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LigandPNGBDBM50582730(CHEMBL5087055)
Affinity DataKd:  3.70nMAssay Description:Binding affinity to human LRRK2 WT expressed in mammalian system assessed as dissociation constant measured at 1 uM by DiscoveRx KINOMEscan assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails Article
PubMed
LigandPNGBDBM50582731(CHEMBL5092087)
Affinity DataKd:  6.60nMAssay Description:Binding affinity to human LRRK2 WT expressed in mammalian system assessed as dissociation constant measured at 1 uM by DiscoveRx KINOMEscan assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails Article
PubMed
LigandPNGBDBM50582730(CHEMBL5087055)
Affinity DataKd:  3.90nMAssay Description:Binding affinity to human LRRK2 (H970/E2527) G2019S mutant expressed in mammalian system assessed as dissociation constant measured at 1 uM by Discov...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails Article
PubMed
LigandPNGBDBM50582731(CHEMBL5092087)
Affinity DataKd:  5.5nMAssay Description:Binding affinity to human LRRK2 (H970/E2527) G2019S mutant expressed in mammalian system assessed as dissociation constant measured at 1 uM by Discov...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails Article
PubMed
TargetReceptor-type tyrosine-protein kinase FLT3(Human)
Vernalis (R&D)

Curated by ChEMBL
LigandPNGBDBM50582730(CHEMBL5087055)
Affinity DataKd:  470nMAssay Description:Binding affinity to human FLT3 ITD, D835V (V592/Y969) mutant expressed in mammalian system assessed as dissociation constant measured at 1 uM by Disc...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails Article
PubMed
TargetReceptor-type tyrosine-protein kinase FLT3(Human)
Vernalis (R&D)

Curated by ChEMBL
LigandPNGBDBM50582731(CHEMBL5092087)
Affinity DataKd:  67nMAssay Description:Binding affinity to human FLT3 ITD, D835V (V592/Y969) mutant expressed in mammalian system assessed as dissociation constant measured at 1 uM by Disc...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails Article
PubMed
TargetPhosphatidylinositol 4-kinase beta(Human)
Vernalis (R&D)

Curated by ChEMBL
LigandPNGBDBM50582730(CHEMBL5087055)
Affinity DataKd:  850nMAssay Description:Binding affinity to human PIK4CB (M1/M828) WT expressed in mammalian system assessed as dissociation constant measured at 1 uM by DiscoveRx KINOMEsca...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails Article
PubMed
TargetPhosphatidylinositol 4-kinase beta(Human)
Vernalis (R&D)

Curated by ChEMBL
LigandPNGBDBM50582731(CHEMBL5092087)
Affinity DataKd:  730nMAssay Description:Binding affinity to human PIK4CB (M1/M828) WT expressed in mammalian system assessed as dissociation constant measured at 1 uM by DiscoveRx KINOMEsca...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Mouse)
Lundbeck Research Usa

Curated by ChEMBL
LigandPNGBDBM50585248(CHEMBL2338352)
Affinity DataIC50: 0.650nMAssay Description:Antagonist activity at mouse P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium-flux measured after 60 mins by F...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetP2X purinoceptor 7(Human)
Lundbeck Research Usa

Curated by ChEMBL
LigandPNGBDBM50352039(CHEMBL1823817)
Affinity DataIC50: 0.760nMAssay Description:Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium-flux measured after 60 mins by F...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Rat)
Lundbeck Research Usa

Curated by ChEMBL
LigandPNGBDBM50587051(CHEMBL5086274)
Affinity DataIC50: 2.40nMAssay Description:Antagonist activity at rat P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium-flux measured after 60 mins by FLI...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Human)
Lundbeck Research Usa

Curated by ChEMBL
LigandPNGBDBM50267791(AZD-9056 | AZD9056)
Affinity DataIC50: 3.5nMAssay Description:Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium-flux measured after 60 mins by F...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Rat)
Lundbeck Research Usa

Curated by ChEMBL
LigandPNGBDBM50234965(A-740003 | N-(1-{[(Cyanoimino)(5-quinolinylamino)m...)
Affinity DataIC50: 4nMAssay Description:Antagonist activity at rat P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium-flux measured after 60 mins by FLI...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Rat)
Lundbeck Research Usa

Curated by ChEMBL
LigandPNGBDBM50267791(AZD-9056 | AZD9056)
Affinity DataIC50: 4.40nMAssay Description:Antagonist activity at rat P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium-flux measured after 60 mins by FLI...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetP2X purinoceptor 7(Rat)
Lundbeck Research Usa

Curated by ChEMBL
LigandPNGBDBM50585248(CHEMBL2338352)
Affinity DataIC50: 4.70nMAssay Description:Antagonist activity at rat P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium-flux measured after 60 mins by FLI...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50582714(CHEMBL5075978)
Affinity DataIC50: 5nMAssay Description:Inhibition of recombinant human GST tagged truncated LRRK2 G2019S mutant using fluorescein-labeled LRRKtide as substrate in presence of ATP preincuba...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Human)
Lundbeck Research Usa

Curated by ChEMBL
LigandPNGBDBM198970(BDBM199009 | US9221832, 34 | BDBM199010)
Affinity DataIC50: 5.5nMAssay Description:Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium-flux measured after 60 mins by F...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails Article
PubMed
LigandPNGBDBM50582715(CHEMBL5091909)
Affinity DataIC50: 6nMAssay Description:Inhibition of recombinant human GST tagged truncated LRRK2 G2019S mutant using fluorescein-labeled LRRKtide as substrate in presence of ATP preincuba...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails Article
PubMed
LigandPNGBDBM50582714(CHEMBL5075978)
Affinity DataIC50: 6nMAssay Description:Inhibition of recombinant human LRRK2 WT using fluorescein-labeled LRRKtide as substrate in presence of ATP preincubated for 50 mins followed by anti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails Article
PubMed
LigandPNGBDBM50582715(CHEMBL5091909)
Affinity DataIC50: 6nMAssay Description:Inhibition of recombinant human LRRK2 WT using fluorescein-labeled LRRKtide as substrate in presence of ATP preincubated for 50 mins followed by anti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Rat)
Lundbeck Research Usa

Curated by ChEMBL
LigandPNGBDBM50237707(A-804598 | CHEMBL1628690)
Affinity DataIC50: 6.10nMAssay Description:Antagonist activity at rat P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium-flux measured after 60 mins by FLI...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM50582726(CHEMBL5086506)
Affinity DataIC50: 10nMAssay Description:Inhibition of recombinant human GST tagged truncated LRRK2 G2019S mutant using fluorescein-labeled LRRKtide as substrate in presence of ATP preincuba...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails Article
PubMed
LigandPNGBDBM50582707(CHEMBL5086513)
Affinity DataIC50: 11nMAssay Description:Inhibition of recombinant human GST tagged truncated LRRK2 G2019S mutant using fluorescein-labeled LRRKtide as substrate in presence of ATP preincuba...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails Article
PubMed
LigandPNGBDBM50582730(CHEMBL5087055)
Affinity DataIC50: 11nMAssay Description:Inhibition of LRRK2-WT in C57BL/6 mouse brain at 10 to 150 mg/kg and measured after 1 hrs by western blottingMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails Article
PubMed
LigandPNGBDBM50582729(CHEMBL5089152)
Affinity DataIC50: 12nMAssay Description:Inhibition of recombinant human GST tagged truncated LRRK2 G2019S mutant using fluorescein-labeled LRRKtide as substrate in presence of ATP preincuba...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails Article
PubMed
LigandPNGBDBM50582729(CHEMBL5089152)
Affinity DataIC50: 12nMAssay Description:Inhibition of recombinant human GST tagged truncated LRRK2 G2019S mutant using fluorescein-labeled LRRKtide as substrate in presence of ATP preincuba...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails Article
PubMed
LigandPNGBDBM50582730(CHEMBL5087055)
Affinity DataIC50: 12nMAssay Description:Inhibition of recombinant human GST tagged truncated LRRK2 G2019S mutant using fluorescein-labeled LRRKtide as substrate in presence of ATP preincuba...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Human)
Lundbeck Research Usa

Curated by ChEMBL
LigandPNGBDBM50587051(CHEMBL5086274)
Affinity DataIC50: 12nMAssay Description:Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium-flux measured after 60 mins by F...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM50582731(CHEMBL5092087)
Affinity DataIC50: 14nMAssay Description:Inhibition of recombinant human GST tagged truncated LRRK2 G2019S mutant using fluorescein-labeled LRRKtide as substrate in presence of ATP preincuba...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails Article
PubMed
LigandPNGBDBM50582707(CHEMBL5086513)
Affinity DataIC50: 15nMAssay Description:Inhibition of recombinant human LRRK2 WT using fluorescein-labeled LRRKtide as substrate in presence of ATP preincubated for 50 mins followed by anti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails Article
PubMed
LigandPNGBDBM50582726(CHEMBL5086506)
Affinity DataIC50: 16nMAssay Description:Inhibition of recombinant human LRRK2 WT using fluorescein-labeled LRRKtide as substrate in presence of ATP preincubated for 50 mins followed by anti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails Article
PubMed
LigandPNGBDBM50582730(CHEMBL5087055)
Affinity DataIC50: 16nMAssay Description:Inhibition of LRRK2-WT-pSER935 in C57BL/6 mouse brain at 10 to 150 mg/kg and measured after 1 hrs by western blottingMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails Article
PubMed
LigandPNGBDBM50582729(CHEMBL5089152)
Affinity DataIC50: 19nMAssay Description:Inhibition of recombinant human LRRK2 WT using fluorescein-labeled LRRKtide as substrate in presence of ATP preincubated for 50 mins followed by anti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails Article
PubMed
LigandPNGBDBM50582729(CHEMBL5089152)
Affinity DataIC50: 19nMAssay Description:Inhibition of recombinant human LRRK2 WT using fluorescein-labeled LRRKtide as substrate in presence of ATP preincubated for 50 mins followed by anti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails Article
PubMed
LigandPNGBDBM50582730(CHEMBL5087055)
Affinity DataIC50: 20nMAssay Description:Inhibition of recombinant human LRRK2 WT using fluorescein-labeled LRRKtide as substrate in presence of ATP preincubated for 50 mins followed by anti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Human)
Lundbeck Research Usa

Curated by ChEMBL
LigandPNGBDBM50416603(CHEMBL1222883)
Affinity DataIC50: 20nMAssay Description:Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium-flux measured after 60 mins by F...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM50582721(CHEMBL5080937)
Affinity DataIC50: 21nMAssay Description:Inhibition of recombinant human GST tagged truncated LRRK2 G2019S mutant using fluorescein-labeled LRRKtide as substrate in presence of ATP preincuba...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Human)
Lundbeck Research Usa

Curated by ChEMBL
LigandPNGBDBM50318021(2-chloro-N-((4,4-difluoro-1-hydroxycyclohexyl)meth...)
Affinity DataIC50: 21nMAssay Description:Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium-flux measured after 60 mins by F...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM50582731(CHEMBL5092087)
Affinity DataIC50: 22nMAssay Description:Inhibition of LRRK2-WT in C57BL/6 mouse brain at 10 to 150 mg/kg and measured after 1 hrs by western blottingMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Mouse)
Lundbeck Research Usa

Curated by ChEMBL
LigandPNGBDBM50587051(CHEMBL5086274)
Affinity DataIC50: 22nMAssay Description:Antagonist activity at mouse P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium-flux measured after 60 mins by F...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM50582731(CHEMBL5092087)
Affinity DataIC50: 23nMAssay Description:Inhibition of recombinant human LRRK2 WT using fluorescein-labeled LRRKtide as substrate in presence of ATP preincubated for 50 mins followed by anti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails Article
PubMed
LigandPNGBDBM50582731(CHEMBL5092087)
Affinity DataIC50: 23nMAssay Description:Inhibition of LRRK2-WT-pSER935 in C57BL/6 mouse brain at 10 to 150 mg/kg and measured after 1 hrs by western blottingMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails Article
PubMed
LigandPNGBDBM50582727(CHEMBL5075824)
Affinity DataIC50: 25nMAssay Description:Inhibition of recombinant human GST tagged truncated LRRK2 G2019S mutant using fluorescein-labeled LRRKtide as substrate in presence of ATP preincuba...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails Article
PubMed
LigandPNGBDBM50582720(CHEMBL5073900)
Affinity DataIC50: 27nMAssay Description:Inhibition of recombinant human GST tagged truncated LRRK2 G2019S mutant using fluorescein-labeled LRRKtide as substrate in presence of ATP preincuba...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails Article
PubMed
LigandPNGBDBM50582712(CHEMBL5090953)
Affinity DataIC50: 28nMAssay Description:Inhibition of recombinant human GST tagged truncated LRRK2 G2019S mutant using fluorescein-labeled LRRKtide as substrate in presence of ATP preincuba...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails Article
PubMed
LigandPNGBDBM50582719(CHEMBL5083563)
Affinity DataIC50: 30nMAssay Description:Inhibition of recombinant human GST tagged truncated LRRK2 G2019S mutant using fluorescein-labeled LRRKtide as substrate in presence of ATP preincuba...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Human)
Lundbeck Research Usa

Curated by ChEMBL
LigandPNGBDBM50237707(A-804598 | CHEMBL1628690)
Affinity DataIC50: 32nMAssay Description:Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium-flux measured after 60 mins by F...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM50582712(CHEMBL5090953)
Affinity DataIC50: 34nMAssay Description:Inhibition of recombinant human LRRK2 WT using fluorescein-labeled LRRKtide as substrate in presence of ATP preincubated for 50 mins followed by anti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails Article
PubMed
LigandPNGBDBM50582721(CHEMBL5080937)
Affinity DataIC50: 34nMAssay Description:Inhibition of recombinant human LRRK2 WT using fluorescein-labeled LRRKtide as substrate in presence of ATP preincubated for 50 mins followed by anti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails Article
PubMed
TargetP2X purinoceptor 7(Mouse)
Lundbeck Research Usa

Curated by ChEMBL
LigandPNGBDBM50237707(A-804598 | CHEMBL1628690)
Affinity DataIC50: 34nMAssay Description:Antagonist activity at mouse P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium-flux measured after 60 mins by F...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
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