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. |
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DC21148 |
IPI-443 |
A potent, selective, orally active p110δ/γ PI3K dual inhibitor with cellular IC50 of 0.29 and 7.1 nM, respectively. |
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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). |
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DC23441 |
CS-0777 |
A potent, selective, orally active S1P receptor-1 (S1P1) agonist with EC50 of 1.1 nM, 320-fold selectivity over S1P3. |
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DC25065 |
NIBR 0213
Featured
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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). |
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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. |
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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). |
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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. |
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DC20654 |
AM-0902
Featured
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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). |
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DC21179 |
JNJ 41876666 |
A potent, selective, orally active TRPM8 channel antaognist with IC50 of 0.8 nM, . |
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DC23198 |
Adomeglivant |
A potent, selective, orally active, small-molecule antagonist of human glucagon receptor with Ki of 6.66 nM. |
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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. |
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DC23581 |
TASP0315003 |
A potent, selective, orally available GlyT1 inhibitor with IC50 of 1.6 nM, weakly inhibits rat GlyT2 (IC50=138 nM). |
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DC23611 |
DCCCyB |
A potent, selective, orally available GlyT1 inhibitor with IC50 of 29 nM, demonstrates excellent in vivo occupancy of GlyT1 transporters in vivo.. |
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DC23599 |
PF-0346275
Featured
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PF-0346275 is a potent, selective, orally available GlyT1 inhibitor with Ki of 11.6 nM, without activity against GlyT2 (IC50>10 uM). |
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DC23486 |
DS-1558 |
A potent, selective, orally available GPR40 agonist with EC50 of 3.7 nM. |
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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. |
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DC24182 |
Nilotinib monohydrochloride monohydrate
Featured
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A potent, selective, orally available inhibitor of both native and mutant Bcr-Abl with IC50 of 20-80 nM. |
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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. |
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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. |
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DC21177 |
JNJ 39758979
Featured
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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. |
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DC24048 |
NVP-BKM120 hydrochloride
Featured
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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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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. |
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DC24065 |
EPZ-011989 trifluoroacetate |
A potent, selective, orally bioavailable inhibitor of EZH2 with Ki of < 3 nM. |
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DC23552 |
AS-2444697 HCl
Featured
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A potent, selective, orally bioavailable IRAK-4 inhibitor that potently inhibits human and rat IRAK-4 activity with subnanomolar order, >30-fold selectivity over IRAK-1. |
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DC22941 |
AZD-9056 |
A potent, selective, orally bioavailable P2X7 receptor antagonist. |
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DC21607 |
SB-649868
Featured
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SB-649868 is a potent and selective orally active orexin (OX) 1 and OX2 receptor antagonist (pKi =9.4 and 9.5 at the OX1 and OX2 receptor, respectively). |
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DC21598 |
RWJ-56110 |
A potent, selective, peptide-mimetic PAR-1 antagonist with binding IC50 of 0.44 uM, with no effect on PAR-2, PAR-3, or PAR-4. |
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DC20691 |
ASP 3652 |
A potent, selective, peripherally active and orally available FAAH inhibitor for treatment of chronic prostatitis/chronic pelvic pain syndrome.. |
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DC23043 |
Tpl2-IN-2p |
A potent, selective, reversible and ATP-competitive inhibitor of Tpl2 kinase with IC50 of 50 nM. |
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