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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC22195 PF-6689840
PF-6689840 (PF6689840) is a potent and selective Type II PTK6/Brk inhibitor with IC50 of 54 nM in biochemical assays.
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DC11320 PF-6274484
PF-6274484 is an inhibitor of the EGF receptor (EGFR; IC50s = 0.18 and 0.14 nM for wild-type EGFR and inhibitor-resistant EGFRL858R/T790M, respectively).
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DC11188 PF-4778574
PF-4778574 (PF4778574) is a brain penetrant, positive allosteric modulator (potentiator) of AMPA receptor with Ki of 85 nM, increases S-AMPA-evoked responses in rat primary cortical neurons with EC50 of 45-919 nM.
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DC23247 PF-4776548
PF-4776548 (PF-04776548) novel HIV integrase inhibitor for treatment of HIV infections..
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DC11808 PF-46396
PF-46396 is a specific small-molecule inhibitor of HIV-1 Gag maturation that interferes specifically with the cleavage of the CA/SP1 (p25) Gag precursor to the mature CA (p24) protein.
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DC21473 PF-4363467
PF-4363467 (PF 04363467) is a novel highly potent, brain penetrant dopamine D3/D2 receptor antagonist with Ki of 1.3/692 nM respectively, with high selectivity for D3R versus other biogenic amine receptors.
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DC21859 PF-3893787
PF-3893787 (ZPL 3893787) is a potent and selective H4 receptor antagonist with binding Ki of 2.4 nM.
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DC8152 PF3845yne
PF3845yne is a Alkyne analogues of PF3845.
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DC23449 PF-3635659
PF-3635659 (PF-03635659) is a potent, very long dissociative half-life (slow off-rate, >1440 min) muscarinic M3 antagonist with Ki of 0.2 nM, shows potential for the treatment of chronic obstructive pulmonary disease (COPD)..
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DC22421 PF-232798
PF-232798 (PF-00232798) is a potent CCR5 antagonist with IC50 of <0.1 nM in gp160 fusion assay, exhibits potent broad-spectrum anti-HIV-1 activity.
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DC22907 PF-219061
PF-219061 (PF 219061, PF219061) is a potent, selective agonist of dopamine D3 receptor with EC50 of 8 nM.
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DC23575 PF-184298
PF-184298 is a potent, selective dual serotonin and noradrenaline monoamine reuptake inhibitor (SNRI) with IC50 of 6 nM and 21 nM, respectively.
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DC21494 PF-152
PF-152 is a potent, highly selective and orally bioavailable MMP13 inhibitor with Ki of 1.5 nM, with no activity against MMP3 (Ki>10 uM).
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DC11153 PF-06855800
PF-06855800 (PF06855800) is a potent, selective, SAM competitive, BBB-penetrant, orally active inhibitor of protein arginine methyltransferase PRMT5 with Ki of 0.02 nM.
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DC11116 PF-06827443
PF-06827443 (PF06827443) is a potent, orally bioavailable, and CNS-penetrant M1-selective positive allosteric modulator (PAM) with EC50 of 47 nM, shows no activity against M2-M5 at 10 uM.
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DC21480 PF-06815345
PF-06815345 (PF 6815345) is a potent prodrug PCSK9 modulator that inhibits PCSK9 secretion in vitro translation assay.
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DC21493 PF-06815189
PF-06815189 is a potent, selective phosphodiesterase 2 (PDE2) inhibitor with IC50 of 0.4 nM, >1,000-fold selectivity over PDE5.
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DC22755 PF-06807656
PF-06807656 is a potent, selective renal outer medullary potassium channel (ROMK, Kir1.1a) inhibitor with IC50 of 61 nM for hROMK in patch-clamp assays.
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DC21492 PF-06795071
PF-06795071 is a potent, selective, covalent Monoacylglycerol Lipase (MAGL) inhibitor with IC50 of 3 nM, >1,000-fold selectivity over FAAH.
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DC11111 PF-06764427
PF-06764427 (PF06764427) is a potent, selective M1 muscarinic acetylcholine receptor (mAChR) positive allosteric modulator with EC50 of 55 nM, has no measurable agonist or PAM activity at the M2-M5 receptors at 10 uM.
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DC21491 PF-06751979
PF-06751979 is a potent, selective, brain penetrant BACE1 inhibitor with binding IC50 of 7.3, 27-fold selectivity over BACE2.
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DC11224 PF-06747711
PF-06747711 (PF06747711) is a potent, selective, orally bioavailable RORC2 (RORγt) inverse agonist with IC50 of 4.1 nM.
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DC10634 PF-06726304
PF-06726304 is a selective EZH2 inhibitor with Ki values of 0.7 nM and 3 nM for WT EZH2 and Y641N respectively; also inhibits H3K27me3 with the IC50 value of 15 nM.
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DC21490 PF-06679142
PF-06679142 is a novel potent, orally active, α1β1γ1/α2β1γ1-isoform selective AMPK activator with Kd of 14 nM, EC50 of 22 nM for α1β1γ1-AMPK, shows minimal activity at the β2-containing isoforms (α1β2γ1, α2β2γ1, α2β2γ3).
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DC11966 PF-06678419
PF-06678419 (PF06678419) is a potent, selective inhibitor of the Na+/citrate transporter NaCT (SLC13A5) that shows inhibition of citrate uptake in the HEKNaCT cells with IC50 of 0.44 uM.
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DC21489 PF-06651600 malonate
PF-06651600 malonate is a novel potent, selective JAK3 inhibitor with IC50 of 0.346 nM, displays >1,000-fold selectivity over JAK1 and JAK2.
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DC11722 PF-06459988
PF-06459988 (PF06459988, PF 6459988) is a potent, selective, irreversible EGFR mutants with IC50 of 13, 7, 21 and 90 nM for EGFR L858R-T790M, Del-T790M, L858R, and EGFR Del, respectively.
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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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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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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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