DC23596 |
Luseogliflozin |
A potent, selective, orally acitve SGLT2 inhibitor with IC50 of 2.26 nM, 1650-fold selectivity over SGLT1. |
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DC21307 |
MKC-733 |
A potent, selective, orally active 5-HT3 receptor agonist with high affinity for canine intestinal smooth muscle 5-HT3 receptors. |
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DC11667 |
PF-592379 |
A potent, selective, orally active agonist of dopamine D3 receptor with EC50 of 21 nM. |
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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. |
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DC20774 |
VTP 37948 |
A potent, selective, orally active BACE1 inhibitor for the treatment of Alzheimer's disease.. |
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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. |
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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. |
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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. |
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DC21187 |
JTE907
Featured
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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. |
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DC21793 |
VER-250840 |
A potent, selective, orally active Chk1 inhibitor with IC50 of < 1 nM, Ki=69 pM. |
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DC22898 |
L-365260 |
A potent, selective, orally active cholecystokinin receptor 2 (CCK2) antagonist with IC50 of 2 nM. |
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DC22485 |
Gefitinib hydrochloride
Featured
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A potent, selective, orally active EGFR inhibitor with IC50 of 23 nM. |
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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. |
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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). |
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DC11704 |
CFI-401870 |
A potent, selective, orally active Mps1 (TTK) inhibitor with IC50 of 3.1 nM. |
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DC25200 |
PF-1355
Featured
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PF-1355 is a potent, selective, orally active Myeloperoxidase (MPO) inhibitor with EC50 of 1.47 uM. |
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DC22900 |
MLE-4901
Featured
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A potent, selective, orally active neurokinin 3 (NK3R) antagonist for the treatment of schizophrenia. |
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DC22664 |
Fezolinetant
Featured
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Fezolinetant is an antagonist of the neurokinin 3 receptor (NK3R), used for the treatment of menopausal hot flushes. |
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DC22686 |
SCH 221510 |
A potent, selective, orally active nociceptin opioid receptor (NOP) agonist with EC50 of 12 nM, Ki of 0.3 nM. |
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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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DC11615 |
γ-secretase modulator 14a |
A potent, selective, orally active γ-secretase modulator with Aβ42 IC50 of 39 nM. |
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