Novel inhibitors

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Cat. No.	Product Name	Field of Application
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.
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.
DC22882	KRH-3955	A potent, selective, orally bioavailable inhibitor of CXCR4 that efficiently inhibits SDF-1α binding to CXCR4 with IC50 of 0.61 nM.

Novel inhibitors

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