GLAFENINE


Synonyms	Glafenin Glafenine Glaphenine Glycerylaminophenaquine NSC-757808 R 1707 R-1707
Status
Molecule Category	UNKNOWN
ATC	N02BG03
UNII	46HL4I09AH
EPA CompTox	DTXSID1048546


Active Pharmaceutical Ingredients Bioactive chemicals	Exact Similarity SubStructure	Threshold (%) >= 70


InChI Key	GWOFUCIGLDBNKM-UHFFFAOYSA-N
Smiles	O=C(OCC(O)CO)c1ccccc1Nc1ccnc2cc(Cl)ccc12
InChI	InChI=1S/C19H17ClN2O4/c20-12-5-6-14-17(7-8-21-18(14)9-12)22-16-4-2-1-3-15(16)19(25)26-11-13(24)10-23/h1-9,13,23-24H,10-11H2,(H,21,22)

Mechanism of Action	Action	Reference
Cyclooxygenase inhibitor	INHIBITOR	PubMed PubMed PubMed


Protein: Cyclooxygenase Description: Prostaglandin G/H synthase 1 Organism : Homo sapiens P23219 ENSG00000095303











Protein: Cyclooxygenase Description: Prostaglandin G/H synthase 2 Organism : Homo sapiens P35354 ENSG00000073756

Targets	EC50(nM)	IC50(nM)	Kd(nM)	Ki(nM)	Inhibition(%)
Enzyme Hydrolase	-	-	-	-	21
Transporter Electrochemical transporter SLC superfamily of solute carriers SLC21/SLCO family of organic anion transporting polypeptides	-	-	-	-	131
Transporter Primary active transporter ATP-binding cassette ABCB subfamily	-	22300	-	-	-

Assay Description	Organism	Bioactivity
Anti-inflammatory effect expressed as % inhibition at 50 mg/kg in acute carrageenan paw edema test in rats	Rattus norvegicus	36.0 %
Inhibition of human FAAH at 1 uM	Homo sapiens	21.07 %
Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM	Cricetulus griseus	188.49 %
Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM	Cricetulus griseus	130.73 %
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells at 10 uM after 48 hours by high content imaging	Homo sapiens	38.56 %
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate	Severe acute respiratory syndrome coronavirus 2	5.748 %
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging	Chlorocebus sabaeus	-0.13 %	Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging	Chlorocebus sabaeus	-0.13 %

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