NUCC-390 dihydrochloride (NUCC390) is a small molecule agonist of CXCR4, recapitulates the activity of CXCL12α.

LN6023 (LN-6023) a potent, selective and first-in-class inhibitor of the atypical chemokine receptor 3 (ACKR3, CXCR7) with β-arrestin EC50 of 3.5 uM.

Ki19003 (Ki 19003) is a potent, specific CCR3 antagonist, inhibits the CCL11-induced migration of CCR3-expressing L1.2 cells with IC50 of 20 nM.

GW782415W (GW782415) is a potent, specific CCR3 antagonist, inhibits chemotaxis of human and murine eosinophils pKi of 8.08 and 7.85, respectively.

DF2755A is a selective, allosteric, orally acting inhibitor of CXCR1/2 (Kd=2.24/0.94 nM), inhibits human PMN (hPMN) migration induced by CXCL8 and CXCL1 with IC50 of 4.2 and 2.1 nM, respectively.

AZD3778 (AZD-3778) is a dual CCR3 and H1-receptor antagonistwith Ki of 54 nM for guinea-pig H1-receptor, inhibits binding of CR3 radioligand 125I-eotaxin to human CCR3-receptor expressed on CHO-cells with IC50 of 8 nM.

AZ12436092 (AZ 12436092) is a potent, selective CCR3 antagonist with binding pKi value of 9.2.

ACT-672125 (ACT672125) is a potent, selective CXCR3 antagonist with IC50 of 239 nM in human blood.

BMS-694153 is a potent, selective calcitonin gene-related peptide (CGRP) receptor antagonist with Ki of 0.013 nM for hCGRP (inhibition of 125I-CGRP binding in SK-N-MC cell membranes).

URB447 (URB-447) is a peripherally restricted CB(1) antagonist/CB(2) agonist with IC50 of 313 nM (rat CB1) and 41 nM (human CB2).

LEI-102 (LEI 102) is a potent, selective cannabinoid CB2 receptor agonist with binding pKi of 8.0, 1000-fold selectivity over CB1R.

JWH133 (JWH-133) is a potent and selective CB2 agonist with Ki of 3.4 nM, 200-fold selective over CB1 receptors, inhibits glioma growth in vivo.

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.