DC22113 |
PF-04895162 |
PF-04895162 (ICA-105665, PF 4895162) is an orally available agonist of neuronal Kv7 potassium channel, opens Kv7.2/7.3 and Kv7.3/7.5 potassium channels, also known as KCNQ2/3 and KCNQ3/5 channels. |
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DC9948 |
SNX-5422(PF04929113)
Featured
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PF-04929113 (SNX-5422) is a potent and selective Hsp90 inhibitor (Kd of 41 nM). PF-04929113 also inhibits Her-2 degradation (IC50 of 37 nM). |
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DC10418 |
PF-04957325 |
PF-04957325 is a highly potent and selective PDE8 inhibitor, with IC50 values of 0.7 nM for PDE8A and less than 0.3 nM for PDE8B. |
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DC23629 |
PF-04958242 |
PF-04958242 is a novel potent, selctive, and orally-active AMPA receptor (AMPAR) positive allosteric modulator (PAM) with Ki of 170 nM, EC50 of 370 nM. |
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DC20164 |
PF-04965842 (Abrocitinib)
Featured
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PF-04965842 is a selective Janus kinase 1 (JAK1) inhibitor, demonstrating potent activity against JAK1 with an IC50 of 29 nM. Its selectivity is evident from its significantly higher IC50 values for other JAK family members: 803 nM for JAK2, > 10,000 nM for JAK3, and 1,250 nM for TYK2. This selectivity profile suggests that PF-04965842 preferentially targets JAK1 over other JAK isoforms, which could be advantageous in reducing off-target effects and improving therapeutic outcomes in conditions where JAK1 signaling is implicated. |
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DC3108 |
PF-04971729 (Ertugliflozin)
Featured
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PF-04971729 is a potent and selective inhibitor of the sodium-dependent glucose cotransporter 2, is currently in phase 2 trials for the treatment of diabetes mellitus. |
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DC8527 |
PF-04979064 |
PF-04979064 is a highly potent and orally bioavailable PI3K/mTOR dual inhibitor developed through structure-based drug design. It inhibited mTOR, PI3Kα, β, δ and γ isoforms and AKT phosphorylation with IC50 as 2.64 nM, 0.395 nM, 0.111 nM, 0.122 nM and 28. |
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DC23667 |
PF-04991532 |
PF-04991532 (PF4991532) is a potent, hepatoselective Glucokinase (GK) activator with EC50 of 90±45 nM. |
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DC9915 |
PF04995274,PF 04995274
Featured
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PF-04995274 is a 5-HT4 receptor partial agonist. It thought to act centrally as a pro-cognitive agent that being developed for the treatment of Alzheimer's disease (AD). |
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DC21475 |
PF-05105679
Featured
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PF-05105679 is a potent, selective TRPM8 channel inhibitor with IC50 of 103 nM (human TRPM8 currents inhibition). |
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DC21486 |
PF-05150122
Featured
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PF-05150122 is a potent, state-dependent, subtype selective Nav1.7 inhibitor with IC50 of 21 nM, no significant activity against Nav1.5.. |
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DC10050 |
PF05175157
Featured
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PF-05175157 is a potent and selective inhibitor of both acetyl-CoA carboxylase isoform ACC1 located primarily in liver and adipose tissue and isoform ACC2 dominant in skeletal and heart muscle, with IC50 values of 27 nM and 33 nM, respectively. |
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DC11937 |
PF 05180999
Featured
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PF-05180999 (PF 5180999) is a potent, selective, brain-penetrating and orally bioavailable phosphodiesterase 2A (PDE2A) inhibitor with IC50 of 1 nM. |
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DC26091 |
PF-05198007
Featured
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PF-05198007 is a potent, state-dependent, subtype selective Nav1.7 inhibitor with IC50 of 9 nM, no significant activity against Nav1.5 (IC50>10 uM). |
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DC22221 |
PF-05212377 |
PF-05212377 (SAM-760, PF 5212377) is a potent and selective 5-HT6 receptor antagonist with potential therapy for the symptomatic treatment of mild to moderate Alzheimer's disease.. |
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DC20145 |
PF-05231023
Featured
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PF-05231023, a long-acting fibroblast growth factor 21 (FGF21) analog, is a FGF21-receptor agonist, suitable for development as a potential treatment for T2DM. |
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DC12334 |
PF-05241328 |
PF-05241328 is a potent and selective inhibitor of human Nav1.7 voltage-dependent sodium channels (Nav1.7), with an IC50 of 31 nM. |
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DC21476 |
PF-05381941
Featured
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PF-05381941 (PF 05381941, PF05381941) is a potent, dual TAK1/p38a inhibitor with IC50 of 156/186 nM respectively, with good kinome selectivity against 50 representative kinases. |
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DC22192 |
PF-05661014 |
PF-05661014 is a potent, selective Nav1.3 inhibitor with IC50 of 0.26 uM, shows no activity for Nav1.7 (IC50>10 uM). |
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DC12518 |
PF-06256142
Featured
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PF-06256142 (PF06256142) is a potent and selective orthosteric agonist of the D1 receptor with EC50 (cAMP) of 33 nM, shows exquisitely selectivity over D2. |
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DC11734 |
PF-06263276 |
PF-06263276 (PF06263276, PF 6263276) is a potent, selective pan JAK inhibitor with IC50 of 2.2, 23.1, 59.9 and 29.7 nM for JAK1, JAK2, JAK3, and TYK2, respectively. |
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DC10631 |
PF-06273340
Featured
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PF-06273340 is a highly potent, kinases elective, well-tolerated pan-Trk inhibitor with IC50 values of 6, 4, 3 nM for TrkA, TrkB, Trk C, respectively. |
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DC10500 |
PF-06282999
Featured
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PF-06282999 is a potent and selective myeloperoxidase inhibitor which is potential useful for the treatment of cardiovascular diseases. |
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DC12594 |
PF-06305591
Featured
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PF-06305591 (PF06305591) is a potent, highly selective selective NaV1.8 blocker with IC50 of 15 nM, displays no significant activity against other sodium channel subtypes, K+ channels and Ca2+ channels. |
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DC21488 |
PF-06372865
Featured
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PF-06372865 is a novel potent, α2/3 functionally selective GABAA receptor positive allosteric modulator. |
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DC11466 |
PF-06409577
Featured
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PF-06409577 is a potent and selective allosteric activator of AMPK α1β1γ1 isoform with an EC50 of 7 nM. |
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DC11185 |
PF-06426779 |
PF-06426779 (PF06426779) is a potent, selective IRAK4 inhibitor with IC50 of 1 nM against full-length IRAK4 kinase and cell-based IC50 of 12 nM. |
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DC22780 |
PF-06446846 hydrochloride
Featured
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PF-06446846 (PF-6446846) is a potent, highly selective inhibitor of PCSK9 translation with IC50 of 0.3 uM for inhibition the secretion of PCSK9 by Huh7 cells. |
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DC22783 |
PF-06446846
Featured
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PF-06446846 (PF-6446846) is a potent, highly selective inhibitor of PCSK9 translation with IC50 of 0.3 uM for inhibition the secretion of PCSK9 by Huh7 cells. |
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DC7971 |
PF-06447475
Featured
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PF-06447475 is a highly potent, selective, brain penetrant LRRK2 inhibitor with IC0 of 3 nM/11 nM for Wt LRRK2/G2019S LRRK2 respectively. |
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