DC2086 |
PF-670462
Featured
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PF 670462 is a selective casein kinase, CK1ε and CK1δ inhibitor which also shows potency against 42 other kinases. |
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DC20027 |
PF 750
Featured
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PF 750 is a selective and covalent fatty acid amide hydrolase (FAAH) inhibitor, with IC50s varied from 16.2-595 nM in different pre-incubation times. Covalently modifies the enzyme’s active site serine nucleophile. |
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DC21500 |
PF-00610355 |
PF-00610355 (PF 610355) is a potent, selective, and long-acting β2-adrenoreceptor agonist with EC50 of 0.26 nM. |
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DC21495 |
PF-02413873 |
PF-02413873 (PF-2413873) is a potent, selective, fully competitive, and orally active progesterone receptor (PR) antagonist with Ki of 9.7 nM. |
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DC23574 |
PF-02575799 |
PF-02575799 is a highly potent microsomal triglyceride transfer protein (MTP) inhibitor with IC50 of 0.77 nM. |
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DC21470 |
PF-03049423 |
PF-03049423 is a potent, selective, orally active, and brain penetrant inhibitor of PDE5 with IC50 of 0.2 nM. |
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DC8382 |
PF-03084014 (Nirogacestat)
Featured
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PF-03084014 (PF-3084014) is a selective gamma-secretase inhibitor with IC50 of 6.2 nM in a cell-free assay. Phase 2. |
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DC21496 |
PF-03382792 |
PF-03382792 (PF-3382792) is a clinical compound under phase 1 investigation for an unknown indication.. |
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DC23622 |
PF-03463275 |
PF-03463275 (PF 3463275) ia an orally bioavailable, centrally penetrant, potent, reversible, selective, and competitive inhibitor of the human GlyT1 transporter with Ki of 13 nM. |
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DC23422 |
PF-03654746 |
PF-03654746 (PF 3654746) is a potent, selective, orally bioactive antagonist of H3 receptor with Ki of 2.3 nM. |
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DC23448 |
PF-03654764 |
PF-03654764 (PF 3654764) is a potent, selective, orally bioactive antagonist of H3 receptor with Ki of 1.4 nM. |
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DC21483 |
PF03715455
Featured
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PF-03715455 is a potent inhaled p38 MAPK inhibitor. PF-03715455 shows some selectivity for p38α over p38β with respective IC50 values of 0.88 and 23 nM. PF-03715455 potently inhibits LPS-induced TNFα production in human whole blood (IC50=1.7 nM). PF-03715455 has potential for the treatment of COPD (chronic obstructive pulmonary disease)[1][2].PF-03715455 is a moderate inhibitor of CYP1A2, CYP2C19, and CYP2D6 and a potent inhibitor of CYP’s 2C9 and CYP3A4[2].PF-03715455 treatment shows that the Vss and T1/2 are 0.19 L/kg, 1 hour, respectively[2]. Animal Model: Male CD Sprague Dawley rats (300-450 g)[2] Dosage: 1 mg/kg Administration: I.v. (Pharmacokinetic Analysis) Result: The Vss, and T1/2 were 0.19 L/kg, 1 hour, respectively. |
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DC9367 |
PF-03814735 |
PF-03814735 is a novel, potent, orally bioavailable, reversible small-molecule Aurora kinase inhibitor with IC50 of 0.8, 5, 10 and 22 nM for Aurora A, Aurora B, Flt 1 and FAk, respectively. |
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DC23708 |
PF-03882845 |
PF-03882845 is highly potent, selective, nonsteroidal, orally bioavailable Mineralocorticoid receptor antagonist with IC50 of 4.5 nM. |
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DC21498 |
PF-04191834 |
PF-04191834 (PF-4191834) is a potent, non‐iron chelating, non‐redox, selective and competitive inhibitor of 5-lipoxygenase (5‐LO) with Ki of 10 nM. |
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DC24071 |
PF-04217903 methanesulfonate
Featured
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PF-04217903 is a potent, selective, ATP-competitive c-Met kinase inhibitor with Ki of 4.8 nM, inhibits HGF-stimulated tyrosine phosphorylation of wild type c-Met with IC50 of 7.3 nM in cell-based assays. |
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DC21479 |
PF-04308515 |
PF-04308515 (PF 4308515) is a potent glucocorticoid receptor (GR) agonist with anti-inflammatory activity.. |
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DC12550 |
PF-04449613 |
PF-04449613 (PF04449613) is a potent and selective inhibitor of PDE9.. |
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DC26092 |
PF-04455242 hydrochloride |
PF-04455242 is a potent, selective κ-opioid receptor (KOR) antagonist with Ki of 3 nM/21 nM/22 nM for hKOR/rKOR/mKOR, respectively. |
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DC23423 |
PF-04455242 |
PF-04455242 is a potent, selective κ-opioid receptor (KOR) antagonist with Ki of 3 nM/21 nM/22 nM for hKOR/rKOR/mKOR, respectively. |
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DC9442 |
PF-04457845
Featured
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PF-04457845 is a potent and exquisitely selective inhibitor of FAAH, with an IC50 of 7.2 nM, and both analgesic and antiinflammatory effects in animal studies comparable to naproxen. |
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DC21499 |
PF-04531083 |
PF-04531083 (PF 4531083) is a potent and selective, orally available sodium channel Nav1.8 blocker for treatment of pain. . |
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DC22408 |
PF-04634817 |
PF-04634817 is a potent, orally bioavailble CCR2 and CCR5 chemokine receptor antagonist for the treatment of diabetic nephropathies and diabetic macular oedema. . |
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DC22409 |
PF-04634817 succinate |
PF-04634817 is a potent, orally bioavailble CCR2 and CCR5 chemokine receptor antagonist, for the treatment of diabetic nephropathies and diabetic macular oedema. . |
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DC23682 |
PF-04677490 |
PF-04677490 is a potent, selective PDE1 inhibitor with IC50 of 21 nM for PDE1B. |
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DC23631 |
PF-04701475 |
PF-04701475 is a nove positive allosteric modulator of AMPA receptor, a prototype used to explore AMPAR-mediated pharmacology in vivo.. |
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DC23600 |
PF-04856264
Featured
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PF-04856264 is a potent, selective Nav1.7 blocker with IC50 of 28 nM, dispalys >1,000-fold selectivity over Nav1.5. |
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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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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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