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TargetBromodomain-containing protein 2 [364-436](Homo sapiens (Human))
The Regents of The University of Michigan

US Patent
LigandPNGBDBM50092323(CHEMBL3581656 | US9675697, Cpd. No. 21)
Affinity DataKi: <10nM ΔG°: <-45.7kJ/mole IC50:  93nMpH: 7.5 T: 2°CAssay Description:The FAM labeled fluorescent probe (BRD-1F) was synthesized based on a known small-molecule BET bromodomain inhibitor. Kd values of BRD-1F to these th...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBromodomain-containing protein 2 [364-436](Homo sapiens (Human))
The Regents of The University of Michigan

US Patent
LigandPNGBDBM179460(US9675697, Cpd. No. 17)
Affinity DataKi: <10nM ΔG°: <-45.7kJ/mole IC50:  142nMpH: 7.5 T: 2°CAssay Description:The FAM labeled fluorescent probe (BRD-1F) was synthesized based on a known small-molecule BET bromodomain inhibitor. Kd values of BRD-1F to these th...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetBromodomain-containing protein 4 [368-440](Homo sapiens (Human))
The Regents of The University of Michigan

US Patent
LigandPNGBDBM179460(US9675697, Cpd. No. 17)
Affinity DataKi:  16nM ΔG°:  -44.5kJ/mole IC50:  197nMpH: 7.5 T: 2°CAssay Description:The FAM labeled fluorescent probe (BRD-1F) was synthesized based on a known small-molecule BET bromodomain inhibitor. Kd values of BRD-1F to these th...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetBromodomain-containing protein 2 [364-436](Homo sapiens (Human))
The Regents of The University of Michigan

US Patent
LigandPNGBDBM179457(US9675697, Cpd. No. 3)
Affinity DataKi:  35nM ΔG°:  -42.6kJ/mole IC50:  255nMpH: 7.5 T: 2°CAssay Description:The FAM labeled fluorescent probe (BRD-1F) was synthesized based on a known small-molecule BET bromodomain inhibitor. Kd values of BRD-1F to these th...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetBromodomain-containing protein 4 [368-440](Homo sapiens (Human))
The Regents of The University of Michigan

US Patent
LigandPNGBDBM50092323(CHEMBL3581656 | US9675697, Cpd. No. 21)
Affinity DataKi:  38nM ΔG°:  -42.4kJ/mole IC50:  310nMpH: 7.5 T: 2°CAssay Description:The FAM labeled fluorescent probe (BRD-1F) was synthesized based on a known small-molecule BET bromodomain inhibitor. Kd values of BRD-1F to these th...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBromodomain-containing protein 2 [364-436](Homo sapiens (Human))
The Regents of The University of Michigan

US Patent
LigandPNGBDBM50092318(CHEMBL3581657 | US9675697, Cpd. No. 2)
Affinity DataKi:  42.3nM ΔG°:  -42.1kJ/mole IC50:  286nMpH: 7.5 T: 2°CAssay Description:The FAM labeled fluorescent probe (BRD-1F) was synthesized based on a known small-molecule BET bromodomain inhibitor. Kd values of BRD-1F to these th...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBromodomain-containing protein 2 [364-436](Homo sapiens (Human))
The Regents of The University of Michigan

US Patent
LigandPNGBDBM179458(US9675697, Cpd. No. 4)
Affinity DataKi:  57nM ΔG°:  -41.3kJ/mole IC50:  349nMpH: 7.5 T: 2°CAssay Description:The FAM labeled fluorescent probe (BRD-1F) was synthesized based on a known small-molecule BET bromodomain inhibitor. Kd values of BRD-1F to these th...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetBromodomain-containing protein 4 [368-440](Homo sapiens (Human))
The Regents of The University of Michigan

US Patent
LigandPNGBDBM179457(US9675697, Cpd. No. 3)
Affinity DataKi:  83nM ΔG°:  -40.4kJ/mole IC50:  514nMpH: 7.5 T: 2°CAssay Description:The FAM labeled fluorescent probe (BRD-1F) was synthesized based on a known small-molecule BET bromodomain inhibitor. Kd values of BRD-1F to these th...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetBromodomain-containing protein 4 [368-440](Homo sapiens (Human))
The Regents of The University of Michigan

US Patent
LigandPNGBDBM50092318(CHEMBL3581657 | US9675697, Cpd. No. 2)
Affinity DataKi:  114nM ΔG°:  -39.6kJ/mole IC50:  608nMpH: 7.5 T: 2°CAssay Description:The FAM labeled fluorescent probe (BRD-1F) was synthesized based on a known small-molecule BET bromodomain inhibitor. Kd values of BRD-1F to these th...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBromodomain-containing protein 4 [368-440](Homo sapiens (Human))
The Regents of The University of Michigan

US Patent
LigandPNGBDBM179458(US9675697, Cpd. No. 4)
Affinity DataKi:  232nM ΔG°:  -37.9kJ/mole IC50:  873nMpH: 7.5 T: 2°CAssay Description:The FAM labeled fluorescent probe (BRD-1F) was synthesized based on a known small-molecule BET bromodomain inhibitor. Kd values of BRD-1F to these th...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetBromodomain-containing protein 2 [364-436](Homo sapiens (Human))
The Regents of The University of Michigan

US Patent
LigandPNGBDBM50092339(CHEMBL3581648 | US9675697, RX-7)
Affinity DataKi:  366nM ΔG°:  -36.7kJ/mole IC50:  1.35E+3nMpH: 7.5 T: 2°CAssay Description:The FAM labeled fluorescent probe (BRD-1F) was synthesized based on a known small-molecule BET bromodomain inhibitor. Kd values of BRD-1F to these th...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBromodomain-containing protein 4 [368-440](Homo sapiens (Human))
The Regents of The University of Michigan

US Patent
LigandPNGBDBM179476(US9675697, Cpd. No. 34)
Affinity DataKi:  775nM ΔG°:  -34.9kJ/mole IC50:  3.67E+3nMpH: 7.5 T: 2°CAssay Description:The FAM labeled fluorescent probe (BRD-1F) was synthesized based on a known small-molecule BET bromodomain inhibitor. Kd values of BRD-1F to these th...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetBromodomain-containing protein 4 [368-440](Homo sapiens (Human))
The Regents of The University of Michigan

US Patent
LigandPNGBDBM50092339(CHEMBL3581648 | US9675697, RX-7)
Affinity DataKi:  850nM ΔG°:  -34.6kJ/mole IC50:  2.90E+3nMpH: 7.5 T: 2°CAssay Description:The FAM labeled fluorescent probe (BRD-1F) was synthesized based on a known small-molecule BET bromodomain inhibitor. Kd values of BRD-1F to these th...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBromodomain-containing protein 2 [364-436](Homo sapiens (Human))
The Regents of The University of Michigan

US Patent
LigandPNGBDBM179476(US9675697, Cpd. No. 34)
Affinity DataKi:  1.20E+3nM ΔG°:  -33.8kJ/mole IC50:  3.20E+3nMpH: 7.5 T: 2°CAssay Description:The FAM labeled fluorescent probe (BRD-1F) was synthesized based on a known small-molecule BET bromodomain inhibitor. Kd values of BRD-1F to these th...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetTissue factor(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM50235149(CHEMBL4066780)
Affinity DataIC50:  0.0280nMAssay Description:Inhibition of LPS-induced tissue factor procoagulant activity in human THP1 cells preincubated for 1 hr followed by LPS addition measured after 5 hrs...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCasein kinase II subunit alpha'(Homo sapiens (Human))
Bristol-Myers Squibb

US Patent
LigandPNGBDBM142829(US8940736, 391)
Affinity DataIC50:  0.0300nMpH: 7.4 T: 2°CAssay Description:The effectiveness of compounds of the present invention as inhibitors of protein kinases can be readily tested by assays known to those skilled in th...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBifunctional epoxide hydrolase 2(Homo sapiens (Human))
Shenyang Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM50595239(CHEMBL5190894)
Affinity DataIC50:  0.0300nMAssay Description:Inhibition of sEH (unknown origin)More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Hangzhou Xixi Hospital

Curated by ChEMBL
LigandPNGBDBM50021574(BMS-907351 | CABOZANTINIB | CHEBI:72317 | Cabomety...)
Affinity DataIC50:  0.0350nMAssay Description:Inhibition of VEGFR-2 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTissue factor(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM50235153(CHEBI:67985 | CHEMBL510111)
Affinity DataIC50:  0.0350nMAssay Description:Inhibition of LPS-induced tissue factor procoagulant activity in human THP1 cells preincubated for 1 hr followed by LPS addition measured after 5 hrs...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPalmitoleoyl-protein carboxylesterase NOTUM(Homo sapiens (Human))
University College London

Curated by ChEMBL
LigandPNGBDBM50554469(CHEMBL4796694)
Affinity DataIC50:  0.0510nMAssay Description:Inhibition of human Notum (S81-T451 residues) C330S mutant expressed in HEK293S cells using OPTS substrate incubated for 40 mins by fluorescence base...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTissue factor(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM50235152(CHEBI:4747 | CHEMBL230128)
Affinity DataIC50:  0.0540nMAssay Description:Inhibition of LPS-induced tissue factor procoagulant activity in human THP1 cells preincubated for 1 hr followed by LPS addition measured after 5 hrs...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCasein kinase II subunit alpha'(Homo sapiens (Human))
Bristol-Myers Squibb

US Patent
LigandPNGBDBM142775(US8940736, 7)
Affinity DataIC50:  0.0700nMpH: 7.4 T: 2°CAssay Description:The effectiveness of compounds of the present invention as inhibitors of protein kinases can be readily tested by assays known to those skilled in th...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetPalmitoleoyl-protein carboxylesterase NOTUM(Homo sapiens (Human))
University College London

Curated by ChEMBL
LigandPNGBDBM50554470(CHEMBL4752559)
Affinity DataIC50:  0.0750nMAssay Description:Inhibition of human Notum (S81-T451 residues) C330S mutant expressed in HEK293S cells using OPTS substrate incubated for 40 mins by fluorescence base...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTissue factor(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM50235142(CHEMBL4070749)
Affinity DataIC50:  0.0780nMAssay Description:Inhibition of LPS-induced tissue factor procoagulant activity in human THP1 cells preincubated for 1 hr followed by LPS addition measured after 5 hrs...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBifunctional epoxide hydrolase 2(Homo sapiens (Human))
Shenyang Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM50556773(CHEMBL4745610)
Affinity DataIC50:  0.0820nMAssay Description:Inhibition of recombinant human sEH using PHOME as substrate measured after 15 mins by fluorescence assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Hangzhou Xixi Hospital

Curated by ChEMBL
LigandPNGBDBM50021574(BMS-907351 | CABOZANTINIB | CHEBI:72317 | Cabomety...)
Affinity DataIC50:  0.0860nMAssay Description:Inhibition of VEGFR-2 (unknown origin) by HTRF methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCasein kinase II subunit alpha'(Homo sapiens (Human))
Bristol-Myers Squibb

US Patent
LigandPNGBDBM142816(US8940736, 281)
Affinity DataIC50:  0.0900nMpH: 7.4 T: 2°CAssay Description:The effectiveness of compounds of the present invention as inhibitors of protein kinases can be readily tested by assays known to those skilled in th...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetCasein kinase II subunit alpha'(Homo sapiens (Human))
Bristol-Myers Squibb

US Patent
LigandPNGBDBM142774(US8940736, 6)
Affinity DataIC50:  0.0900nMpH: 7.4 T: 2°CAssay Description:The effectiveness of compounds of the present invention as inhibitors of protein kinases can be readily tested by assays known to those skilled in th...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetTissue factor(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM50235147(Vitalboside A)
Affinity DataIC50:  0.0950nMAssay Description:Inhibition of LPS-induced tissue factor procoagulant activity in human THP1 cells preincubated for 1 hr followed by LPS addition measured after 5 hrs...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetE3 ubiquitin-protein ligase Mdm2(Homo sapiens (Human))
Shanghai Institute Of Materia Medica

Curated by ChEMBL
LigandPNGBDBM50605104(CHEMBL5180980)
Affinity DataIC50: <0.100nMAssay Description:Inhibition of human MDM2 by TR-FRET assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails PubMed
TargetRAC-gamma serine/threonine-protein kinase(Homo sapiens (Human))
Chinese Academy Of Sciences

Curated by ChEMBL
LigandPNGBDBM50528415(CHEMBL4457064)
Affinity DataIC50:  0.100nMAssay Description:Inhibition of Akt3 (unknown origin) by mobile shift assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetBifunctional epoxide hydrolase 2(Homo sapiens (Human))
Shenyang Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM50556760(CHEMBL4781218)
Affinity DataIC50:  0.100nMAssay Description:Inhibition of recombinant human sEH using PHOME as substrate measured after 15 mins by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCasein kinase II subunit alpha'(Homo sapiens (Human))
Bristol-Myers Squibb

US Patent
LigandPNGBDBM142835(US8940736, 402)
Affinity DataIC50:  0.110nMpH: 7.4 T: 2°CAssay Description:The effectiveness of compounds of the present invention as inhibitors of protein kinases can be readily tested by assays known to those skilled in th...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetCasein kinase II subunit alpha'(Homo sapiens (Human))
Bristol-Myers Squibb

US Patent
LigandPNGBDBM142792(US8940736, 160)
Affinity DataIC50:  0.110nMpH: 7.4 T: 2°CAssay Description:The effectiveness of compounds of the present invention as inhibitors of protein kinases can be readily tested by assays known to those skilled in th...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetCasein kinase II subunit alpha'(Homo sapiens (Human))
Bristol-Myers Squibb

US Patent
LigandPNGBDBM142777(US8940736, 49)
Affinity DataIC50:  0.110nMpH: 7.4 T: 2°CAssay Description:The effectiveness of compounds of the present invention as inhibitors of protein kinases can be readily tested by assays known to those skilled in th...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetRAC-gamma serine/threonine-protein kinase(Homo sapiens (Human))
Chinese Academy Of Sciences

Curated by ChEMBL
LigandPNGBDBM50528409(CHEMBL4441825)
Affinity DataIC50:  0.120nMAssay Description:Inhibition of Akt3 (unknown origin) by mobile shift assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetCasein kinase II subunit alpha(Homo sapiens (Human))
Bristol-Myers Squibb

US Patent
LigandPNGBDBM142829(US8940736, 391)
Affinity DataIC50:  0.130nMpH: 7.4 T: 2°CAssay Description:The effectiveness of compounds of the present invention as inhibitors of protein kinases can be readily tested by assays known to those skilled in th...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetCasein kinase II subunit alpha'(Homo sapiens (Human))
Bristol-Myers Squibb

US Patent
LigandPNGBDBM142822(US8940736, 328)
Affinity DataIC50:  0.130nMpH: 7.4 T: 2°CAssay Description:The effectiveness of compounds of the present invention as inhibitors of protein kinases can be readily tested by assays known to those skilled in th...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetCasein kinase II subunit alpha(Homo sapiens (Human))
Bristol-Myers Squibb

US Patent
LigandPNGBDBM142817(US8940736, 285)
Affinity DataIC50:  0.140nMpH: 7.4 T: 2°CAssay Description:The effectiveness of compounds of the present invention as inhibitors of protein kinases can be readily tested by assays known to those skilled in th...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetCasein kinase II subunit alpha(Homo sapiens (Human))
Bristol-Myers Squibb

US Patent
LigandPNGBDBM142774(US8940736, 6)
Affinity DataIC50:  0.150nMpH: 7.4 T: 2°CAssay Description:The effectiveness of compounds of the present invention as inhibitors of protein kinases can be readily tested by assays known to those skilled in th...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetCasein kinase II subunit alpha'(Homo sapiens (Human))
Bristol-Myers Squibb

US Patent
LigandPNGBDBM142784(US8940736, 117)
Affinity DataIC50:  0.150nMpH: 7.4 T: 2°CAssay Description:The effectiveness of compounds of the present invention as inhibitors of protein kinases can be readily tested by assays known to those skilled in th...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetCasein kinase II subunit alpha'(Homo sapiens (Human))
Bristol-Myers Squibb

US Patent
LigandPNGBDBM142806(US8940736, 229)
Affinity DataIC50:  0.160nMpH: 7.4 T: 2°CAssay Description:The effectiveness of compounds of the present invention as inhibitors of protein kinases can be readily tested by assays known to those skilled in th...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetCasein kinase II subunit alpha(Homo sapiens (Human))
Bristol-Myers Squibb

US Patent
LigandPNGBDBM142835(US8940736, 402)
Affinity DataIC50:  0.160nMpH: 7.4 T: 2°CAssay Description:The effectiveness of compounds of the present invention as inhibitors of protein kinases can be readily tested by assays known to those skilled in th...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetCasein kinase II subunit alpha'(Homo sapiens (Human))
Bristol-Myers Squibb

US Patent
LigandPNGBDBM142834(US8940736, 399)
Affinity DataIC50:  0.160nMpH: 7.4 T: 2°CAssay Description:The effectiveness of compounds of the present invention as inhibitors of protein kinases can be readily tested by assays known to those skilled in th...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetCasein kinase II subunit alpha(Homo sapiens (Human))
Bristol-Myers Squibb

US Patent
LigandPNGBDBM142775(US8940736, 7)
Affinity DataIC50:  0.170nMpH: 7.4 T: 2°CAssay Description:The effectiveness of compounds of the present invention as inhibitors of protein kinases can be readily tested by assays known to those skilled in th...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetPalmitoleoyl-protein carboxylesterase NOTUM(Homo sapiens (Human))
University College London

Curated by ChEMBL
LigandPNGBDBM50554462(CHEMBL4784029)
Affinity DataIC50:  0.190nMAssay Description:Inhibition of human Notum (S81-T451 residues) C330S mutant expressed in HEK293S cells using OPTS substrate incubated for 40 mins by fluorescence base...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetPalmitoleoyl-protein carboxylesterase NOTUM(Homo sapiens (Human))
University College London

Curated by ChEMBL
LigandPNGBDBM50554475(CHEMBL4757064)
Affinity DataIC50:  0.190nMAssay Description:Inhibition of human Notum (S81-T451 residues) C330S mutant expressed in HEK293S cells using OPTS substrate incubated for 40 mins by fluorescence base...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetCasein kinase II subunit alpha'(Homo sapiens (Human))
Bristol-Myers Squibb

US Patent
LigandPNGBDBM142778(US8940736, 55)
Affinity DataIC50:  0.200nMpH: 7.4 T: 2°CAssay Description:The effectiveness of compounds of the present invention as inhibitors of protein kinases can be readily tested by assays known to those skilled in th...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetPoly [ADP-ribose] polymerase 2(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM207586(US10501467, Example 31 | US9260440, 31 | US9617273...)
Affinity DataIC50:  0.200nMAssay Description:Inhibition of PARP-2 (unknown origin) pre-incubated for 30 mins before addition of activated DNA and NAD by chemiluminescent assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetHepatocyte growth factor receptor(Homo sapiens (Human))
Shenyang Pharmaceutical University

US Patent
LigandPNGBDBM344393((E)-N1-(3-fluoro-4-(6-methoxy-7-(3-(piperidin-1-yl...)
Affinity DataIC50:  0.200nMAssay Description:c-Met Kinase Activity was Measured with an ELISA Reader. The Specific Operation as Follows:To the plate filled with 0.25 mg/mL PGT, the compounds, 50...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
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