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. |
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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. |
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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. |
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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. |
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DC22684 |
JNJ-46778212
Featured
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A potent, selective, CNS penetrant and orally bioavailable mGlu5 positive allosteric modulator that potentiates human mGlu5 with EC50 of 260 nM. |
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DC11558 |
DLK-IN-14 |
A potent, selective, CNS penetrant dual leucine zipper kinase (DLK, MAP3K12) inhibitor with Ki of 3 nM. |
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DC11870 |
RORγt-IN-9a |
A potent, selective, CNS penetrant, orally bioavailable RORγt with pIC50 of 8.3 in FRET assays. |
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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. |
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DC22903 |
SW-106
Featured
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SW106 is a potent, selective, competitive PTH/PTH-related peptide receptor (PPR) antagonist with IC50 of 0.99 uM. |
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DC11898 |
Gosogliptin |
A potent, selective, competitive, orally active dipeptidyl peptidase-4 (DPP-4) inhibitor with IC50 of 13 nM. |
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DC11899 |
Gosogliptin dihydrochloride |
A potent, selective, competitive, orally active dipeptidyl peptidase-4 (DPP-4) inhibitor with IC50 of 13 nM. |
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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.. |
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DC21442 |
ONO 2050297 |
A potent, selective, dual CysLT1 and CysLT2 antagonist with IC50 of 17 and 0.87 nM, respectively.. |
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DC11666 |
BMS-470539 |
A potent, selective, full agonist of human and murine MC1R with EC50 of 16.8 and 11.6 nM, respectively. |
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DC20736 |
AZD 9272 |
A potent, selective, highly CNS-penetrant and orally available mGluR5 negative allosteric modulator Kd of 2.8 nM. |
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DC20723 |
AZD 2066 |
A potent, selective, highly CNS-penetrant mGluR5 antagonist. |
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DC11721 |
PF-06747775 |
A potent, selective, irreversible EGFR mutants with IC50 of 12, 3, 4 and 5 nM for EGFR L858R-T790M, Del-T790M, L858R, and EGFR Del, respectively. |
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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. |
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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). |
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DC22804 |
CMPD-1 |
A potent, selective, non-ATP-competitive inhibitor of p38α-mediated MK2a phosphorylation with apparent Ki of 330 nM. |
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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.. |
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DC23195 |
CBR-5884
Featured
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A potent, selective, noncompetitive inhibitor of 3-phosphoglycerate dehydrogenase (PHGDH) with IC50 of 7 uM. |
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DC11746 |
JNJ-27141491 |
A potent, selective, noncompetitive, orally active CCR2 antagonist with IC50 of 172 nM. |
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DC22449 |
PD-146176 |
A potent, selective, non-competitve inhibitor of 15-lipoxygenase (15-LOX) with Ki of 197 nM. |
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DC22447 |
FAAH-IN-2 |
A potent, selective, noncovalent FAAH inhibitor with IC50 of 28 nM toward human FAAH and 100 nM toward rat FAAH. |
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DC11756 |
SR 140333 |
A potent, selective, non-peptide NK1 receptor antagonist with Ki of 0.74 nM, IC50 of 1.6 nM. |
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DC22680 |
Conivaptan |
A potent, selective, nonpeptide vasopressin V1A and V2 receptor antagonist with Ki of 0.48 nM and 3.04 nM respectively. |
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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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DC20617 |
AA-CW236
Featured
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A potent, selective, non-pseudosubstrate inhibitor of O(6) -alkylguanine DNA methyltransferase (MGMT) with low-nanomolar potency. |
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DC21593 |
RUC-4
Featured
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A potent, selective, non-RGD-mimetic αIIbβ3 integrin receptor antagonist with IC50 of 45 nM, with no activity on αVβ3 receptors. . |
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