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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

Proglumide sodium is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide sodium selective blocks CCK’s effects in the central nervous system (CNS). Proglumide sodium has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide sodium also has antiepileptic and antioxidant activities.

SUN B8155, a non-peptide agonist of calcitonin (CT) receptor, selectively mimics the biological actions of calcitonin. Calcitonin, a 32-amino acid peptide hormone secreted mainly from the thyroid gland, plays an important role in maintaining bone homeostasis.

ML 339 is a potent and selective hCXCR6 antagonist (IC50 = 140 nM), 100-fold less active at the murine CXCR6 receptor (IC50 = 18 uM); ML 339 exhibits selectivity over CXCR5, CXCR4, CCR6 and APJ receptors.