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TargetTyrosine-protein kinase JAK2(Mouse)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50355501(RUXOLITINIB PHOSPHATE | INCB-018424 | RUXOLITINIB ...)
Affinity DataEC50:  186nMAssay Description:Inhibition of JAK2 V617F mutant expressed in mouse BaF3 cells cells assessed as reduction in cell viabilityMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetPeroxisome proliferator-activated receptor delta(Human)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM50555357(CHEMBL1254751)
Affinity DataEC50:  1.25E+4nMAssay Description:Antagonist activity at PPARdelta LBD (unknown origin) assessed as increase in recruitment of SMRT ID2 corepressor peptide by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetPeroxisome proliferator-activated receptor delta(Human)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM50555363(CHEMBL4758410)
Affinity DataEC50:  2.02E+4nMAssay Description:Antagonist activity at PPARdelta LBD (unknown origin) assessed as increase in recruitment of SMRT ID2 corepressor peptide by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetPeroxisome proliferator-activated receptor delta(Human)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM50383373(GSK0660 | CHEMBL592652)
Affinity DataEC50:  4.34E+3nMAssay Description:Antagonist activity at PPARdelta LBD (unknown origin) assessed as increase in recruitment of SMRT ID2 corepressor peptide by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetPeroxisome proliferator-activated receptor gamma(Human)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM50555357(CHEMBL1254751)
Affinity DataEC50:  6.85E+3nMAssay Description:Agonist activity at PPARgamma LBD (unknown origin) assessed as increase in recruitment of coactivator peptide fluorescein-TRAP220/DRIP by TR-FRET ass...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetPeroxisome proliferator-activated receptor gamma(Human)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM50555363(CHEMBL4758410)
Affinity DataEC50:  9.95E+3nMAssay Description:Agonist activity at PPARgamma LBD (unknown origin) assessed as increase in recruitment of coactivator peptide fluorescein-TRAP220/DRIP by TR-FRET ass...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetPeroxisome proliferator-activated receptor gamma(Human)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM50085048((S)-2-(2-benzoylphenylamino)-3-(4-(2-(methyl(pyrid...)
Affinity DataEC50:  17nMAssay Description:Agonist activity at PPARgamma LBD (unknown origin) assessed as increase in recruitment of coactivator peptide fluorescein-TRAP220/DRIP by TR-FRET ass...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetPeroxisome proliferator-activated receptor gamma(Human)
Seoul National University

Curated by ChEMBL
LigandPNGBDBM50085045(5-((4-((6-hydroxy-2,5,7,8-tetramethyl-3,4-dihydro-...)
Affinity DataEC50:  1.38E+3nMAssay Description:Agonist activity at PPARgamma LBD (unknown origin) assessed as increase in recruitment of coactivator peptide fluorescein-TRAP220/DRIP by TR-FRET ass...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50386567(CHEMBL2048437)
Affinity DataIC50: 1.30nMAssay Description:Antagonist activity at human P2X7 receptor in human THP1 cells assessed as inhibition of BzATP-induced IL8 release pretreated for 30 mins before bzAT...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetTyrosine-protein kinase JAK3(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50193995(CP-690550 | 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrro...)
Affinity DataIC50: 1.60nMAssay Description:Inhibition of JAK3 (unknown origin) measured after 1 hr in presence of ATP by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetTyrosine-protein kinase JAK1(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50193995(CP-690550 | 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrro...)
Affinity DataIC50: 3.20nMAssay Description:Inhibition of human JAK1 using GEEPLYWSFPAKKK as substrate measured after 40 mins in presence of ATP by scintillation counting methodMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetTyrosine-protein kinase JAK1(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50355501(RUXOLITINIB PHOSPHATE | INCB-018424 | RUXOLITINIB ...)
Affinity DataIC50: 3.20nMAssay Description:Inhibition of human JAK1 using GEEPLYWSFPAKKK as substrate measured after 40 mins in presence of ATP by scintillation counting methodMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50355501(RUXOLITINIB PHOSPHATE | INCB-018424 | RUXOLITINIB ...)
Affinity DataIC50: 4.10nMAssay Description:Inhibition of recombinant human C-terminal 6His-tagged JAK2 (808 to end amino acids) expressed in Sf21 cells measured after 1 hr in presence of ATP b...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase JAK2(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50193995(CP-690550 | 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrro...)
Affinity DataIC50: 4.10nMAssay Description:Inhibition of recombinant human C-terminal 6His-tagged JAK2 (808 to end amino acids) expressed in Sf21 cells measured after 1 hr in presence of ATP b...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50386567(CHEMBL2048437)
Affinity DataIC50: 4.90nMAssay Description:Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced ethidium bromide uptake after 2 hrs by f...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50386566(CHEMBL2048438)
Affinity DataIC50: 9.20nMAssay Description:Antagonist activity at human P2X7 receptor in human THP1 cells assessed as inhibition of BzATP-induced IL8 release pretreated for 30 mins before bzAT...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50386566(CHEMBL2048438)
Affinity DataIC50: 13nMAssay Description:Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced ethidium bromide uptake after 2 hrs by f...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50075452(CHEMBL3415315)
Affinity DataIC50: 14nMAssay Description:Antagonist activity at P2X7 receptor in LPS/IFN-gamma-differentiated human THP1 cells assessed as inhibition of BzATP-induced IL-1beta release preinc...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50075454(CHEMBL3415330)
Affinity DataIC50: 15nMAssay Description:Antagonist activity at P2X7 receptor in LPS/IFN-gamma-differentiated human THP1 cells assessed as inhibition of BzATP-induced IL-1beta release preinc...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50075452(CHEMBL3415315)
Affinity DataIC50: 23nMAssay Description:Antagonist activity at recombinant human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced intracellular ethidium bromi...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50075455(CHEMBL3415331)
Affinity DataIC50: 27nMAssay Description:Antagonist activity at P2X7 receptor in LPS/IFN-gamma-differentiated human THP1 cells assessed as inhibition of BzATP-induced IL-1beta release preinc...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50075458(CHEMBL3415334)
Affinity DataIC50: 29nMAssay Description:Antagonist activity at P2X7 receptor in LPS/IFN-gamma-differentiated human THP1 cells assessed as inhibition of BzATP-induced IL-1beta release preinc...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50075455(CHEMBL3415331)
Affinity DataIC50: 30nMAssay Description:Antagonist activity at recombinant human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced intracellular ethidium bromi...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50230061((S)-4-(3-(4-benzoylpiperazin-1-yl)-2-(benzyloxycar...)
Affinity DataIC50: 34nMAssay Description:Antagonist activity at human P2X7 receptorMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50230072((S)-tert-butyl 4-(3-(4-(isoquinolin-5-ylsulfonylox...)
Affinity DataIC50: 41nMAssay Description:Antagonist activity at human P2X7 receptorMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50533709(CHEMBL4564551)
Affinity DataIC50: 42nMAssay Description:Inhibition of recombinant human C-terminal 6His-tagged JAK2 (808 to end amino acids) expressed in Sf21 cells measured after 1 hr in presence of ATP b...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50386572(CHEMBL2048286)
Affinity DataIC50: 42nMAssay Description:Antagonist activity at human P2X7 receptor in human THP1 cells assessed as inhibition of BzATP-induced IL8 release pretreated for 30 mins before bzAT...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50075457(CHEMBL3415333)
Affinity DataIC50: 49nMAssay Description:Antagonist activity at P2X7 receptor in LPS/IFN-gamma-differentiated human THP1 cells assessed as inhibition of BzATP-induced IL-1beta release preinc...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50075467(CHEMBL3415342)
Affinity DataIC50: 50nMAssay Description:Antagonist activity at P2X7 receptor in LPS/IFN-gamma-differentiated human THP1 cells assessed as inhibition of BzATP-induced IL-1beta release preinc...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50075467(CHEMBL3415342)
Affinity DataIC50: 50nMAssay Description:Antagonist activity at P2X7 receptor in LPS/IFN-gamma-differentiated human THP1 cells assessed as inhibition of BzATP-induced IL-1beta release preinc...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50087267((S)-4-(2-(N-methylisoquinoline-5-sulfonamido)-3-ox...)
Affinity DataIC50: 51nMAssay Description:Antagonist activity at human P2X7 receptorMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50386573(CHEMBL2048285)
Affinity DataIC50: 56nMAssay Description:Antagonist activity at human P2X7 receptor in human THP1 cells assessed as inhibition of BzATP-induced IL8 release pretreated for 30 mins before bzAT...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50533711(CHEMBL4460736)
Affinity DataIC50: 63nMAssay Description:Inhibition of recombinant human C-terminal 6His-tagged JAK2 (808 to end amino acids) expressed in Sf21 cells measured after 1 hr in presence of ATP b...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50533704(CHEMBL4475579)
Affinity DataIC50: 64nMAssay Description:Inhibition of recombinant human C-terminal 6His-tagged JAK2 (808 to end amino acids) expressed in Sf21 cells measured after 1 hr in presence of ATP b...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50533706(CHEMBL4474787)
Affinity DataIC50: 67nMAssay Description:Inhibition of recombinant human C-terminal 6His-tagged JAK2 (808 to end amino acids) expressed in Sf21 cells measured after 1 hr in presence of ATP b...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50075457(CHEMBL3415333)
Affinity DataIC50: 69nMAssay Description:Antagonist activity at recombinant human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced intracellular ethidium bromi...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50075467(CHEMBL3415342)
Affinity DataIC50: 70nMAssay Description:Antagonist activity at recombinant human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced intracellular ethidium bromi...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50075467(CHEMBL3415342)
Affinity DataIC50: 70nMAssay Description:Antagonist activity at recombinant human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced intracellular ethidium bromi...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50533712(CHEMBL4518995)
Affinity DataIC50: 72nMAssay Description:Inhibition of recombinant human C-terminal 6His-tagged JAK2 (808 to end amino acids) expressed in Sf21 cells measured after 1 hr in presence of ATP b...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetTyrosine-protein kinase JAK1(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50533713(CHEMBL4445037)
Affinity DataIC50: 72nMAssay Description:Inhibition of human JAK1 using GEEPLYWSFPAKKK as substrate measured after 40 mins in presence of ATP by scintillation counting methodMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50075466(CHEMBL3415341)
Affinity DataIC50: 72nMAssay Description:Antagonist activity at P2X7 receptor in LPS/IFN-gamma-differentiated human THP1 cells assessed as inhibition of BzATP-induced IL-1beta release preinc...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50075466(CHEMBL3415341)
Affinity DataIC50: 73nMAssay Description:Antagonist activity at recombinant human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced intracellular ethidium bromi...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50533713(CHEMBL4445037)
Affinity DataIC50: 74nMAssay Description:Inhibition of recombinant human C-terminal 6His-tagged JAK2 (808 to end amino acids) expressed in Sf21 cells measured after 1 hr in presence of ATP b...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50386568(CHEMBL2048436)
Affinity DataIC50: 77nMAssay Description:Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced ethidium bromide uptake after 2 hrs by f...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50075451(CHEMBL3415314)
Affinity DataIC50: 80nMAssay Description:Antagonist activity at P2X7 receptor in LPS/IFN-gamma-differentiated human THP1 cells assessed as inhibition of BzATP-induced IL-1beta release preinc...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50075456(CHEMBL3415332)
Affinity DataIC50: 81nMAssay Description:Antagonist activity at P2X7 receptor in LPS/IFN-gamma-differentiated human THP1 cells assessed as inhibition of BzATP-induced IL-1beta release preinc...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50075465(CHEMBL3415340)
Affinity DataIC50: 81nMAssay Description:Antagonist activity at P2X7 receptor in LPS/IFN-gamma-differentiated human THP1 cells assessed as inhibition of BzATP-induced IL-1beta release preinc...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetTyrosine-protein kinase JAK1(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50533707(CHEMBL4537821)
Affinity DataIC50: 82nMAssay Description:Inhibition of human JAK1 using GEEPLYWSFPAKKK as substrate measured after 40 mins in presence of ATP by scintillation counting methodMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50075454(CHEMBL3415330)
Affinity DataIC50: 84nMAssay Description:Antagonist activity at recombinant human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced intracellular ethidium bromi...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Gwangju Institute of Science and Technology (Gist)

Curated by ChEMBL
LigandPNGBDBM50533707(CHEMBL4537821)
Affinity DataIC50: 96nMAssay Description:Inhibition of recombinant human C-terminal 6His-tagged JAK2 (808 to end amino acids) expressed in Sf21 cells measured after 1 hr in presence of ATP b...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
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