Compile Data Set for Download or QSAR
Report error Found 55 Enz. Inhib. hit(s) with all data for entry = 50012265
LigandPNGBDBM50556029(CHEMBL4759667)
Affinity DataIC50: 0.0250nMAssay Description:Inhibition of human platelets derived PDE5 using [3H]-cGMP as substrate incubated for 60 min by scintillation proximity assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
LigandPNGBDBM50088373(CHEBI:46295 | Vardenafil | cid_110634)
Affinity DataIC50: 0.0290nMAssay Description:Inhibition of human platelets derived PDE5 using [3H]-cGMP as substrate incubated for 60 min by scintillation proximity assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetNeutrophil elastase(Human)
Endotherm

Curated by ChEMBL
LigandPNGBDBM50120437(CHEMBL3617973)
Affinity DataIC50: 0.0650nMAssay Description:Inhibition of human neutrophil elastase using MeOSuc-AAPV-AMC as substrate measured after 60 mins by fluorescence methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
TargetBeta-secretase 1(Human)
Endotherm

Curated by ChEMBL
LigandPNGBDBM312923(US9605006, 22 | 5-But-2-ynyloxy-pyrazine-2-carboxy...)
Affinity DataIC50: 0.200nMAssay Description:Inhibition of BACE1 in HEK293 cells harboring APP assessed as reduction in amyloidbeta 40 level measured after 18 to 20 hrs by AlphaLISA AssayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
TargetNeutrophil elastase(Human)
Endotherm

Curated by ChEMBL
LigandPNGBDBM50556037(CHEMBL4744163)
Affinity DataIC50: 0.25nMAssay Description:Inhibition of human neutrophil elastase using MeOSuc-AAPV-AMC as substrate measured after 60 mins by fluorescence methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
TargetBeta-secretase 1(Human)
Endotherm

Curated by ChEMBL
LigandPNGBDBM50556043(CHEMBL4740873)
Affinity DataIC50: 0.590nMAssay Description:Inhibition of BACE1 in HEK293 cells harboring APP assessed as reduction in amyloidbeta 40 level measured after 18 to 20 hrs by AlphaLISA AssayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
TargetBeta-secretase 1(Human)
Endotherm

Curated by ChEMBL
LigandPNGBDBM50556042(CHEMBL4740455)
Affinity DataIC50: 0.990nMAssay Description:Inhibition of BACE1 in HEK293 cells harboring APP assessed as reduction in amyloidbeta 40 level measured after 18 to 20 hrs by AlphaLISA AssayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
Endotherm

Curated by ChEMBL
LigandPNGBDBM50556031(CHEMBL4782243)
Affinity DataIC50: 1.80nMAssay Description:Inhibition of wild type ESR1 (unknown origin) by transactivation assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
Endotherm

Curated by ChEMBL
LigandPNGBDBM50556030(CHEMBL4760678)
Affinity DataIC50: 2nMAssay Description:Inhibition of wild type ESR1 (unknown origin) by transactivation assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
LigandPNGBDBM50556032(CHEMBL4748292)
Affinity DataIC50: 2nMAssay Description:Inhibition of GST-tagged recombinant human CDK1/GST-tagged human cyclin B expressed in Sf-9 cells incubated for 10 mins by scintillation counting met...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
TargetBeta-secretase 1(Human)
Endotherm

Curated by ChEMBL
LigandPNGBDBM50556040(CHEMBL4796231)
Affinity DataIC50: 2nMAssay Description:Inhibition of BACE1 in HEK293 cells harboring APP assessed as reduction in amyloidbeta 40 level measured after 18 to 20 hrs by AlphaLISA AssayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
LigandPNGBDBM50556032(CHEMBL4748292)
Affinity DataIC50: 3nMAssay Description:Inhibition of GST-tagged recombinant human CDK2/GST-tagged human cyclin E expressed in Sf-9 cells incubated for 10 mins by scintillation counting met...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
TargetNuclear receptor ROR-gamma(Human)
Endotherm

Curated by ChEMBL
LigandPNGBDBM50461084(CHEMBL4225088)
Affinity DataIC50: 3.20nMAssay Description:Inverse agonist activity at RORgammat in human CD4-positive T cells assessed as reduction in Th17 level incubated for 5 days by MSD electrochemilumin...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
TargetCyclin-T1/Cyclin-dependent kinase 9(Human)
Endotherm

Curated by ChEMBL
LigandPNGBDBM50556034(CHEMBL4762845)
Affinity DataIC50: 4nMAssay Description:Inhibition of recombinant full length His-tagged human CDK9/cyclin T1 expressed in baculovirus expression system using biotinylated peptide biotin-Tt...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
LigandPNGBDBM50553480(CHEMBL4741442)
Affinity DataIC50: 4nMAssay Description:Inhibition of GST-tagged recombinant human CDK2/GST-tagged human cyclin E expressed in Sf-9 cells incubated for 10 mins by scintillation counting met...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetCyclin-T1/Cyclin-dependent kinase 9(Human)
Endotherm

Curated by ChEMBL
LigandPNGBDBM50468265(CHEMBL4282338)
Affinity DataIC50: 5nMAssay Description:Inhibition of CDK9/Cyclin T1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
LigandPNGBDBM50468265(CHEMBL4282338)
Affinity DataIC50: 7nMAssay Description:Inhibition of GST-tagged recombinant human CDK1/GST-tagged human cyclin B expressed in Sf-9 cells incubated for 10 mins by scintillation counting met...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
LigandPNGBDBM6145(US8802686, 2 | US8802686, C2)
Affinity DataIC50: 8nMAssay Description:Inhibition of GST-tagged recombinant human CDK2/GST-tagged human cyclin E expressed in Sf-9 cells incubated for 10 mins by scintillation counting met...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
TargetDipeptidyl peptidase 4(Human)
Endotherm

Curated by ChEMBL
LigandPNGBDBM50556035(CHEMBL4746458)
Affinity DataIC50: 8.80nMAssay Description:Inhibition of human DPP4 expressed in baculovirus expression system using Gly-Pro-AMC as substrate by fluorometric assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
LigandPNGBDBM50468265(CHEMBL4282338)
Affinity DataIC50: 9nMAssay Description:Inhibition of GST-tagged recombinant human CDK2/GST-tagged human cyclin E expressed in Sf-9 cells incubated for 10 mins by scintillation counting met...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
LigandPNGBDBM6145(US8802686, 2 | US8802686, C2)
Affinity DataIC50: 9nMAssay Description:Inhibition of GST-tagged recombinant human CDK1/GST-tagged human cyclin B expressed in Sf-9 cells incubated for 10 mins by scintillation counting met...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
LigandPNGBDBM50468265(CHEMBL4282338)
Affinity DataIC50: 11nMAssay Description:Inhibition of CDK4/Cyclin D1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
TargetCyclin-T1/Cyclin-dependent kinase 9(Human)
Endotherm

Curated by ChEMBL
LigandPNGBDBM50553488(CHEMBL4743691)
Affinity DataIC50: 11nMAssay Description:Inhibition of recombinant full length His-tagged human CDK9/cyclin T1 expressed in baculovirus expression system using biotinylated peptide biotin-Tt...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
TargetCyclin-T1/Cyclin-dependent kinase 9(Human)
Endotherm

Curated by ChEMBL
LigandPNGBDBM50528818(CHEMBL4439321)
Affinity DataIC50: 13nMAssay Description:Inhibition of recombinant full length His-tagged human CDK9/cyclin T1 expressed in baculovirus expression system using biotinylated peptide biotin-Tt...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
TargetDipeptidyl peptidase 4(Human)
Endotherm

Curated by ChEMBL
LigandPNGBDBM50556036(CHEMBL4776573)
Affinity DataIC50: 18nMAssay Description:Inhibition of human DPP4 expressed in baculovirus expression system using Gly-Pro-AMC as substrate by fluorometric assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
TargetCyclin-T1/Cyclin-dependent kinase 9(Human)
Endotherm

Curated by ChEMBL
LigandPNGBDBM50553489(CHEMBL4742789)
Affinity DataIC50: 24nMAssay Description:Inhibition of recombinant full length His-tagged human CDK9/cyclin T1 expressed in baculovirus expression system using biotinylated peptide biotin-Tt...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
LigandPNGBDBM50556039(CHEMBL4797263)
Affinity DataIC50: 27nMAssay Description:Inhibition of CYP24A1 (unknown origin) expressed in Chinese hamster V79 cells using [3H-1beta]-1alpha,25(OH)2D3 as substrate preincubated for 30 mins...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
TargetBeta-secretase 1(Human)
Endotherm

Curated by ChEMBL
LigandPNGBDBM50556041(CHEMBL4779761)
Affinity DataIC50: 28nMAssay Description:Inhibition of BACE1 in HEK293 cells harboring APP assessed as reduction in amyloidbeta 40 level measured after 18 to 20 hrs by AlphaLISA AssayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
LigandPNGBDBM50556038(CHEMBL389014)
Affinity DataIC50: 28nMAssay Description:Inhibition of human CYP24A1 expressed in Chinese hamster V79 cells using [3H-1beta]-1alpha,25(OH)2D3 as substrate preincubated for 10 mins followed b...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
LigandPNGBDBM50556038(CHEMBL389014)
Affinity DataIC50: 28nMAssay Description:Inhibition of human CYP24A1 expressed in Chinese hamster V79 cells using [3H-1beta]-1alpha,25(OH)2D3 as substrate preincubated for 10 mins followed b...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
LigandPNGBDBM50158486((1R,3S,5Z)-5-{2-[(1R,3aS,4E,7aR)-1-[(2R)-4-(benzen...)
Affinity DataIC50: 28nMAssay Description:Inhibition of human CYP24A1 expressed in Chinese hamster V79 cells using [3H-1beta]-1alpha,25(OH)2D3 as substrate preincubated for 10 mins followed b...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
LigandPNGBDBM50556032(CHEMBL4748292)
Affinity DataIC50: 32nMAssay Description:Inhibition of GST-tagged recombinant human VEGFR2 expressed in Sf-9 cells incubated for 10 mins by scintillation counting methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
TargetBromodomain-containing protein 4(Human)
Endotherm

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataIC50: 33nMAssay Description:Displacement of tetra-acetylated Histone H4 peptide from BRD4 (unknown origin) incubated for 1 hr by FRET analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
TargetBromodomain-containing protein 4(Human)
Endotherm

Curated by ChEMBL
LigandPNGBDBM205429( (R)-JQ1 (3) | US9320741, (R)-JQ1 | US10407441, Co...)
Affinity DataIC50: 33nMAssay Description:Inhibition of human His-tagged BRD4 bromodomain2 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells using H4K5acK8acK12acK16ac as substrate prei...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
LigandPNGBDBM50553480(CHEMBL4741442)
Affinity DataIC50: 34nMAssay Description:Inhibition of GST-tagged recombinant human VEGFR2 expressed in Sf-9 cells incubated for 10 mins by scintillation counting methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
TargetDipeptidyl peptidase 4(Human)
Endotherm

Curated by ChEMBL
LigandPNGBDBM185581(US9156848, 2)
Affinity DataIC50: 34nMAssay Description:Inhibition of human DPP4 expressed in baculovirus expression system using Gly-Pro-AMC as substrate by fluorometric assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
TargetCyclin-T1/Cyclin-dependent kinase 9(Human)
Endotherm

Curated by ChEMBL
LigandPNGBDBM180805(US9133171, 15 | US9133171, 16 | US9133171, 10)
Affinity DataIC50: 37nMAssay Description:Inhibition of recombinant full length His-tagged human CDK9/cyclin T1 expressed in baculovirus expression system using biotinylated peptide biotin-Tt...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
TargetDipeptidyl peptidase 4(Human)
Endotherm

Curated by ChEMBL
LigandPNGBDBM185582(US9156848, 3)
Affinity DataIC50: 37nMAssay Description:Inhibition of human DPP4 expressed in baculovirus expression system using Gly-Pro-AMC as substrate by fluorometric assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
LigandPNGBDBM50553480(CHEMBL4741442)
Affinity DataIC50: 50nMAssay Description:Inhibition of GST-tagged recombinant human CDK1/GST-tagged human cyclin B expressed in Sf-9 cells incubated for 10 mins by scintillation counting met...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
TargetBromodomain-containing protein 4(Human)
Endotherm

Curated by ChEMBL
LigandPNGBDBM205429( (R)-JQ1 (3) | US9320741, (R)-JQ1 | US10407441, Co...)
Affinity DataIC50: 77nMAssay Description:Inhibition of human His-tagged BRD4 bromodomain1 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells using H4K5acK8acK12acK16ac as substrate prei...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
TargetCyclin-T1/Cyclin-dependent kinase 9(Human)
Endotherm

Curated by ChEMBL
LigandPNGBDBM50556033(CHEMBL4793497)
Affinity DataIC50: 104nMAssay Description:Inhibition of recombinant full length His-tagged human CDK9/cyclin T1 expressed in baculovirus expression system using biotinylated peptide biotin-Tt...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
LigandPNGBDBM50468265(CHEMBL4282338)
Affinity DataIC50: 163nMAssay Description:Inhibition of GST-tagged recombinant human VEGFR2 expressed in Sf-9 cells incubated for 10 mins by scintillation counting methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
LigandPNGBDBM8610(24F2-1,25(OH)D3 | Ketoconazole (k) | KTZ | 1-[4-(4...)
Affinity DataIC50: 300nMAssay Description:Inhibition of human CYP24A1 expressed in Chinese hamster V79 cells using [3H-1beta]-1alpha,25(OH)2D3 as substrate preincubated for 10 mins followed b...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
LigandPNGBDBM6145(US8802686, 2 | US8802686, C2)
Affinity DataIC50: 477nMAssay Description:Inhibition of GST-tagged recombinant human VEGFR2 expressed in Sf-9 cells incubated for 10 mins by scintillation counting methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
TargetCarbonic anhydrase 2(Human)
Endotherm

Curated by ChEMBL
LigandPNGBDBM50553480(CHEMBL4741442)
Affinity DataIC50: 514nMAssay Description:Inhibition of human carbonic anhydrase 2 using 4-nitrophenyl acetate as substrate by spectrophotometryMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
LigandPNGBDBM50556038(CHEMBL389014)
Affinity DataIC50: 554nMAssay Description:Inhibition of CYP27B in human SW900 cells using 3H-(23,24)-25-(OH)D3 as substrate incubated for 5 hrs by HPLC methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
TargetSterol 26-hydroxylase, mitochondrial(Human)
Endotherm

Curated by ChEMBL
LigandPNGBDBM50556038(CHEMBL389014)
Affinity DataIC50: 1.00E+3nMAssay Description:Inhibition of CYP27A1 (unknown origin) expressed in Chinese hamster V79 cells using 1alpha-(OH)D3 as substrate measured after 24 hrs by HPLC analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
LigandPNGBDBM50553488(CHEMBL4743691)
Affinity DataIC50: 1.08E+3nMAssay Description:Inhibition of recombinant GST-tagged human CDK2/GST-tagged cyclin E expressed in sf9 cells using biotinylated peptide biotin-Ttds-YISPLKSPYKISEG as s...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
LigandPNGBDBM50528818(CHEMBL4439321)
Affinity DataIC50: 1.10E+3nMAssay Description:Inhibition of recombinant GST-tagged human CDK2/GST-tagged cyclin E expressed in sf9 cells using biotinylated peptide biotin-Ttds-YISPLKSPYKISEG as s...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
LigandPNGBDBM50556034(CHEMBL4762845)
Affinity DataIC50: 2.92E+3nMAssay Description:Inhibition of recombinant GST-tagged human CDK2/GST-tagged cyclin E expressed in sf9 cells using biotinylated peptide biotin-Ttds-YISPLKSPYKISEG as s...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/26/2022
Entry Details Article
PubMed
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