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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