain-penetrant positive allosteric modulator of the mGlu4 receptor.

1235318-89-4
DC12213 AGN 210676 (Simenepag)

AGN 210676 is a selective prostaglandin EP2 agonist extracted from patent US20070203222A1, Compound example 23, has an EC50 of 5 nM.

910562-15-1
DC11005 AGN192836

AGN192836 (AGN 192836) is a potent, selective α2 adrenergic (alpha 2-adrenoceptor) agonist with EC50 of 8.7, 41 and 6.6 nM for α2A, α2B and α2C receptor, respectively.

171102-29-7
DC3171 Agomelatine

Agomelatine is classified as a norepinephrine-dopamine disinhibitor (NDDI) due to its antagonism of the 5-HT2C receptor.

138112-76-2
DCAPI1467 Alcaftadine

Alcaftadine

147084-10-4
DC9334 Alfuzosin

Alfuzosin is an α1 adrenergic receptor antagonist used to treat benign prostatic hyperplasia (BPH).

81403-80-7
DC7692 Almorexant HCl (Act-078573) Featured

Almorexant(ACT078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively.

913358-93-7
DC8284 Almotriptan Malate(PNU180638) Featured

Almotriptan Malate is a 5-HT1B/1D-receptor agonist used to treat migraine.

181183-52-8
DC10234 Alosetron Hydrochloride

Alosetron Hydrochloride is the hydrochloride salt form of alosetron, a potent and selective 5-HT3 receptor antagonist.

122852-69-1
DC8606 Alvimopan monohydrate

Alvimopan(LY 246736; ADL 8-2698) is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery.

1383577-62-5
DC8605 Alvimopan dihydrate

Alvimopan(LY 246736; ADL 8-2698) is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery.

170098-38-1
DC8621 AM095 Featured

AM095 is a potent LPA1 receptor antagonist with IC50 values of 0.98 and 0.73 μM for recombinant human or mouse LPA1 respectively.

1345614-59-6
DC8622 AM095 free acid Featured

AM095 is a potent LPA1 receptor antagonist with IC50 values of 0.98 and 0.73 μM for recombinant human or mouse LPA1 respectively.

1228690-36-5
DC12230 AM211 Featured

AM211 is a potent, selective and orally bioavailable prostaglandin D2 (PGD2) receptor type 2 (DP2) antagonist

1175526-27-8
DC8765 AM251 Featured

AM251 is a potent CB1 receptor antagonist (IC50 = 8 nM, Ki = 7.49 nM) that displays 306-fold selectivity over CB2 receptors; also potent GPR55 agonist (EC50 = 39 nM).

183232-66-8
DC8886 Iodopravadoline(AM-630) Featured

AM630 is a selective CB2 receptor antagonist that binds to CB1 and CB2 receptors with Ki values of 5.2 µM and 31.2 nM, respectively.

164178-33-0
DC11552 AM-6538

AM-6538 (AM6538) is a potent, selective cannabinoid receptor CB1 antagonist with Ki of 5.1 nM..

1245626-00-9
DC11221 AM9405

AM9405 (AM-9405) is novel potent, peripherally active cannabinoid type 1 (CB1) and 5-HT3 receptor agonist, inhibits the EFS-induced twitch contraction of the ileum and the colon with IC50 of 0.076 and 45.71 nM, respectively.

DC8623 AM966 Featured

AM966 is a high affinity, selective, oral LPA1 (lysophosphatidic acid receptor, IC50=17 nM) antagonist, with selectivity for this receptor over the other LPA receptors.

1228690-19-4
DC5056 AMD3465 Featured

AMD3465 is a Potent, selective CXCR4 antagonist; exhibits 8-fold higher affinity than AMD 3100 (Cat.No. 3299). Inhibits SDF-1α-ligand binding (Ki = 41.7 nM).

185991-07-5
DC7867 AMG-837 Featured

AMG 837 is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents.

865231-46-5
DC6310 AMG 853(AMG853;Vidupiprant)

AMG 853 is novel a CRTH2 and DP Dual Antagonist.

1169483-24-2
DC5083 Cinacalcet (AMG-073) HCl Featured

AMG-073 HCl (Cinacalcet HCl) represents a new class of compounds for the treatment of hyperparathyroidism.

364782-34-3
DC11747 Iperoxo

Iperoxo is a superagonist of the muscarinic acetylcholine receptors and an OxotremorineM analog.

247079-84-1
DC7357 Anamorelin Featured

Anamorelin(RC1291; ONO-7643) is a synthetic orally active ghrelin receptor agonist which is under development for the management of non-small lung cancer associated cachexia/anorexia.

249921-19-5
DC11428 Olorinab

APD-371 (APD371, Olorinab) is a potent, selective and orally available CB2 agonist with EC50 of 6.2 nM; displays no activity against CB1 receptors (EC50>10 uM); exhibits activity in rat model of osteoarthritis pain.

1268881-20-4
DC11513 Aprocitentan (ACT-132577) Featured

Aprocitentan (ACT-132577) is the major and pharmacologically active metabolite of macitentan, which is dual ETA/ETB antagonist designed for tissue targeting.

1103522-45-7
DC10731 Arecaidine but-2-ynyl ester tosylate

Arecaidine but-2-ynyl ester tosylate is a potent muscarinic agonist that shows 4.6-fold that is selectivity for mAChR M2 in the atrium versus those in the ileum.

119630-77-2
DC9147 Aripiprazole

Aripiprazole(Abilify) is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM.

129722-12-9
DC11174 ASP7657 Featured

ASP7657 (ASP-7657) is a potent, selective, orally active prostaglandin EP4 receptor antagonist with Ki values of 6.02 nM and 2.21 nM for rat and human EP4 receptors, resepctively.

1196045-28-9
DC7364 AT-56 Featured

AT-56 is a selective, competitive, and highly bioavailable inhibitor of lipocalin-type prostaglandin D synthase (L-PGDS) with a Ki value of 75 µM.

162640-98-4
DC9020 Atenolol

Atenolol is a selective β1 receptor antagonist.

29122-68-7
DC9878 ATI-2341

ATI-2341, pepducin targeting the C-X-C chemokine receptor type 4 (CXCR4), is an allosteric agonist activating the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization.

1337878-62-2
DC8998 Atipamezole HCl

Atipamezole Hcl(MPV1248 Hcl) is an alpha-adrenoceptor antagonist with high affinity and selectivity for the alpha 2-receptor.

104075-48-1
DC8925 Atipamezole Featured

Atipamezole(MPV1248) is an alpha-adrenoceptor antagonist with high affinity and selectivity for the alpha 2-receptor.

104054-27-5
DC10018 Atrasentan hydrochloride Featured

Atrasentan Hcl(A-147627) is an endothelin antagonist receptor (IC50=0.0551 nM, ETA) being developed for the treatment of prostate cancer.

195733-43-8
DC11399 AVN-492 Featured

AVN-492 is a very specific and highly-selective antagonist with picomolar affinity to 5-HT6R (Ki=91 pM).

1220646-23-0
DC9436 Avosentan

Avosentan(Ro 67-0565; SPP-301) is a potent, selective endothelin receptor(ETA receptor) antagonist.

290815-26-8
DC11147 AZ084

AZ084 (AZ-084) is a potent, selective, allosteric, orally available CCR8 antagonist with Ki of 0.9 nM.

929300-19-6
DC11975 AZ 10397767

AZ10397767 is a potent, selective CXCR2 inhibitor that inhibits CXCL8 binding to CXCR2 with pIC50 of 9.0.

333742-63-5
DC10879 AZ3451 Featured

AZ3451 is a potent and selective allosteric antagonist of protease-activated receptor 2 (PAR2)

2100284-59-9
DC11742 AZ-8838

AZ-8838 (AZ8838) is a potent, and selective PAR2 antagonist with Kd of 125 nM.

2100285-41-2
DC8713 Azaperone

Azaperone acts as a dopamine antagonist but also has some antihistaminic and anticholinergic properties. Azaperone is a pyridinylpiperazine and butyrophenone neuroleptic drug with sedative and antiemetic effects, which is used mainly as a tranquilizer in

1649-18-9
DCAPI1427 Azasetron HCL

Azasetron Hydrochloride is a 5-HT3 receptor antagonist which is used as an anti-emetic.

123040-16-4
DC9469 Azatadine (dimaleate)

Azatadine dimaleate is an histamine and cholinergic inhibitor with IC50 of 6.5 nM and 10 nM, respectively.

3978-86-7
DC7572 AZD1981 Featured

AZD1981 is a potent, selective CRTh2 (DP2) receptor antagonist with IC50 of 4 nM, showing >1000-fold selectivity over more than 340 other enzymes and receptors, including DP1

802904-66-1
DC10724 AZD2098 Featured

AZD2098 is a potent CC-chemokine receptor 4 (CCR4) inhibitor, used for asthma research.

566203-88-1
DC10739 AZD4635 Featured

AZD4635 is a novel adenosine 2A receptor (A2AR) inhibitor with a Ki of 1.7 nM.

1321514-06-0
DC10773 AZD5069 Featured

AZD-5069 is a potent and selective CXCR2 antagonist with the potential to inhibit neutrophil migration into the airways in patients with COPD.

878385-84-3
DC9130 Azelastine HCl

Azelastine HCl is a potent, second-generation, selective, histamine antagonist.

79307-93-0
DC4210 Azilsartan kamedoxomil Featured

Azilsartan medoxomil is an angiotensin II receptor antagonist indicated for the treatment of mild to moderate essential hypertension.

863031-24-7
DCAPI1469 azilsartan Featured

Azilsartan(TAK-536) is a specific and potent angiotensin II type 1 receptor antagonist with IC50 of 2.6 nM.

147403-03-0
DC11516 Balovaptan Featured

Balovaptan (RG7314, RG-7314) is a potent, selective vasopressin-1 receptor antagonist..

1228088-30-9
DC9117 Bambuterol HCl

Bambuterol Hcl is a long acting beta-adrenoceptor agonist (LABA) used in the treatment of asthma; it also is a prodrug of terbutaline.

81732-46-9
DC8298 BAN ORL 24 Featured

BAN ORL 24 is a potent, selective, competitive ORL1 non-peptide agonist. Displays 1000-fold selectivity over classical opioid receptors.

1401463-54-4
DC10385 BAR501 Featured

BAR501 is a potent and selective agonist of GPBAR1 with an EC50 of 1 μM.

1632118-69-4
DC10021 Batefenterol Featured

Batefenterol(GSK961081,TD-5959)is a Muscarinic Antagonist and β2-Agonist possessing both muscarinic antagonist (MA) and β2-adrenoceptor agonist (BA) properties (MABA).

743461-65-6
DC9783 Bay 59-3074 Featured

Bay 59-3074 is a novel CB1/CB2 receptor partial agonist (Ki values are 48.3 and 45.5 nM at human CB1 and CB2 receptors respectively).

406205-74-1
DC8313 BD1047.2HBr Featured

BD 1047 dihydrobromide is a selective antagonist of σ receptors.

138356-21-5
DC10280 BD1063 dhydrochloride Featured

BD1063 dhydrochloride is a potent and selective sigma 1 receptor antagonist.

206996-13-6
DC12290 Befiradol hydrochloride (F 13640 hydrochloride)

Befiradol hydrochloride is a selective 5-HT1A receptor agonist.

DCAPI1500 Bepotastine Besilate Featured

Bepotastine Beslilate (Bepreve) is a histamine H1 receptor anatagonist.

190786-44-8
DC8898 Bepotastine Featured

Bepotastine is a non-sedating, selective antagonist of the histamine 1 (H1) receptor.

125602-71-3
DC8967 Betahistine Dihydrochloride

Betahistine Dihydrochloride is a histamine H3 receptors inhibitor used as an antivertigo drug.

5579-84-0
DC8830 Betahistine Featured

Betahistine is a strong affinity histamine H3 receptor antagonist and weak affinity agonist of histamine H1 receptors.

5638-76-6
DC9426 B-HT 920

B-HT 920(Talipexole 2Hcl) is a dopamine D2 receptor agonist, α2-adrenoceptor agonist and 5-HT3 receptor antagonist, which displays antiParkinsonian activity.

36085-73-1
DC9670 BIBS39 Featured

BIBS 39 is a new nonpeptide angiotensin II (AII) receptor antagonist.

133085-33-3
DC7995 Bilastine Featured

Bilastine is a selective histamine H1 receptor antagonist used for treatment of allergic rhinoconjunctivitis and urticaria.

202189-78-4
DCAPI1079 Bimatoprost Featured

Bimatoprost is a prostaglandin analog used topically (as eye drops) to control the progression of glaucoma and in the management of ocular hypertension.

155206-00-1
DC11003 BL5923

BL5923 (BL-5923) is a potent, highly specific, orally available inhibitor of CCR1 with IC50 of 20.4 and 22.8 nM for human and mouse CCR1, resepctively.

921208-19-7
DC7087 Blonanserin(AD-5423)

Blonanserin(AD-5423) is a D2/5-HT2 receptor antagonist, atypical antipsychotic.

132810-10-7
DC7840 BML-190 Featured

BML-190 is an indomethacin morpholinylamide which functions as a selective inverse agonist of the human cannabinoid CB2 receptor.

2854-32-2
DC10459 BMS-986020 Featured

BMS-986020 is an LPA1 antagonist.

1257213-50-5
DC11923 BMS-986120 Featured

BMS-986120 (BMS986120) is a potent, selective, orally bioavailable, and reversible PAR4 antagonist with Kd of 0.098 nM for human PAR4.

1478712-37-6
DC10924 BMS986202 Featured

BMS-986202 is a clinical Tyk2 inhibitor that binds to Tyk2 JH2 with IC50 of 0.19 nM and shows remarkably selectivity over other kinases including Jak family members.

DC9937 BMT-145027

BMT-145027 is a potent mGluR5 PAM with no inherent mGluR5 agonist activity.

2018282-44-3
DC7377 BMY 7378 Featured

BMY 7378 is a multi-targeted inhibitor of α2C-adrenoceptor and α1D-adrenoceptor with pKi of 6.54 and 8.2, respectively, and acts as a mixed agonist and antagonist for 5-HT1A receptor with pKi of 8.3.

21102-95-4
DC9437 Bosentan

Bosentan is a competitive and dual antagonist of endothelin-1 at the endothelin-A (ET-A) and endothelin-B (ET-B) receptors.

147536-97-8
DCAPI1483 Bosentan Hydrate

Bosentan is an endothelin (ET) receptors antagonist for ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively.

157212-55-0
DC8883 BP897 Featured

BP897 is a partially selective D3 dopamine receptor agonist.

314776-92-6
DC10618 BPTU Featured

BPTU is an Allosteric antagonist of P2Y1 (EC50 = 0.06-0.3 μM).

870544-59-5
DC8392 BQ-123 Featured

BQ-123 is a selective endothelin A receptor (ETA) antagonist with IC50 of 7.3 nM. Phase 2.

136553-81-6
DC10338 Bradykinin

Bradykinin is an active peptide that is generated by the kallikrein-kinin system. It is a inflammatory mediator and also recognized as a neuromediator and regulator of several vascular and renal functions.

58-82-2
DC7097 Cebranopadol(GRT-6005) Featured

branopadol(GRT-6005) is a novel first in class compounds with potent agonist activity on ORL-1 (opioid receptor like -1) and the well established mu opioid receptor.

863513-91-1
DC8286 Brexpiprazole(OPC34712) Featured

Brexpiprazole is a novel D2 dopamine partial agonist.

913611-97-9
DC7888 BRL54443

BRL 54443 is a 5-HT1E and 5-HT1F receptor agonist with pKi of 8.7 and 9.25, respectively, with a weak binding affinity for 5-HT1A, 5-HT1B, 5-HT1D receptors.

57477-39-1
DC7091 BRL-15572 dihydrochloride

BRL-15572 2Hcl is a 5-HT1D receptor antagonist with pKi of 7.9, also shows a considerable affinity at 5-HT1A and 5-HT2B receptors, exhibiting 60-fold selectivity over 5-HT1B receptor.

1173022-77-9
DC9141 Brompheniramine hydrogen maleate

Brompheniramine maleate is a histamine H1 receptors antagonist.

980-71-2
DC10954 BS148

BS148 (BS-148) is a potent, selective σ2 receptor agonist with pKi of 7.71, displays 25-fold selectivity over σ1.

2162116-09-6
DC10945 BU09059

BU09059 is a potent, selective, short-acting kappa-opioid receptor antagonist with Ki of 1.72 nM, displays 15- and 616-fold selectivity over μ- and δ-receptors respectively.

1541206-05-6
DC10693 O-Butyryl timolol Featured

Butyryltimolol is a lipophilic ester prodrug of timolol, a beta adrenergic blocer with antihypertensive and hemodynamic properties.

106351-79-5
DC7675 BX-471(ZK 811752) Featured

BX471 is a potent, selective non-peptide CCR1 antagonist (Ki = 1 nM for human CCR1); exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.

217645-70-0
DC9423 Cabergoline

Cabergoline, an ergot derivative, is a potent dopamine receptor agonist on D2 receptors.

81409-90-7
DC9386 Calcium-Sensing Receptor Antagonists I

Calcium-Sensing Receptor Antagonists I is an antagonist of calcium-sensing parathyroid hormone receptors.

478963-79-0
DC9185 Candesartan cilexetil Featured

Candesartan Cilexetil (TCV-116) is an angiotensin II receptor antagonist used mainly for the treatment of hypertension.

145040-37-5
DC9142 Candesartan

Candesartan is an angiotensin II receptor antagonist with IC50 of 0.26 nM.

139481-59-7
DC7005 Cangrelor free acid Featured

Cangrelor is a P2Y12 inhibitor, and was approved in June 2015 as an antiplatelet drug for intravenous application. Cangrelor is a high-affinity, reversible inhibitor of P2Y12 receptors that causes almost complete inhibition of ADP-induced platelet aggrega

163706-06-7
DC10222 CarbinoxaMine Maleate

Carbinoxamine maleate is a histamine-H1 receptor blocking agent with antihistamine and anticholinergic properties.

3505-38-2
DC8054 Cariprazine (RGH-188) Featured

Cariprazine (RGH-188) is a novel putative antipsychotic drug that exerts partial agonism at dopamine D2/D3 receptors, with preferential binding to D3 receptors, and partial agonism at serotonin 5-HT1A receptors.

839712-12-8
DC11354 Carteolol (hydrochloride)

Carteolol is an antagonist of β-adrenergic receptors (Kd = 13 nM).

51781-21-6
DC10847 CAY10441(RO1138452) Featured

CAY10441 is a Selective prostacyclin IP receptor antagonist.

221529-58-4
DC12099 CAY10595

CAY10595 is a potent CRTH2/DP2 receptor antagonist that binds to the human receptor with a Ki of 10 nM.

916047-16-0
DC11204 CCR6 inhibitor 35

CCR6 inhibitor 35 is a potent and selective CCR6 inhibitor with IC50 of 6.0 nM (hCCR6).

DC10206 CCX140

CCX140 is a potent CCR2 antagonist.

1100318-47-5
DC10357 Cenerimod

Cenerimod (ACT-334441) is a potent and orally available sphingosine 1-phosphate 1 receptor (S1P1) agonist extracted from patent WO 2016184939 A1 and WO 2011007324 A1, example 1, with an EC50 of 2.7 nM.

1262414-04-9
DC9765 CERC-501(LY-2456302,Aticaprant) Featured

CERC-501(LY-2456302) is a potent, selective antagonist of the kappa opioid receptor (KOR) (Ki = 0.81 nM vs. 24.0 nM and 155 nM for the μ-opioid receptor (MOR) and δ-opioid receptor (DOR), respectively.

1174130-61-0
DC9154 Cetirizine 2HCl

Cetirizine 2Hcl, a second-generation antihistamine, is a major metabolite of hydroxyzine, and a racemic selective H1 receptor inverse agonist used in the treatment of allergies, hay fever, angioedema, and urticaria.

83881-52-1
DC10440 Namodenoson (CF-102) Featured

CF-102(2-Cl-IB-MECA) is a selective A3 adenosine receptor agonist (Ki = 0.33 nM). Displays 2500- and 1400-fold selectivity over A1 and A2A receptors respectively. target: A3 adenosine receptor agonist;

163042-96-4
DC8471 CGS 21680 hydrochloride Featured

CGS 21680 hydrochloride is an A2A adenosine receptor agonist (Ki = 27 nM).

124431-80-7
DC9111 Chlorpheniramine Maleate

Chlorpheniramine maleate is an histamine H1 receptor antagonist with IC50 of 12 nM.

113-92-8
DC9062 Chlorprothixene

Chlorprothixene has strong binding affinities to dopamine and histamine receptors, such as D1, D2, D3, D5, H1, 5-HT2, 5-HT6 and 5-HT7, with Ki of 18 nM, 2.96 nM, 4.56 nM, 9 nM, 3.75 nM, 9.4 nM, 3 nM and 5.6 nM, respectively.

113-59-7
DC10873 CID16020046 Featured

CID 16020046 is a potent and selective GPR55(LPI receptor) antagonist; inhibitsGPR55 constitutive activity with IC50 of 0.15 uM.

834903-43-4
DC9002 Cimetidine

Cimetidine is a histamine-2 (H2) receptor antagonist.

51481-61-9
DC8801 Cinacalcet (AMG-073) Featured

Cinacalcet(AMG-073) is an orally active, second-generation calcimimetic compound; AMG 073 represents a new class of compounds for the treatment of hyperparathyroidism.

226256-56-0
DC9896 Cinnarizine Featured

Cinnarizine is a medication derivative of piperazine, and characterized as an antihistamine and a calcium channel blocker.

298-57-7
DC2062 Ciproxifan (FUB-359) Featured

Ciproxifan is an antagonists of H3-type histamine receptors.

184025-18-1
DC9466 Ciproxifan (maleate) Featured

Ciproxifan maleate(FUB-359 maleate) is a highly potent and selective histamin H3-receptor antagonist with IC50 of 9.2 nM, with low apparent affinity at other receptor subtypes.

184025-19-2
DC3147 Clopidogrel hydrogensulfate

Clopidogrel (Plavix) is an oral, thienopyridine class antiplatelet agent.

120202-66-6
DCAPI1417 Clopidogrel

Clopidogrel is an irreversible inhibitor of the P2Y12 receptor, which is responsible for initiating signal transduction via a GPCR. The signal cascade initiates platelet aggregation and thus clopidogrel has the effect of “thinning” the blood.

113665-84-2
DCAPI1545 Cloprostenol sodium

Cloprostenol Sodium is a synthetic F series prostaglandin that functions as a potent agonist towards the PGF2αR (FP receptor). It is known that Cloprostenol Sodium is less selective than other agonists such as fluprostenol, however it displays more potenc

55028-72-3
DC7991 8-​Chloro-​11-​(4-​methyl-​1-​piperazinyl)​-​5H-​dibenzo[b,e]​(1,4)​diazepine N-oxide Featured

Clozapine N-oxide is a major metabolite of Clozapine noted to decrease SR-2A (5-HT2 serotonin receptor) density in vitro.

34233-69-7
DC9067 Clozapine

Clozapine(HF 1854) is a 5-HT2A/2C and dopamine receptor blocker with Ki values of 21, 170, 170, 230 and 330 nM for D4, D3, D1, D2 and D5 receptors respectively.

5786-21-0
DCAPI1091 Conivaptan hydrochloride Featured

Conivaptan(YM 087) is a non-peptide inhibitor of antidiuretic hormone (vasopressin receptor antagonist) with Ki values of 0.48 and 3.04 nM for rat liver V1A receptor and rat kidney V2 receptor respectively.

168626-94-6
DC11048 Contilisant

Contilisant is a neuroprotective, non-toxic, antioxidant, permeable ligand, showing in vitro pharmacological properties on the selected biological targets (hAChE IC50=0.53 uM.

2135615-68-6
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