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. |
|
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. |
|
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. |
|
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. |
|
DC24065 |
EPZ-011989 trifluoroacetate |
A potent, selective, orally bioavailable inhibitor of EZH2 with Ki of < 3 nM. |
|
DC23552 |
AS-2444697 HCl
Featured
|
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. |
|
DC22941 |
AZD-9056 |
A potent, selective, orally bioavailable P2X7 receptor antagonist. |
|
DC21607 |
SB-649868
Featured
|
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). |
|
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. |
|
DC20691 |
ASP 3652 |
A potent, selective, peripherally active and orally available FAAH inhibitor for treatment of chronic prostatitis/chronic pelvic pain syndrome.. |
|
DC23043 |
Tpl2-IN-2p |
A potent, selective, reversible and ATP-competitive inhibitor of Tpl2 kinase with IC50 of 50 nM. |
|
DC23933 |
MK-0893 |
A potent, selective, reversible and competitive antagonist of glucagon receptor with high binding affinity (IC(=50=6.6 nM) and functional cAMP activity (IC50=15.7 nM). |
|
DC20412 |
II-B08 |
A potent, selective, reversible inhibitor of PTP SHP2 with IC50 of 5.5 uM, exhibits >3-fold selectivity for SHP2 over other PTPs. |
|
DC11875 |
GlpG inhibitor 11 |
A potent, selective, reversible rhomboid proteases inhibitor with Ki of 45 nM for GlpG . |
|
DC22892 |
KNT-127 |
A potent, selectove δ-opioid receptor agonist with Ki of 0.16 nM, dispalys 133.5-fold and 960.5-fold selectivity over μOR and κOR respectively. |
|
DC22563 |
TN1 |
A potent, small molecule fetal hemoglobin (HbF) inducer with EC50 of 100 nM. |
|
DC20606 |
8-Thioquinoline |
A potent, small molecule inhibitor of the proteasome subunit Rpn11 with IC50 of 2.5 uM.. |
|
DC21321 |
ML349
Featured
|
A potent, specific acyl protein thioesterase 2 (APT-2, LYPLA2) inhibitor with IC50 of 144 nM and Ki of 120 nM, >20-fold selectivity over APT-1 and serine hydrolase enzyme family. |
|
DC22529 |
FPTQ |
A potent, specific and allosteric mGluR1 antagonist with IC50 of 6 nM and 1.4 nM for human and mouse mGluR1, respectively.. |
|
DC25075 |
Sivelestat sodium |
A potent, specific and competitive inhibitor of human neutrophil elastase with IC50 of 44 nM. |
|
DC23074 |
Sivelestat
Featured
|
A potent, specific and competitive inhibitor of human neutrophil elastase with IC50 of 44 nM. |
|
DC23494 |
GRI 977143
Featured
|
A potent, specific and nonlipid agonist of LPA2 receptor with EC50 of 3.3 uM, does not activate any of the other LPA GPCRs (>10 uM). |
|