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Table 2 Screening hits from the Pharmakon 1600 library

From: BET bromodomain inhibitors and agonists of the beta-2 adrenergic receptor identified in screens for compounds that inhibit DUX4 expression in FSHD muscle cells

Drug MBD3L2 EC50 (nanomolar) MYH2 EC50 (nanomolar) Mechanism
Clenbuterol hydrochloride < 60 > 5000 Beta-2 adrenergic agonist
Tulobuterol hydrochloride < 60 > 5000 Beta-2 adrenergic agonist
Albuterol < 60 < 60 Beta-2 adrenergic agonist
Fenoterol hydrobromide < 60 < 60e Beta-2 adrenergic agonist
Fluticasone < 60 < 60d Glucocorticoid
Nylidrin (Buphenine isoxsuprine) < 60 < 60c Beta-2 adrenergic agonist
Sirolimus < 60 < 60 Immunosuppressant
Terbutaline hemisulfate < 60 < 60c Beta-2 adrenergic agonist
Vinblastine < 60b < 60 Antineoplastic, spindle poison
Dequalinium 70 5000 Anti-infective, antineoplastic
Bisoctrizole 100c > 5000 Sunscreen
Isoetharine 100 5000 Beta-1 and beta-2 adrenergic agonist
Penicillamine 180c > 5000 Chelating agent
Benzethonium chloride 190 400 Anti-infective
Cetylpyridinium chloride 200 300 Anti-infective
Epinephrine bitartrate 200 4000 Alpha and beta-adrenergic agonist
Phenylephrine 200 4000 Alpha-1 adrenergic agonist
Piromidic acid < 500a > 5000 Antibacterial
Acenocoumarol 500b > 5000 Anticoagulant
Atorvastatin 500c > 5000 HmG-CoA reductase inhibitor
Cresopirine 500 > 5000 Anti-inflammatory, fever reducer
Dicoumarol 500b > 5000 Anticoagulant
Thiostrepton 500 700f Antibacterial
Thimerosal 500   Anti-infective, organomercury
Ethylnorepinephrine 600 5000 Alpha and beta adrenergic agonist
Fluvoxamine 1000 4000 SSRI, antidepressant
Clozapine 1000 2000 Antipsychotic
Adrenalone hydrochloride 1000 1500 Alpha-adrenergic agonist
Butamben 1000f 1000 Local anesthetic
Thonzonium 1000 1000 Mucolytic antibacterial
Mebendazole 1000f   Anthelmintic
Puromycin 1000f   Antibacterial, antineoplastic
Colforsin 1500d > 5000 Adenylyl cyclase activator
Dimercaprol 1500 3000 Chelating agent
Benzalkonium 1500   Anti-infective
Norepinephrine 1600 4000 Alpha and beta adrenergic agonist
Polymyxin B 1700 3500 Antibacterial
Oxedrine (synephrine) 2000 5000 Alpha and beta adrenergic agonist and antagonist
Nonoxynol-9 2000   Spermicide
Papaverine 2500 10,000 Vasodilator
Pentamidine 3000   Antiprotozoal
Triamcinolone 3000   Corticosteroid
Dichlorephen 3500   Anthelmintic
Ebselen 4000   Antioxidant, anti-inflammatory
Minocycline 5000 10,000 Antibacterial
Inosine 5000 > 5000 Nucleoside
Sulbentine 5000 > 5000 Antifungal
Artesunate 5000   Anti-malarial
Broxaldine 5000   Antifungal
Broxyquinoline 5000   Anti-infectant
Meclocycline 5000   Antibacterial
Sennoside A 5000   Cathartic/laxative
  1. aMaximum 50% inhibition
  2. bMaximum 60% inhibition
  3. cMaximum 65% inhibition
  4. dMaximum 70% inhibition
  5. eMaximum 85% inhibition
  6. fToxicity