| DC23070 |
MAP4K4-IN-11e |
A potent, selective, ATP-competitive inhibitor of MAP4K4 with IC50 of 1.9 uM, without effect on other stress pathway related kinases. |
|
| DC23964 |
BMS-509744 |
A potent, selective, ATP-competitive ITK inhibitor with IC50 of 19 nM. |
|
| DC22551 |
DFMTI |
A potent, selective, brain penetrant and orally active mGluR1 antagonist with 4.3 nM and 3.6 nM for huam and rat mGluR1, respectively. |
|
| DC22895 |
VU0477573 |
A potent, selective, brain penetrant partial negative allosteric modulator of mGlu5 receptor with Ki of 14 nM, Ca assay IC50 of 32 nM. |
|
| DC22964 |
PQ-10
Featured
|
A potent, selective, brain penetrant PDE10A inhibitor with Ki of 4 nM. |
|
| DC23695 |
PF-05085727 |
A potent, selective, brain penetrant phosphodiesterase 2A (PDE2A) inhibitor with IC50 of 2 nM, >4,000-fold selectivity over PDE1 and PDE3-11. |
|
| DC22920 |
AMN 082 dihydrochloride |
A potent, selective, brain penetrant, orally acitve mGluR7 allosteric agonist that inhibits forskolin-stimulated cAMP accumulation in mGluR7b CHO cells with EC50 of 64±32 nM. |
|
| DC23640 |
ASP2535 |
A potent, selective, brain permeable, orally available glycine transporter-1 (GlyT1) inhibitor with IC50 of 92 nM (rat GlyT1), 50-fold selectivity over GlyT2. |
|
| DC20549 |
SHP2 inhibitor 11a-1 |
A potent, selective, cell active SHP2 inhibitor with IC50 of 200 nM, displays >5-fold selectivity against 20 other mammalian PTPs. |
|
| DC22877 |
CPI703 |
A potent, selective, cell-active CBP/EP300 bromodomain inhibitor with IC50 of 0.47 uM for CBP. |
|
| DC25052 |
Src I338G-IN-3g |
A potent, selective, cell-permeable I338G v-Src inhibitor with IC50 of 430 nM, shows no inhibition of wild-type v-Src at 300 uM. |
|
| DC21474 |
PF-04781340 |
A potent, selective, CNS penetrant 5-HT2C receptor agonist with Ki of 3 nM and EC50 of 9 nM, without significant P-gp efflux liability. |
|
| DC22708 |
VU 0255035 |
A potent, selective, CNS penetrant and competitive orthosteric antagonist of M1 mAChR with IC50 of 132 nM, >75-fold selectivity over M2-M5. |
|
| DC22667 |
mGlu5 PAM 4k |
A potent, selective, CNS penetrant and orally bioavailable mGlu5 positive allosteric modulator that potentiates human mGlu5 with EC50 of 130 nM. |
|
| DC22684 |
JNJ-46778212
Featured
|
A potent, selective, CNS penetrant and orally bioavailable mGlu5 positive allosteric modulator that potentiates human mGlu5 with EC50 of 260 nM. |
|
| DC22730 |
JNJ-42253432 |
A potent, selective, CNS-penetrant P2X7 antagonist with pKi of 9.1 and 7.9 for rat and huamn P2X7 channel, respectively. |
|
| DC22903 |
SW-106
Featured
|
SW106 is a potent, selective, competitive PTH/PTH-related peptide receptor (PPR) antagonist with IC50 of 0.99 uM. |
|
| DC23069 |
KRAS G12C inhibitor 1 |
A potent, selective, covalent KRAS G12C inhibitor that selectively inhibit KRAS G12C-dependent signaling and cancer cell growth at sub-micromolar concentrations.. |
|
| DC21442 |
ONO 2050297 |
A potent, selective, dual CysLT1 and CysLT2 antagonist with IC50 of 17 and 0.87 nM, respectively.. |
|
| 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). |
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