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Found 1397 with Last Name = 'artis' and Initial = 'dr'
TargetCoagulation factor VII(Homo sapiens (Human))
Genentech

LigandPNGBDBM14714((2R)-N-[(3-aminobenzene)sulfonyl]-2-[(4-carbamimid...)
Affinity DataKi:  0.350nM ΔG°:  -53.4kJ/molepH: 7.8 T: 2°CAssay Description:The enzyme reactions were initiated by the addition of substrate, and the color developed from the release of p-nitroanilide from each chromogenic su...More data for this Ligand-Target Pair
TargetVitamin K-dependent protein C(Homo sapiens (Human))
Genentech

LigandPNGBDBM14714((2R)-N-[(3-aminobenzene)sulfonyl]-2-[(4-carbamimid...)
Affinity DataKi:  87nM ΔG°:  -39.9kJ/molepH: 7.8 T: 2°CAssay Description:The enzyme reactions were initiated by the addition of substrate, and the color developed from the release of p-nitroanilide from each chromogenic su...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPlasma kallikrein(Homo sapiens (Human))
Genentech

LigandPNGBDBM14714((2R)-N-[(3-aminobenzene)sulfonyl]-2-[(4-carbamimid...)
Affinity DataKi:  114nM ΔG°:  -39.2kJ/molepH: 7.8 T: 2°CAssay Description:The enzyme reactions were initiated by the addition of substrate, and the color developed from the release of p-nitroanilide from each chromogenic su...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPlasminogen(Homo sapiens (Human))
Genentech

LigandPNGBDBM14714((2R)-N-[(3-aminobenzene)sulfonyl]-2-[(4-carbamimid...)
Affinity DataKi:  1.20E+3nM ΔG°:  -33.5kJ/molepH: 7.8 T: 2°CAssay Description:The enzyme reactions were initiated by the addition of substrate, and the color developed from the release of p-nitroanilide from each chromogenic su...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetUrokinase-type plasminogen activator(Homo sapiens (Human))
Genentech

LigandPNGBDBM14714((2R)-N-[(3-aminobenzene)sulfonyl]-2-[(4-carbamimid...)
Affinity DataKi: >3.40E+3nM ΔG°: >-30.9kJ/molepH: 7.8 T: 2°CAssay Description:The enzyme reactions were initiated by the addition of substrate, and the color developed from the release of p-nitroanilide from each chromogenic su...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCoagulation factor X(Homo sapiens (Human))
Genentech

LigandPNGBDBM14714((2R)-N-[(3-aminobenzene)sulfonyl]-2-[(4-carbamimid...)
Affinity DataKi: >3.50E+3nM ΔG°: >-30.8kJ/molepH: 7.8 T: 2°CAssay Description:The enzyme reactions were initiated by the addition of substrate, and the color developed from the release of p-nitroanilide from each chromogenic su...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProthrombin(Homo sapiens (Human))
Genentech

LigandPNGBDBM14714((2R)-N-[(3-aminobenzene)sulfonyl]-2-[(4-carbamimid...)
Affinity DataKi:  3.60E+3nM ΔG°:  -30.8kJ/molepH: 7.8 T: 2°CAssay Description:The enzyme reactions were initiated by the addition of substrate, and the color developed from the release of p-nitroanilide from each chromogenic su...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTissue-type plasminogen activator(Homo sapiens (Human))
Genentech

LigandPNGBDBM14714((2R)-N-[(3-aminobenzene)sulfonyl]-2-[(4-carbamimid...)
Affinity DataKi: >3.90E+3nM ΔG°: >-30.6kJ/molepH: 7.8 T: 2°CAssay Description:The enzyme reactions were initiated by the addition of substrate, and the color developed from the release of p-nitroanilide from each chromogenic su...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine protease 1(Bos taurus (bovine))
Genentech

LigandPNGBDBM14714((2R)-N-[(3-aminobenzene)sulfonyl]-2-[(4-carbamimid...)
Affinity DataKi:  4.00E+3nM ΔG°:  -30.5kJ/molepH: 7.8 T: 2°CAssay Description:The enzyme reactions were initiated by the addition of substrate, and the color developed from the release of p-nitroanilide from each chromogenic su...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14775(3-(cyclopentyloxy)-N-(3,5-dichloropyridin-4-yl)-4-...)
Affinity DataIC50:  0.0210nMAssay Description:Phosphodiesterase activities were assayed in the presence of inhibitor compounds. Measurement takes advantage of the selective binding of 5-AMP or 5-...More data for this Ligand-Target Pair
LigandPNGBDBM14775(3-(cyclopentyloxy)-N-(3,5-dichloropyridin-4-yl)-4-...)
Affinity DataIC50:  0.0410nMAssay Description:Phosphodiesterase activities were assayed in the presence of inhibitor compounds. Measurement takes advantage of the selective binding of 5-AMP or 5-...More data for this Ligand-Target Pair
TargetIntegrin alpha-4/beta-1(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50060228((5S,8R,13R,15aS)-8-{[(2R,3S)-1-Acetyl-3-(4-hydroxy...)
Affinity DataIC50:  0.5nMAssay Description:Inhibition of purified alpha-4 beta-1 binding to VCAM-1 was determined in an ELISA assay.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  0.680nMAssay Description:Phosphodiesterase activities were assayed in the presence of inhibitor compounds. Measurement takes advantage of the selective binding of 5-AMP or 5-...More data for this Ligand-Target Pair
LigandPNGBDBM14774(3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl...)
Affinity DataIC50:  0.840nMAssay Description:Phosphodiesterase activities were assayed in the presence of inhibitor compounds. Measurement takes advantage of the selective binding of 5-AMP or 5-...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 8(Homo sapiens (Human))
Elan Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50352620(CHEMBL1822151)
Affinity DataIC50:  1nMAssay Description:Inhibition of recombinant JNK1 using ser73 of c-jun as substrate preincubated for 15 mins measured after 60 mins by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 8(Homo sapiens (Human))
Elan Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50352624(CHEMBL1822305 | US9796706, Compound 139)
Affinity DataIC50:  1nMAssay Description:Inhibition of recombinant JNK1 using ser73 of c-jun as substrate preincubated for 15 mins measured after 60 mins by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 8(Homo sapiens (Human))
Elan Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50352621(CHEMBL1822152)
Affinity DataIC50:  1nMAssay Description:Inhibition of recombinant JNK1 using ser73 of c-jun as substrate preincubated for 15 mins measured after 60 mins by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-specific 3',5'-cyclic phosphodiesterase [531-875](Homo sapiens (Human))
Plexxikon

LigandPNGBDBM14776(2-{2-ethoxy-5-[(4-ethylpiperazine-1-)sulfonyl]phen...)
Affinity DataIC50:  1nMAssay Description:Phosphodiesterase activities were assayed in the presence of inhibitor compounds. Measurement takes advantage of the selective binding of 5-AMP or 5-...More data for this Ligand-Target Pair
TargetIntegrin alpha-4/beta-1(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50060185((6S,9R,14R,16aS)-9-[(S)-2-Acetylamino-3-(4-hydroxy...)
Affinity DataIC50:  1nMAssay Description:Inhibition of purified alpha-4 beta-1 binding to VCAM-1 was determined in an ELISA assay.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin D(Homo sapiens (Human))
Elan Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50438363(CHEMBL2408751)
Affinity DataIC50:  1nMAssay Description:Inhibition of cathepsin-D (unknown origin) using C-terminal biotinylated peptide substrate treated 30 mins before addition of peptide substrate measu...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-specific 3',5'-cyclic phosphodiesterase [531-875](Homo sapiens (Human))
Plexxikon

LigandPNGBDBM14777((2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,1...)
Affinity DataIC50:  1.20nMAssay Description:Phosphodiesterase activities were assayed in the presence of inhibitor compounds. Measurement takes advantage of the selective binding of 5-AMP or 5-...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 10(Homo sapiens (Human))
Elan Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM16016(CHEMBL437747 | N-cyclohexyl-4-[4-(3,4-dichlorophen...)
Affinity DataIC50:  1.60nMAssay Description:Inhibition of recombinant JNK3 after 60 mins by TR-FRET assayMore data for this Ligand-Target Pair
TargetBeta-secretase 1(Homo sapiens (Human))
Imago Pharmaceuticals

US Patent
LigandPNGBDBM258304(US9493485, 9-145)
Affinity DataIC50:  1.90nMpH: 4.5 T: 2°CAssay Description:Compounds are also assessed for BACE1 and Cathepsin D activity using an FP Assay. Compounds to be assessed (e.g. compounds as described in the above ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetBeta-secretase 1(Homo sapiens (Human))
Imago Pharmaceuticals

US Patent
LigandPNGBDBM258329(US9493485, 13-182)
Affinity DataIC50:  2nMpH: 7.0Assay Description:BACE1 activity can be assessed in an AlphaScreenŽ assay. Compounds to be assessed (e.g. compounds as described in the above examples) are serially di...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetMitogen-activated protein kinase 8(Homo sapiens (Human))
Elan Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50352618(CHEMBL1822149)
Affinity DataIC50:  2nMAssay Description:Inhibition of recombinant JNK1 using ser73 of c-jun as substrate preincubated for 15 mins measured after 60 mins by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetIntegrin alpha-4/beta-1(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50060226((5S,8R,13R,15aS)-8-[(S)-2-Acetylamino-3-(4-hydroxy...)
Affinity DataIC50:  2nMAssay Description:Inhibition of purified alpha-4 beta-1 binding to VCAM-1 was determined in an ELISA assay.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 8(Homo sapiens (Human))
Elan Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50352615(CHEMBL1822146)
Affinity DataIC50:  2nMAssay Description:Inhibition of recombinant JNK1 using ser73 of c-jun as substrate preincubated for 15 mins measured after 60 mins by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 10(Homo sapiens (Human))
Elan Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50352621(CHEMBL1822152)
Affinity DataIC50:  2nMAssay Description:Inhibition of recombinant JNK3 using ser73 of c-jun as substrate preincubated for 15 mins measured after 60 mins by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 8(Homo sapiens (Human))
Elan Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50352628(CHEMBL1822309 | US9796706, Compound 136)
Affinity DataIC50:  2nMAssay Description:Inhibition of recombinant JNK1 using ser73 of c-jun as substrate preincubated for 15 mins measured after 60 mins by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin D(Homo sapiens (Human))
Elan Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50438362(CHEMBL2408752)
Affinity DataIC50:  2nMAssay Description:Inhibition of cathepsin-D (unknown origin) using C-terminal biotinylated peptide substrate treated 30 mins before addition of peptide substrate measu...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 10(Homo sapiens (Human))
Elan Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50352620(CHEMBL1822151)
Affinity DataIC50:  2nMAssay Description:Inhibition of recombinant JNK3 using ser73 of c-jun as substrate preincubated for 15 mins measured after 60 mins by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-specific 3',5'-cyclic phosphodiesterase [531-875](Homo sapiens (Human))
Plexxikon

LigandPNGBDBM14390(5-[2-ethoxy-5-(4-methyl-1-piperazinylsulfonyl)phen...)
Affinity DataIC50:  2.20nMAssay Description:Phosphodiesterase activities were assayed in the presence of inhibitor compounds. Measurement takes advantage of the selective binding of 5-AMP or 5-...More data for this Ligand-Target Pair
TargetIntegrin alpha-4/beta-1(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50060183((5S,8R,13R,15aS)-8-[(S)-2-Acetylamino-3-(4-hydroxy...)
Affinity DataIC50:  3nMAssay Description:Inhibition of purified alpha-4 beta-1 binding to VCAM-1 was determined in an ELISA assay.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetIntegrin alpha-4/beta-1(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50108219((5S,8R,13R)-8-[(S)-2-Acetylamino-3-(4-hydroxy-phen...)
Affinity DataIC50:  3nMAssay Description:Inhibition of purified alpha-4 beta-1 binding to VCAM-1 was determined in an ELISA assay.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 10(Homo sapiens (Human))
Elan Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50352624(CHEMBL1822305 | US9796706, Compound 139)
Affinity DataIC50:  3nMAssay Description:Inhibition of recombinant JNK3 using ser73 of c-jun as substrate preincubated for 15 mins measured after 60 mins by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 8(Homo sapiens (Human))
Elan Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50352614(CHEMBL1822145)
Affinity DataIC50:  3nMAssay Description:Inhibition of recombinant JNK1 using ser73 of c-jun as substrate preincubated for 15 mins measured after 60 mins by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 8(Homo sapiens (Human))
Elan Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50352613(CHEMBL1822144)
Affinity DataIC50:  3nMAssay Description:Inhibition of recombinant JNK1 using ser73 of c-jun as substrate preincubated for 15 mins measured after 60 mins by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
Imago Pharmaceuticals

US Patent
LigandPNGBDBM258287(US9493485, 9-128)
Affinity DataIC50:  4nMpH: 7.0Assay Description:BACE1 activity can be assessed in an AlphaScreenŽ assay. Compounds to be assessed (e.g. compounds as described in the above examples) are serially di...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetIntegrin alpha-4/beta-1(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50060179((5S,8R,13R,15aS)-8-[(S)-2-Amino-3-(4-hydroxy-3-iod...)
Affinity DataIC50:  4nMAssay Description:Inhibition of purified alpha-4 beta-1 binding to VCAM-1 was determined in an ELISA assay.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 8(Homo sapiens (Human))
Elan Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50352626(CHEMBL1822307 | US9796706, Compound 131)
Affinity DataIC50:  4nMAssay Description:Inhibition of recombinant JNK1 using ser73 of c-jun as substrate preincubated for 15 mins measured after 60 mins by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
Imago Pharmaceuticals

US Patent
LigandPNGBDBM258309(US9493485, 9-150)
Affinity DataIC50:  4nMpH: 4.5 T: 2°CAssay Description:Compounds are also assessed for BACE1 and Cathepsin D activity using an FP Assay. Compounds to be assessed (e.g. compounds as described in the above ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetIntegrin alpha-4/beta-1(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50060230((5S,8R,13R,15aS)-8-{[(2R,3R)-1-Acetyl-3-(4-hydroxy...)
Affinity DataIC50:  4nMAssay Description:Inhibition of purified alpha-4 beta-1 binding to VCAM-1 was determined in an ELISA assay.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetIntegrin alpha-4/beta-1(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50060168((5S,8R,13R,15aS)-8-[(S)-2-Amino-3-(4-hydroxy-pheny...)
Affinity DataIC50:  4nMAssay Description:Inhibition of purified alpha-4 beta-1 binding to VCAM-1 was determined in an ELISA assay.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
Elan Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM16016(CHEMBL437747 | N-cyclohexyl-4-[4-(3,4-dichlorophen...)
Affinity DataIC50:  4nMAssay Description:Inhibition of recombinant p38alpha after 60 mins by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetIntegrin alpha-4/beta-1(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50060233((5S,8R,13R,15aS)-8-[(S)-2-Acetylamino-3-(4-hydroxy...)
Affinity DataIC50:  4nMAssay Description:Inhibition of purified alpha-4 beta-1 binding to VCAM-1 was determined in an ELISA assay.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 8(Homo sapiens (Human))
Elan Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50338292(CHEMBL1682014 | N-(4-chloro-3-(1H-1,2,4-triazol-5-...)
Affinity DataIC50:  4nMAssay Description:Inhibition of recombinant JNK1 after 60 mins by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 8(Homo sapiens (Human))
Elan Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50352609(CHEMBL1822140)
Affinity DataIC50:  4nMAssay Description:Inhibition of recombinant JNK1 using ser73 of c-jun as substrate preincubated for 15 mins measured after 60 mins by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 8(Homo sapiens (Human))
Elan Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50352610(CHEMBL1822141)
Affinity DataIC50:  4nMAssay Description:Inhibition of recombinant JNK1 using ser73 of c-jun as substrate preincubated for 15 mins measured after 60 mins by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1(Homo sapiens (Human))
Imago Pharmaceuticals

US Patent
LigandPNGBDBM258283(US9493485, 9-124)
Affinity DataIC50:  4.5nMpH: 7.0Assay Description:BACE1 activity can be assessed in an AlphaScreenŽ assay. Compounds to be assessed (e.g. compounds as described in the above examples) are serially di...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetBeta-secretase 1(Homo sapiens (Human))
Imago Pharmaceuticals

US Patent
LigandPNGBDBM258304(US9493485, 9-145)
Affinity DataIC50:  4.5nMpH: 7.0Assay Description:BACE1 activity can be assessed in an AlphaScreenŽ assay. Compounds to be assessed (e.g. compounds as described in the above examples) are serially di...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
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