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Found 436 with Last Name = 'dale' and Initial = 't'
TargetCyclin-dependent kinase 2/G1/S-specific cyclin-E1(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM498545((1R,3S)-3-[3-({[2- (methylsulfonyl)phenyl]acetyl}...)
Affinity DataKi:  0.280nMAssay Description:The purpose of CDK2/Cyclin E1 assay is to evaluate the inhibition (% inhibition, Kiapp and Ki values) of small molecule inhibitors by using a fluores...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetCyclin-dependent kinase 2/G1/S-specific cyclin-E1(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM611576(US11718603, Example 1 | US20230321042, Compound C)
Affinity DataKi:  0.550nMAssay Description:The purpose of CDK2/Cyclin E1 assay is to evaluate the inhibition (% inhibition, Kiapp and Ki values) of small molecule inhibitors by using a fluores...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetCyclin-dependent kinase 2/G1/S-specific cyclin-E1(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM498185(US11014911, Example 13 | US11718603, Example 13 | ...)
Affinity DataKi:  1.16nMAssay Description:The purpose of CDK2/Cyclin E1 assay is to evaluate the inhibition (% inhibition, Kiapp and Ki values) of small molecule inhibitors by using a fluores...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM34012(3-fluorophenylalanine derivative, 21b)
Affinity DataKi:  6nM ΔG°:  -45.4kJ/molepH: 7.5 T: 2°CAssay Description:The cis/trans conversion of cis-Suc-AEPFpNA peptide by the PPIase led to the cleavage of para nitroaniline by subtilisin which was monitored at 390 n...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM34011(3-fluorophenylalanine derivative, 21a)
Affinity DataKi:  8nM ΔG°:  -44.7kJ/molepH: 7.5 T: 2°CAssay Description:The cis/trans conversion of cis-Suc-AEPFpNA peptide by the PPIase led to the cleavage of para nitroaniline by subtilisin which was monitored at 390 n...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM34013(3-methylphenylalanine derivative, 22a)
Affinity DataKi:  32nM ΔG°:  -41.3kJ/molepH: 7.5 T: 2°CAssay Description:The cis/trans conversion of cis-Suc-AEPFpNA peptide by the PPIase led to the cleavage of para nitroaniline by subtilisin which was monitored at 390 n...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM34014(3-methylphenylalanine derivative, 22b)
Affinity DataKi:  57nM ΔG°:  -40.0kJ/molepH: 7.5 T: 2°CAssay Description:The cis/trans conversion of cis-Suc-AEPFpNA peptide by the PPIase led to the cleavage of para nitroaniline by subtilisin which was monitored at 390 n...More data for this Ligand-Target Pair
LigandPNGBDBM34015(2,3-difluorophenylalanine derivative, 23a)
Affinity DataKi:  78nM ΔG°:  -39.2kJ/molepH: 7.5 T: 2°CAssay Description:The cis/trans conversion of cis-Suc-AEPFpNA peptide by the PPIase led to the cleavage of para nitroaniline by subtilisin which was monitored at 390 n...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM34016(2,3-difluorophenylalanine derivative, 23b)
Affinity DataKi:  89nM ΔG°:  -38.9kJ/molepH: 7.5 T: 2°CAssay Description:The cis/trans conversion of cis-Suc-AEPFpNA peptide by the PPIase led to the cleavage of para nitroaniline by subtilisin which was monitored at 390 n...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM34009(naphthalene carboxamide, 18a)
Affinity DataKi:  100nM ΔG°:  -38.6kJ/molepH: 7.5 T: 2°CAssay Description:The cis/trans conversion of cis-Suc-AEPFpNA peptide by the PPIase led to the cleavage of para nitroaniline by subtilisin which was monitored at 390 n...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 4/G1/S-specific cyclin-D1(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM498545((1R,3S)-3-[3-({[2- (methylsulfonyl)phenyl]acetyl}...)
Affinity DataKi:  107nMAssay Description:The purpose CDK4/Cyclin D1 assay is to evaluate the inhibition (% inhibition, Kiapp and Ki values) in the presence of small molecule inhibitors by us...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetCyclin-dependent kinase 4/G1/S-specific cyclin-D1(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM611576(US11718603, Example 1 | US20230321042, Compound C)
Affinity DataKi:  149nMAssay Description:The purpose CDK4/Cyclin D1 assay is to evaluate the inhibition (% inhibition, Kiapp and Ki values) in the presence of small molecule inhibitors by us...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM34010(benzothiophene carboxamide, 18b)
Affinity DataKi:  179nM ΔG°:  -37.2kJ/molepH: 7.5 T: 2°CAssay Description:The cis/trans conversion of cis-Suc-AEPFpNA peptide by the PPIase led to the cleavage of para nitroaniline by subtilisin which was monitored at 390 n...More data for this Ligand-Target Pair
TargetCyclin-dependent kinase 6/G1/S-specific cyclin-D3(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM611576(US11718603, Example 1 | US20230321042, Compound C)
Affinity DataKi:  215nMAssay Description:The purpose of the CDK6/Cyclin D3 assay is to evaluate the inhibition (% inhibition, Kiapp and Ki values) in the presence of small molecule inhibitor...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetCyclin-dependent kinase 4/G1/S-specific cyclin-D1(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM498185(US11014911, Example 13 | US11718603, Example 13 | ...)
Affinity DataKi:  243nMAssay Description:The purpose CDK4/Cyclin D1 assay is to evaluate the inhibition (% inhibition, Kiapp and Ki values) in the presence of small molecule inhibitors by us...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetCyclin-dependent kinase 6/G1/S-specific cyclin-D3(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM498545((1R,3S)-3-[3-({[2- (methylsulfonyl)phenyl]acetyl}...)
Affinity DataKi:  254nMAssay Description:The purpose of the CDK6/Cyclin D3 assay is to evaluate the inhibition (% inhibition, Kiapp and Ki values) in the presence of small molecule inhibitor...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetCyclin-dependent kinase 6/G1/S-specific cyclin-D3(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM498185(US11014911, Example 13 | US11718603, Example 13 | ...)
Affinity DataKi:  465nMAssay Description:The purpose of the CDK6/Cyclin D3 assay is to evaluate the inhibition (% inhibition, Kiapp and Ki values) in the presence of small molecule inhibitor...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM34008(amide, 17c)
Affinity DataKi:  525nM ΔG°:  -34.6kJ/molepH: 7.5 T: 2°CAssay Description:The cis/trans conversion of cis-Suc-AEPFpNA peptide by the PPIase led to the cleavage of para nitroaniline by subtilisin which was monitored at 390 n...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM34005(pipecolate deriv., 12b)
Affinity DataKi:  800nM ΔG°:  -33.6kJ/molepH: 7.5 T: 2°CAssay Description:The cis/trans conversion of cis-Suc-AEPFpNA peptide by the PPIase led to the cleavage of para nitroaniline by subtilisin which was monitored at 390 n...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMelanin-concentrating hormone receptor 1(Homo sapiens (Human))
Alchemia

Curated by ChEMBL
LigandPNGBDBM50326858(CHEMBL1254556 | N-((3R,4R,5S,6R)-2,4-bis(4-chlorob...)
Affinity DataKi:  1.20E+3nMAssay Description:Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM34003(pipecolate deriv., 11)
Affinity DataKi:  1.70E+3nM ΔG°:  -31.8kJ/molepH: 7.5 T: 2°CAssay Description:The cis/trans conversion of cis-Suc-AEPFpNA peptide by the PPIase led to the cleavage of para nitroaniline by subtilisin which was monitored at 390 n...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMelanin-concentrating hormone receptor 1(Homo sapiens (Human))
Alchemia

Curated by ChEMBL
LigandPNGBDBM50326859(CHEMBL1254630 | N-((3R,4R,5S,6R)-4-(4-chlorobenzyl...)
Affinity DataKi:  1.80E+3nMAssay Description:Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMelanin-concentrating hormone receptor 1(Homo sapiens (Human))
Alchemia

Curated by ChEMBL
LigandPNGBDBM50326860(CHEMBL1254711 | N-((3R,4R,5S,6R)-2-(4-chlorobenzyl...)
Affinity DataKi:  2.60E+3nMAssay Description:Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMelanin-concentrating hormone receptor 1(Homo sapiens (Human))
Alchemia

Curated by ChEMBL
LigandPNGBDBM50326861(CHEMBL1254796 | N-((3R,4R,5S,6R)-4-(4-chlorobenzyl...)
Affinity DataKi:  3.50E+3nMAssay Description:Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM34007(urea, 17b)
Affinity DataKi:  4.13E+3nM ΔG°:  -29.7kJ/molepH: 7.5 T: 2°CAssay Description:The cis/trans conversion of cis-Suc-AEPFpNA peptide by the PPIase led to the cleavage of para nitroaniline by subtilisin which was monitored at 390 n...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMelanin-concentrating hormone receptor 1(Homo sapiens (Human))
Alchemia

Curated by ChEMBL
LigandPNGBDBM50326862(4-(diaminomethyleneamino)-N-((3R,4R,5S,6R)-5-hydro...)
Affinity DataKi:  5.10E+3nMAssay Description:Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMelanin-concentrating hormone receptor 1(Homo sapiens (Human))
Alchemia

Curated by ChEMBL
LigandPNGBDBM50326863(3-(diaminomethyleneamino)-N-((3R,4R,5S,6R)-5-hydro...)
Affinity DataKi:  6.30E+3nMAssay Description:Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMelanin-concentrating hormone receptor 1(Homo sapiens (Human))
Alchemia

Curated by ChEMBL
LigandPNGBDBM50326864(CHEMBL1254883 | N-((3R,4R,5S,6R)-4-(4-chlorobenzyl...)
Affinity DataKi:  6.60E+3nMAssay Description:Displacement of [I125I]MCH from human MCH1 receptor expressed in CHO cells by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM34006(sulfonamide, 17a)
Affinity DataKi:  8.77E+3nM ΔG°:  -27.9kJ/molepH: 7.5 T: 2°CAssay Description:The cis/trans conversion of cis-Suc-AEPFpNA peptide by the PPIase led to the cleavage of para nitroaniline by subtilisin which was monitored at 390 n...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM34004(pipecolate deriv., 12a)
Affinity DataKi:  9.46E+3nM ΔG°:  -27.7kJ/molepH: 7.5 T: 2°CAssay Description:The cis/trans conversion of cis-Suc-AEPFpNA peptide by the PPIase led to the cleavage of para nitroaniline by subtilisin which was monitored at 390 n...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM34001(pipecolate deriv., 9)
Affinity DataKi: >5.00E+4nM ΔG°: >-23.7kJ/molepH: 7.5 T: 2°CAssay Description:The cis/trans conversion of cis-Suc-AEPFpNA peptide by the PPIase led to the cleavage of para nitroaniline by subtilisin which was monitored at 390 n...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEphrin type-B receptor 4(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50195876(3-(4-amino-3-{4-[3-(2-fluoro-5-trifluoromethyl-phe...)
Affinity DataIC50:  0.400nMAssay Description:Inhibition of human EphB4 by scintillation proximity methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Gsk

LigandPNGBDBM26477(5-[(6,7-dimethoxyquinazolin-4-yl)amino]-2-methylph...)
Affinity DataIC50:  0.600nMpH: 7.5 T: 2°CAssay Description:The assay uses purified baculovirus-expressed GST-VEGFR2 interacting with biotinylated peptide substrates. HTRF is based on the proximity of europium...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 8(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50191472(CHEMBL3956719)
Affinity DataIC50:  0.600nMAssay Description:Inhibition of CDK8 in human 7dF3 cells preincubated for 2 hrs followed by beta-oestradiol addition measured after 24 hrs by luciferase reporter gene ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Gsk

LigandPNGBDBM26467(3-({4-[methyl(3-methyl-1H-indazol-6-yl)amino]pyrim...)
Affinity DataIC50:  0.600nMpH: 7.5 T: 2°CAssay Description:The assay uses purified baculovirus-expressed GST-VEGFR2 interacting with biotinylated peptide substrates. HTRF is based on the proximity of europium...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Gsk

LigandPNGBDBM5829(1-[2-fluoro-5-(trifluoromethyl)phenyl]-3-{4-[methy...)
Affinity DataIC50:  1nMpH: 7.5 T: 2°CAssay Description:The assay was using baculovirus-expressed recombinant protein kinase purified as the intracellular domain fused by GST tag, interacting with biotinyl...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50256016(CHEMBL475768 | N-(3-chloro-4-(3-fluorobenzyloxy)ph...)
Affinity DataIC50:  1nMAssay Description:Inhibition of EGFRMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Gsk

LigandPNGBDBM5828(1-[2-fluoro-5-(trifluoromethyl)phenyl]-3-{4-[methy...)
Affinity DataIC50:  1nMpH: 7.5 T: 2°CAssay Description:The assay was using baculovirus-expressed recombinant protein kinase purified as the intracellular domain fused by GST tag, interacting with biotinyl...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-C(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50191414(CHEMBL3947140)
Affinity DataIC50:  1.30nMAssay Description:Inhibition of Alexa647 tracer binding to full length recombinant human His-tagged CDK8/cyclin C expressed in Baculovirus expression system preincubat...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-C(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50191472(CHEMBL3956719)
Affinity DataIC50:  1.40nMAssay Description:Inhibition of Alexa647 tracer binding to full length recombinant human His-tagged CDK8/cyclin C expressed in Baculovirus expression system preincubat...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 8(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50163767(CHEMBL3798944)
Affinity DataIC50:  1.60nMAssay Description:Binding affinity to His-tagged CDK8 (unknown origin) after 60 mins by FRET based lanthascreen binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 8(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50163774(CHEMBL3797855)
Affinity DataIC50:  1.70nMAssay Description:Binding affinity to His-tagged CDK8 (unknown origin) after 60 mins by FRET based lanthascreen binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Gsk

LigandPNGBDBM26478(6,7-dimethoxy-N-(3-methyl-1H-indazol-6-yl)quinazol...)
Affinity DataIC50:  1.70nMpH: 7.5 T: 2°CAssay Description:The assay uses purified baculovirus-expressed GST-VEGFR2 interacting with biotinylated peptide substrates. HTRF is based on the proximity of europium...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetCyclin-C(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50191373(CHEMBL3966985)
Affinity DataIC50:  1.70nMAssay Description:Inhibition of Alexa647 tracer binding to full length recombinant human His-tagged CDK8/cyclin C expressed in Baculovirus expression system preincubat...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 8(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50163857(CHEMBL3798853)
Affinity DataIC50:  1.90nMAssay Description:Binding affinity to His-tagged CDK8 (unknown origin) after 60 mins by FRET based lanthascreen binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Gsk

LigandPNGBDBM5827(1-[2-fluoro-5-(trifluoromethyl)phenyl]-3-{4-[(2-{[...)
Affinity DataIC50:  2nMpH: 7.5 T: 2°CAssay Description:The assay was using baculovirus-expressed recombinant protein kinase purified as the intracellular domain fused by GST tag, interacting with biotinyl...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 8(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50191373(CHEMBL3966985)
Affinity DataIC50:  2nMAssay Description:Inhibition of CDK8 in human 7dF3 cells preincubated for 2 hrs followed by beta-oestradiol addition measured after 24 hrs by luciferase reporter gene ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50256032(CHEMBL475594 | N-(3-chloro-4-(3-fluorobenzyloxy)ph...)
Affinity DataIC50:  2nMAssay Description:Inhibition of EGFRMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Gsk

LigandPNGBDBM5832(3-{4-[methyl({2-[(3-sulfamoylphenyl)amino]pyrimidi...)
Affinity DataIC50:  2nMpH: 7.5 T: 2°CAssay Description:The assay was using baculovirus-expressed recombinant protein kinase purified as the intracellular domain fused by GST tag, interacting with biotinyl...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Gsk

LigandPNGBDBM5833(3-{4-[methyl({2-[(4-sulfamoylphenyl)amino]pyrimidi...)
Affinity DataIC50:  2nMpH: 7.5 T: 2°CAssay Description:The assay was using baculovirus-expressed recombinant protein kinase purified as the intracellular domain fused by GST tag, interacting with biotinyl...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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