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TargetReplicase polyprotein 1ab(2019-nCoV)
Pfizer

WIPO
LigandPNGBDBM510018(WO2021205290, Example 27 | (3S)-3-({N-[(4-methoxy-...)
Affinity DataIC50: 0.0300nMAssay Description:Proteolytic activity of SARS-CoV-2 Coronavirus 3CL protease is measured using a continuous fluorescence resonance energy transfer assay. The SARS-CoV...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/13/2022
Entry Details
WIPO WO2021205290

TargetReplicase polyprotein 1ab(BtCoV)
Pfizer

WIPO
LigandPNGBDBM420298(WO2005113580-Ex-02 | PF-00835231 | PF-0835231 | cm...)
Affinity DataKi:  0.0300nMAssay Description:Proteolytic activity of SARS-CoV-2 Coronavirus 3CL protease is measured using a continuous fluorescence resonance energy transfer assay. The SARS-CoV...More data for this Ligand-Target Pair
Ligand InfoPurchaseSimilars
In Depth
Date in BDB:
1/13/2022
Entry Details
WIPO WO2021205298

TargetReplicase polyprotein 1ab(BtCoV)
Pfizer

WIPO
LigandPNGBDBM420298(WO2005113580-Ex-02 | PF-00835231 | PF-0835231 | cm...)
Affinity DataKi:  0.0300nMAssay Description:Proteolytic activity of SARS-CoV-2 Coronavirus 3CL protease is measured using a continuous fluorescence resonance energy transfer assay. The SARS-CoV...More data for this Ligand-Target Pair
Ligand InfoPurchaseSimilars
In Depth
Date in BDB:
1/13/2022
Entry Details
WIPO WO2021205298

LigandPNGBDBM50300970(7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)-3-(py...)
Affinity DataIC50: 0.0400nMAssay Description:Inhibition of PDE5More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/30/2010
Entry Details Article
PubMed
LigandPNGBDBM50300964(rac-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)-3...)
Affinity DataIC50: 0.0500nMAssay Description:Inhibition of PDE5More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/30/2010
Entry Details Article
PubMed
LigandPNGBDBM50300953(3-[(trans-4-hydroxycyclohexyl)amino]-7-(6-methoxyp...)
Affinity DataIC50: 0.0500nMAssay Description:Inhibition of PDE5More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/30/2010
Entry Details Article
PubMed
LigandPNGBDBM50300972(7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)-3-(py...)
Affinity DataIC50: 0.0600nMAssay Description:Inhibition of PDE5More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/30/2010
Entry Details Article
PubMed
LigandPNGBDBM50296256(7-(6-methoxypyridin-3-yl)-3-(2-morpholinoethylamin...)
Affinity DataIC50: 0.0700nMAssay Description:Inhibition of PDE5More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/26/2010
Entry Details Article
PubMed
LigandPNGBDBM50300983(7-(6-methoxypyridin-3-yl)-3-(2-(4-methylpiperazin-...)
Affinity DataIC50: 0.0700nMAssay Description:Inhibition of PDE5More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/30/2010
Entry Details Article
PubMed
LigandPNGBDBM50300976(2-(7-(6-methoxypyridin-3-yl)-2-oxo-1-(2-propoxyeth...)
Affinity DataIC50: 0.0700nMAssay Description:Inhibition of PDE5More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/30/2010
Entry Details Article
PubMed
LigandPNGBDBM50296256(7-(6-methoxypyridin-3-yl)-3-(2-morpholinoethylamin...)
Affinity DataIC50: 0.0700nMAssay Description:Inhibition of PDE5More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/30/2010
Entry Details Article
PubMed
LigandPNGBDBM50300977(7-(6-methoxypyridin-3-yl)-3-(2-oxo-2-(pyrrolidin-1...)
Affinity DataIC50: 0.0800nMAssay Description:Inhibition of PDE5More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/30/2010
Entry Details Article
PubMed
LigandPNGBDBM50300989((S)-3-(2-hydroxypropylamino)-7-(6-methoxypyridin-3...)
Affinity DataIC50: 0.0900nMAssay Description:Inhibition of PDE5More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/30/2010
Entry Details Article
PubMed
LigandPNGBDBM50300991((R)-3-(2-hydroxypropylamino)-7-(6-methoxypyridin-3...)
Affinity DataIC50: 0.100nMAssay Description:Inhibition of PDE5More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/30/2010
Entry Details Article
PubMed
TargetInterleukin-1 receptor-associated kinase 4(Human)
Pfizer

US Patent
LigandPNGBDBM319575(5-(((2S,3S,4S)-3-ethyl-4-fluoro-5-oxopyrrolidin-2-...)
Affinity DataIC50: 0.100nMAssay Description:This is an in vitro assay to measure IRAK4 enzymatic activity utilizing the DELFIA (Dissociation-Enhanced Lanthanide Fluorescent Immunoassay, Perkin-...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/15/2019
Entry Details
US Patent

TargetReplicase polyprotein 1ab(FCoV)
Pfizer

WIPO
LigandPNGBDBM420298(WO2005113580-Ex-02 | PF-00835231 | PF-0835231 | cm...)
Affinity DataKi:  0.100nMAssay Description:Proteolytic activity of SARS-CoV-2 Coronavirus 3CL protease is measured using a continuous fluorescence resonance energy transfer assay. The SARS-CoV...More data for this Ligand-Target Pair
Ligand InfoPurchaseSimilars
In Depth
Date in BDB:
1/13/2022
Entry Details
WIPO WO2021205298

LigandPNGBDBM50300962(3-(2-ethoxyethylamino)-7-(6-methoxypyridin-3-yl)-1...)
Affinity DataIC50: 0.110nMAssay Description:Inhibition of PDE5More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/30/2010
Entry Details Article
PubMed
LigandPNGBDBM50300978(3-(2-(4-hydroxypiperidin-1-yl)-2-oxoethylamino)-7-...)
Affinity DataIC50: 0.130nMAssay Description:Inhibition of PDE5More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/30/2010
Entry Details Article
PubMed
LigandPNGBDBM50300985(3-(2-(4-ethylpiperazin-1-yl)-2-oxoethylamino)-7-(6...)
Affinity DataIC50: 0.130nMAssay Description:Inhibition of PDE5More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/30/2010
Entry Details Article
PubMed
LigandPNGBDBM50300963(7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)-3-((t...)
Affinity DataIC50: 0.140nMAssay Description:Inhibition of PDE5More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/30/2010
Entry Details Article
PubMed
LigandPNGBDBM50300948((R)-3-(1-hydroxypropan-2-ylamino)-7-(6-methoxypyri...)
Affinity DataIC50: 0.140nMAssay Description:Inhibition of PDE5More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/30/2010
Entry Details Article
PubMed
LigandPNGBDBM50300980(7-(6-methoxypyridin-3-yl)-3-(2-morpholino-2-oxoeth...)
Affinity DataIC50: 0.150nMAssay Description:Inhibition of PDE5More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/30/2010
Entry Details Article
PubMed
TargetReplicase polyprotein 1ab(2019-nCoV)
Pfizer

WIPO
LigandPNGBDBM50645474(CHEMBL5592467)
Affinity DataKi:  0.170nMAssay Description:Inhibition of SARS-Cov-2 MPro assessed as inhibition constant by FRET assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM50300961(3-(2-ethoxyethylamino)-7-(6-methoxypyridin-3-yl)-1...)
Affinity DataIC50: 0.170nMAssay Description:Inhibition of PDE5More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/30/2010
Entry Details Article
PubMed
LigandPNGBDBM50308556(3-(4-(3-hydroxypropyl)piperazin-1-yl)-1-(2-propoxy...)
Affinity DataIC50: 0.180nMAssay Description:Inhibition of human platelet PDE5 assessed as reduction in conversion of [3H]cGMP to [3H]GMP after 2 hr by scintillation proximity assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/2/2010
Entry Details Article
PubMed
LigandPNGBDBM50308557(3-(4-(2-hydroxyethyl)piperazin-1-yl)-1-(2-propoxye...)
Affinity DataIC50: 0.200nMAssay Description:Inhibition of human platelet PDE5 assessed as reduction in conversion of [3H]cGMP to [3H]GMP after 2 hr by scintillation proximity assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/2/2010
Entry Details Article
PubMed
LigandPNGBDBM50308563(3-(4-(2-hydroxy-2-methylpropyl)piperazin-1-yl)-1-(...)
Affinity DataIC50: 0.210nMAssay Description:Inhibition of human platelet PDE5 assessed as reduction in conversion of [3H]cGMP to [3H]GMP after 2 hr by scintillation proximity assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/2/2010
Entry Details Article
PubMed
LigandPNGBDBM50308558(3-(4-ethylpiperazin-1-yl)-1-(2-propoxyethyl)-7-(6-...)
Affinity DataIC50: 0.220nMAssay Description:Inhibition of human platelet PDE5 assessed as reduction in conversion of [3H]cGMP to [3H]GMP after 2 hr by scintillation proximity assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/2/2010
Entry Details Article
PubMed
LigandPNGBDBM50308564((R)-3-(4-(2-hydroxypropyl)piperazin-1-yl)-1-(2-iso...)
Affinity DataIC50: 0.230nMAssay Description:Inhibition of human platelet PDE5 assessed as reduction in conversion of [3H]cGMP to [3H]GMP after 2 hr by scintillation proximity assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/2/2010
Entry Details Article
PubMed
LigandPNGBDBM50300950((S)-3-(1-hydroxypropan-2-ylamino)-7-(6-methoxypyri...)
Affinity DataIC50: 0.240nMAssay Description:Inhibition of PDE5More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/30/2010
Entry Details Article
PubMed
LigandPNGBDBM50300951((R)-3-(1-hydroxybutan-2-ylamino)-7-(6-methoxypyrid...)
Affinity DataIC50: 0.25nMAssay Description:Inhibition of PDE5More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/30/2010
Entry Details Article
PubMed
LigandPNGBDBM50300957(3-(2-aminoethylamino)-7-(6-methoxypyridin-3-yl)-1-...)
Affinity DataIC50: 0.25nMAssay Description:Inhibition of PDE5More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/30/2010
Entry Details Article
PubMed
LigandPNGBDBM50300957(3-(2-aminoethylamino)-7-(6-methoxypyridin-3-yl)-1-...)
Affinity DataIC50: 0.25nMAssay Description:Inhibition of human platelet PDE5 assessed as reduction in conversion of [3H]cGMP to [3H]GMP after 2 hr by scintillation proximity assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/2/2010
Entry Details Article
PubMed
LigandPNGBDBM50300987(3-(3-hydroxypropylamino)-7-(6-methoxypyridin-3-yl)...)
Affinity DataIC50: 0.260nMAssay Description:Inhibition of PDE5More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/30/2010
Entry Details Article
PubMed
TargetReplicase polyprotein 1ab(2019-nCoV)
Pfizer

WIPO
LigandPNGBDBM420298(WO2005113580-Ex-02 | PF-00835231 | PF-0835231 | cm...)
Affinity DataKi:  0.270nMAssay Description:The respective human coronavirus Mpro in assay buffer (20 mM Tris-HCl, pH 7.3, 100 mM NaCl, 1 mM EDTA, 5 mM TCEP) and 0.1% BSA was added to assay-rea...More data for this Ligand-Target Pair
Ligand InfoPurchaseSimilars
In Depth
Date in BDB:
11/5/2021
Entry Details

LigandPNGBDBM50300971(7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)-3-(py...)
Affinity DataIC50: 0.280nMAssay Description:Inhibition of PDE5More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/30/2010
Entry Details Article
PubMed
TargetTranslocator protein(Rat)
National Institute of Mental Health

Curated by ChEMBL
LigandPNGBDBM50335260(N,N-dihexyl-2-(1-methyl-2-phenyl-1H-indol-3-yl)-2-...)
Affinity DataKi:  0.299nMAssay Description:Displacement of [11C]PK11195 from TSPO in rat kidney mitochondrial membraneMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/4/2013
Entry Details Article
PubMed
LigandPNGBDBM50297794(2-(4-(cyclohexylmethyl)-6-(6-methoxypyridin-3-yl)-...)
Affinity DataIC50: 0.300nMAssay Description:Inhibition of PDE5More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/27/2010
Entry Details Article
PubMed
LigandPNGBDBM50308561((+/-)-3-(4-((2R,3R)-3-hydroxybutan-2-yl)piperazin-...)
Affinity DataIC50: 0.300nMAssay Description:Inhibition of human platelet PDE5 assessed as reduction in conversion of [3H]cGMP to [3H]GMP after 2 hr by scintillation proximity assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/2/2010
Entry Details Article
PubMed
LigandPNGBDBM50297796(4-(cyclohexylmethyl)-6-(2-methoxypyrimidin-5-yl)-2...)
Affinity DataIC50: 0.300nMAssay Description:Inhibition of PDE5More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/27/2010
Entry Details Article
PubMed
TargetInterleukin-1 receptor-associated kinase 4(Human)
Pfizer

US Patent
LigandPNGBDBM319574(4-(((2S,3S,4S)-3-ethyl-4-fluoro-5-oxopyrrolidin-2-...)
Affinity DataIC50: 0.300nMAssay Description:This is an in vitro assay to measure IRAK4 enzymatic activity utilizing the DELFIA (Dissociation-Enhanced Lanthanide Fluorescent Immunoassay, Perkin-...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/15/2019
Entry Details
US Patent

TargetNeprilysin(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50344193((S)-2-(1-((S)-1-carboxy-2-(5-phenyloxazol-2-yl)eth...)
Affinity DataIC50: 0.300nMAssay Description:Inhibition of neutral endopeptidaseMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/4/2011
Entry Details Article
PubMed
TargetTranslocator protein(Rat)
National Institute of Mental Health

Curated by ChEMBL
LigandPNGBDBM50335259(N,N-dibutyl-2-(1-methyl-2-phenyl-1H-indol-3-yl)-2-...)
Affinity DataKi:  0.300nMAssay Description:Displacement of [11C]PK11195 from TSPO in rat kidney mitochondrial membraneMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/4/2013
Entry Details Article
PubMed
TargetReplicase polyprotein 1ab(PEDV)
Pfizer

WIPO
LigandPNGBDBM420298(WO2005113580-Ex-02 | PF-00835231 | PF-0835231 | cm...)
Affinity DataKi:  0.300nMAssay Description:Proteolytic activity of SARS-CoV-2 Coronavirus 3CL protease is measured using a continuous fluorescence resonance energy transfer assay. The SARS-CoV...More data for this Ligand-Target Pair
Ligand InfoPurchaseSimilars
In Depth
Date in BDB:
1/13/2022
Entry Details
WIPO WO2021205298

TargetNeprilysin(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50344195((S)-2-(1-((S)-1-carboxy-2-(5-(4-chlorophenyl)oxazo...)
Affinity DataIC50: 0.300nMAssay Description:Inhibition of neutral endopeptidaseMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/4/2011
Entry Details Article
PubMed
LigandPNGBDBM50297795(4-(cyclohexylmethyl)-6-(6-methoxypyridin-3-yl)-2-(...)
Affinity DataIC50: 0.300nMAssay Description:Inhibition of PDE5More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/27/2010
Entry Details Article
PubMed
LigandPNGBDBM50308553((S)-3-(4-(2-hydroxypropyl)piperazin-1-yl)-1-(2-iso...)
Affinity DataIC50: 0.310nMAssay Description:Inhibition of human platelet PDE5 assessed as reduction in conversion of [3H]cGMP to [3H]GMP after 2 hr by scintillation proximity assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/2/2010
Entry Details Article
PubMed
LigandPNGBDBM50300982(7-(6-methoxypyridin-3-yl)-3-(2-(4-methylpiperazin-...)
Affinity DataIC50: 0.320nMAssay Description:Inhibition of PDE5More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/30/2010
Entry Details Article
PubMed
LigandPNGBDBM50300952(3-(trans-4-hydroxycyclohexylamino)-7-(6-methoxypyr...)
Affinity DataIC50: 0.320nMAssay Description:Inhibition of PDE5More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/30/2010
Entry Details Article
PubMed
LigandPNGBDBM50308562((+/-)-3-(4-((2S,3R)-3-hydroxybutan-2-yl)piperazin-...)
Affinity DataIC50: 0.330nMAssay Description:Inhibition of human platelet PDE5 assessed as reduction in conversion of [3H]cGMP to [3H]GMP after 2 hr by scintillation proximity assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/2/2010
Entry Details Article
PubMed
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