PERZINFOTEL


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


InChI Key	BDABGOLMYNHHTR-UHFFFAOYSA-N
Smiles	O=c1c2c(c1=O)N(CCP(=O)(O)O)CCCN2
InChI	InChI=1S/C9H13N2O5P/c12-8-6-7(9(8)13)11(3-1-2-10-6)4-5-17(14,15)16/h10H,1-5H2,(H2,14,15,16)

Mechanism of Action	Action	Reference
Glutamate [NMDA] receptor antagonist	ANTAGONIST	PubMed PubMed


Protein: Glutamate [NMDA] receptor Description: Glutamate receptor ionotropic, NMDA 2D Organism : Homo sapiens O15399 ENSG00000105464











Protein: Glutamate [NMDA] receptor Description: Glutamate receptor ionotropic, NMDA 3B Organism : Homo sapiens O60391 ENSG00000116032










Protein: Glutamate [NMDA] receptor Description: Glutamate receptor ionotropic, NMDA 1 Organism : Homo sapiens Q05586 ENSG00000176884












Protein: Glutamate [NMDA] receptor Description: Glutamate receptor ionotropic, NMDA 2A Organism : Homo sapiens Q12879 ENSG00000183454










Protein: Glutamate [NMDA] receptor Description: Glutamate receptor ionotropic, NMDA 2B Organism : Homo sapiens Q13224 ENSG00000273079











Protein: Glutamate [NMDA] receptor Description: Glutamate receptor ionotropic, NMDA 2C Organism : Homo sapiens Q14957 ENSG00000161509











Protein: Glutamate [NMDA] receptor Description: Glutamate receptor ionotropic, NMDA 3A Organism : Homo sapiens Q8TCU5 ENSG00000198785

Targets	EC50(nM)	IC50(nM)	Kd(nM)	Ki(nM)	Inhibition(%)
Ion channel Ligand-gated ion channel Ionotropic glutamate receptor NMDA receptor	-	8-30	-	-	-

Assay Description	Organism	Bioactivity
Tested in vitro for antagonistic activity at N-methyl-D-aspartate glutamate receptor by measuring displacement of [3H]TCP from crude synaptic membrane preparations obtained from rat brain	None	7.6 nM
Displacement of [3H]CPP from rat brain synaptic membrane N-methyl-D-aspartate glutamate receptor	Rattus norvegicus	30.0 nM
Displacement of [3H]CGP-39653 from rat brain NMDA receptor	Rattus norvegicus	23.0 nM
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	14.9 %
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate	Severe acute respiratory syndrome coronavirus 2	8.977 %
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	0.04 %	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	0.04 %

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