DC20736 |
AZD 9272 |
A potent, selective, highly CNS-penetrant and orally available mGluR5 negative allosteric modulator Kd of 2.8 nM. |
|
DC20723 |
AZD 2066 |
A potent, selective, highly CNS-penetrant mGluR5 antagonist. |
|
DC22679 |
CM 572 |
A potent, selective, irreversible sigma-2 receptor partial agonist with Ki of 14.6 nM, >700-fold selectivity over sigma-1 receptors. |
|
DC23412 |
BMS-955829 |
A potent, selective, low glutamate fold shift (2.4) mGluR5 positive allosteric modulator with EC50 of 2.6 nM, without inherent mGluR5 agonist activity (EC50>30 uM). |
|
DC22804 |
CMPD-1 |
A potent, selective, non-ATP-competitive inhibitor of p38α-mediated MK2a phosphorylation with apparent Ki of 330 nM. |
|
DC22742 |
KAB-18 |
A potent, selective, noncompetitive human α4β2 nAChRs negative allosteric modulator with IC50 of 13.5 uM, displays no inhibitory activity on Hα3β4 nAChRs at 100 uM.. |
|
DC23195 |
CBR-5884
Featured
|
A potent, selective, noncompetitive inhibitor of 3-phosphoglycerate dehydrogenase (PHGDH) with IC50 of 7 uM. |
|
DC22449 |
PD-146176 |
A potent, selective, non-competitve inhibitor of 15-lipoxygenase (15-LOX) with Ki of 197 nM. |
|
DC22447 |
FAAH-IN-2 |
A potent, selective, noncovalent FAAH inhibitor with IC50 of 28 nM toward human FAAH and 100 nM toward rat FAAH. |
|
DC22680 |
Conivaptan |
A potent, selective, nonpeptide vasopressin V1A and V2 receptor antagonist with Ki of 0.48 nM and 3.04 nM respectively. |
|
DC21738 |
TBC3486 |
A potent, selective, non-peptidic integrin α4β1 (VLA-4) antagonist with IC50 of 9 nM, displays 200-fold selectivity over α4β7 (IC50=2.1 uM). |
|
DC20617 |
AA-CW236
Featured
|
A potent, selective, non-pseudosubstrate inhibitor of O(6) -alkylguanine DNA methyltransferase (MGMT) with low-nanomolar potency. |
|
DC21593 |
RUC-4
Featured
|
A potent, selective, non-RGD-mimetic αIIbβ3 integrin receptor antagonist with IC50 of 45 nM, with no activity on αVβ3 receptors. . |
|
DC23596 |
Luseogliflozin |
A potent, selective, orally acitve SGLT2 inhibitor with IC50 of 2.26 nM, 1650-fold selectivity over SGLT1. |
|
DC21307 |
MKC-733 |
A potent, selective, orally active 5-HT3 receptor agonist with high affinity for canine intestinal smooth muscle 5-HT3 receptors. |
|
DC21606 |
SB-357134 |
A potent, selective, orally active and CNS penetrant 5-HT6 receptor antagonist with pKi of 8.5, displays 1300-fold selectivity over other 13 5-HT receptor subtypes. |
|
DC20774 |
VTP 37948 |
A potent, selective, orally active BACE1 inhibitor for the treatment of Alzheimer's disease.. |
|
DC20665 |
AMG 8718 |
A potent, selective, orally active BACE1 inhibitor with IC50 of 0.7 nM, demonstrates limited selectivity for over BACE2 and high selectivity both renin and pepsin. |
|
DC20324 |
BRS-3 agonist Compound A |
A potent, selective, orally active bombesin receptor subtype-3 (BRS-3) agonist with EC50 of 250/100 nM for human/rat BRS-3, resp+H1437+M1438. |
|
DC20325 |
BRS-3 agonist Compound A racemate |
A potent, selective, orally active bombesin receptor subtype-3 (BRS-3) agonist with EC50 of 270/130 nM for human/rat BRS-3, respectively. |
|
DC21187 |
JTE907
Featured
|
A potent, selective, orally active cannabinoid CB2 receptor inverse agonist with Ki of 35.9, 1.55 and 0.38 nM for human, mouse and rat CB2, respectively. |
|
DC21793 |
VER-250840 |
A potent, selective, orally active Chk1 inhibitor with IC50 of < 1 nM, Ki=69 pM. |
|
DC22898 |
L-365260 |
A potent, selective, orally active cholecystokinin receptor 2 (CCK2) antagonist with IC50 of 2 nM. |
|
DC22485 |
Gefitinib hydrochloride
Featured
|
A potent, selective, orally active EGFR inhibitor with IC50 of 23 nM. |
|
DC21443 |
ONO-5334 |
A potent, selective, orally active inhibitor of cathepsin K with Ki of 0.1 nM, 0.049 nM and 0.85 nM for human, rabbit and rat cathepsin K, respectively. |
|
DC23340 |
CCT-251455 |
A potent, selective, orally active monopolar spindle 1 (MPS1) inhibitor with IC50 of 3 nM, with no activity for CDK2 and Aurora A (IC50>40 uM). |
|
DC25200 |
PF-1355
Featured
|
PF-1355 is a potent, selective, orally active Myeloperoxidase (MPO) inhibitor with EC50 of 1.47 uM. |
|
DC22900 |
MLE-4901
Featured
|
A potent, selective, orally active neurokinin 3 (NK3R) antagonist for the treatment of schizophrenia. |
|
DC22664 |
Fezolinetant
Featured
|
Fezolinetant is an antagonist of the neurokinin 3 receptor (NK3R), used for the treatment of menopausal hot flushes. |
|
DC22686 |
SCH 221510 |
A potent, selective, orally active nociceptin opioid receptor (NOP) agonist with EC50 of 12 nM, Ki of 0.3 nM. |
|