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Inhibitors & Agonists

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Cat. No. Product Name Field of Application Chemical Structure
DC22686 SCH 221510 A potent, selective, orally active nociceptin opioid receptor (NOP) agonist with EC50 of 12 nM, Ki of 0.3 nM.
DC21276 Seltorexant A potent, selective, orally active orexin-2 receptor (OX2R) antagonist with pKi of 8.0 and 8.1 for human and rat OX2R, respectively.
DC21148 IPI-443 A potent, selective, orally active p110δ/γ PI3K dual inhibitor with cellular IC50 of 0.29 and 7.1 nM, respectively.
DC20681 AS1940477 A potent, selective, orally active p38α/p38β inhibitor with IC50 of 11.2/36.5 nM respectively, with no effect on p38γ and δ isoforms (IC50>1 uM).
DC23441 CS-0777 A potent, selective, orally active S1P receptor-1 (S1P1) agonist with EC50 of 1.1 nM, 320-fold selectivity over S1P3.
DC25065 NIBR 0213 Featured A potent, selective, orally active S1P1 antagonist with IC50 of 2.5 nM Ca2+ mobilization assays, without activity on S1P2, S1P3 and S1P4 (IC50>10 uM).
DC21287 MK-4256 A potent, selective, orally active somatostatin receptor SSTR3 antagonist with binding Ki of 0.66 nM, >500-fold selectivity over SSTR1/2/4/5.
DC21295 MK-1421 A potent, selective, orally active somatostatin receptor SSTR3 antagonist with binding Ki of 2.3 nM, >2,500-fold selectivity over SSTR1/2/4/5 (IC50>5 uM).
DC21579 RO 5073012 A potent, selective, orally active TAAR1 partial agonist with Ki of 6 nM, EC50 of 23 nM (hTAAR1), 140-fold selectivity over β2 adrenergic receptors.
DC20654 AM-0902 Featured A potent, selective, orally active TRPA1 channel antagonist with IC50 of 71 and 131 nM for rTRPA1 and hTRPA1 in Ca2+ flux assays respectively, without agonist activity (EC50>40 uM).
DC21179 JNJ 41876666 A potent, selective, orally active TRPM8 channel antaognist with IC50 of 0.8 nM, .
DC11615 γ-secretase modulator 14a A potent, selective, orally active γ-secretase modulator with Aβ42 IC50 of 39 nM.
DC23198 Adomeglivant A potent, selective, orally active, small-molecule antagonist of human glucagon receptor with Ki of 6.66 nM.
DC22681 E 6130 A potent, selective, orally available CX3C chemokine receptor 1 (CX3CR1) modulator that inhibits the fractalkine-induced chemotaxis of human peripheral blood NK cells with IC50 of 4.9 nM.
DC23581 TASP0315003 A potent, selective, orally available GlyT1 inhibitor with IC50 of 1.6 nM, weakly inhibits rat GlyT2 (IC50=138 nM).
DC23611 DCCCyB A potent, selective, orally available GlyT1 inhibitor with IC50 of 29 nM, demonstrates excellent in vivo occupancy of GlyT1 transporters in vivo..
DC23599 PF-0346275 Featured PF-0346275 is a potent, selective, orally available GlyT1 inhibitor with Ki of 11.6 nM, without activity against GlyT2 (IC50>10 uM).
DC23486 DS-1558 A potent, selective, orally available GPR40 agonist with EC50 of 3.7 nM.
DC11683 LY2881835 A potent, selective, orally available GPR40 agonist with EC50 of 8 nM.
DC11682 LY2922083 A potent, selective, orally available GPR40 agonist with EC50 of 9 nM.
DC11680 LY3104607 A potent, selective, orally available GPR40 agonist with Ki of 15 nM, β-arrestin EC50 of 108 nM.
DC23300 T-3256336 A potent, selective, orally available IAP antagonist with IC50 of 1.3, 2.2 and 200 nM for cIAP-1, cIAP-2 and XIAP, respectively.
DC24182 Nilotinib monohydrochloride monohydrate Featured A potent, selective, orally available inhibitor of both native and mutant Bcr-Abl with IC50 of 20-80 nM.
DC23925 Vaniprevir A potent, selective, orally available inhibitor of HCV NS3/4A protease with Ki of 0.05 and 0.9 nM for GT1b and 2a protease, respectively.
DC11620 RIPK2-IN-8 A potent, selective, orally available RIPK2 inhibitor with IC50 of 3 nM.
DC11688 Avacopan Featured Avacopan is a potent, selective, orally availale C5aR (CD88) inhibitor with IC50 of 0.1 nM.
DC23358 CD 161 A potent, selective, orally bioavailable BET bromodomain inhibitor with IC50 of 7.2 and 28.2 nM for BRD4 BD2 and BRD4 BD1, respectively.
DC11623 GPR120 agonist 4x A potent, selective, orally bioavailable GPR120 agonist with EC50 of 42 nM in calcium flux assays.
DC21177 JNJ 39758979 Featured JNJ-39758979 is a selective, orally active, and high-affinity histamine H4 receptor antagonist with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 shows good anti-inflammatory and antipruritic activity.
DC24048 NVP-BKM120 hydrochloride Featured A potent, selective, orally bioavailable inhibitor of class I PI3K isoforms with IC50 of 52 nM/166 nM/116 nM/262 nM for p110α/β/δ/γ, respectively.
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