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TargetInterleukin-1 receptor-associated kinase 4(Rat)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50242696(CHEMBL4083650 | US9932350, 2-5)
Affinity DataEC50:  1.70E+3nMAssay Description:Inhibition of IRAK4 in Lewis rat whole blood assessed as reduction in R848-stimulated TNF alpha production after 4 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/16/2019
Entry Details Article
PubMed
TargetInterleukin-1 receptor-associated kinase 4(Rat)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50242697(CHEMBL4070214 | US9932350, 2-7)
Affinity DataEC50:  2.30E+3nMAssay Description:Inhibition of IRAK4 in Lewis rat whole blood assessed as reduction in R848-stimulated TNF alpha production after 4 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/16/2019
Entry Details Article
PubMed
TargetNuclear receptor subfamily 1 group I member 2(Human)
Merck Research Laboratories Boston

Curated by ChEMBL
LigandPNGBDBM50498590(CHEMBL3609637)
Affinity DataEC50: >3.00E+4nMAssay Description:Activation of PXR (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/3/2020
Entry Details Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50114800(CHEMBL3609749)
Affinity DataEC50:  1.30E+4nMAssay Description:Inhibition of human ERG expressed in CHO cells by patch clamp assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/24/2016
Entry Details Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50114805(CHEMBL3608384)
Affinity DataEC50:  9.00E+3nMAssay Description:Inhibition of human ERG expressed in CHO cells by patch clamp assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/24/2016
Entry Details Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50114806(CHEMBL3609752)
Affinity DataEC50:  2.20E+3nMAssay Description:Inhibition of human ERG expressed in CHO cells by patch clamp assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/24/2016
Entry Details Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50114807(CHEMBL3608385)
Affinity DataEC50:  1.30E+3nMAssay Description:Inhibition of human ERG expressed in CHO cells by patch clamp assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/24/2016
Entry Details Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50114810(CHEMBL3609754)
Affinity DataEC50:  9.00E+3nMAssay Description:Inhibition of human ERG expressed in CHO cells by patch clamp assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/24/2016
Entry Details Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50114837(CHEMBL3609755)
Affinity DataEC50:  7.50E+3nMAssay Description:Inhibition of human ERG expressed in CHO cells by patch clamp assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/24/2016
Entry Details Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50114845(CHEMBL3609759)
Affinity DataEC50:  1.50E+4nMAssay Description:Inhibition of human ERG expressed in CHO cells by patch clamp assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/24/2016
Entry Details Article
PubMed
TargetTyrosine-protein kinase SYK(Human)
Merck

Curated by ChEMBL
LigandPNGBDBM50075813(CHEMBL3415598)
Affinity DataIC50: 0.0100nMAssay Description:Inhibition of full-length GST-tagged human Syk preincubated for 10 mins followed by peptide substrate/ATP addition measured after 45 mins by TR-FRET ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2016
Entry Details Article
PubMed
TargetTyrosine-protein kinase SYK(Human)
Merck

Curated by ChEMBL
LigandPNGBDBM50075735(CHEMBL3415583)
Affinity DataIC50: 0.0600nMAssay Description:Inhibition of full-length GST-tagged human Syk preincubated for 10 mins followed by peptide substrate/ATP addition measured after 45 mins by TR-FRET ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2016
Entry Details Article
PubMed
LigandPNGBDBM50630435(CHEMBL5407732)
Affinity DataIC50: 0.0800nMAssay Description:Inhibition of recombinant N-terminal GST-fused LRRK2 G2109S mutant (970 to 2527 residues) (unknown origin) using LRRKtide peptide as substrate assess...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/20/2024
Entry Details
PubMed
LigandPNGBDBM50630441(CHEMBL5405380)
Affinity DataIC50: 0.0800nMAssay Description:Inhibition of recombinant N-terminal GST-fused LRRK2 G2109S mutant (970 to 2527 residues) (unknown origin) using LRRKtide peptide as substrate assess...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/20/2024
Entry Details
PubMed
LigandPNGBDBM50630442(CHEMBL5433289)
Affinity DataIC50: 0.0800nMAssay Description:Inhibition of recombinant N-terminal GST-fused LRRK2 G2109S mutant (970 to 2527 residues) (unknown origin) using LRRKtide peptide as substrate assess...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/20/2024
Entry Details
PubMed
TargetTyrosine-protein kinase SYK(Human)
Merck

Curated by ChEMBL
LigandPNGBDBM50075740(CHEMBL3415589)
Affinity DataIC50: 0.100nMAssay Description:Inhibition of full-length GST-tagged human Syk preincubated for 10 mins followed by peptide substrate/ATP addition measured after 45 mins by TR-FRET ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2016
Entry Details Article
PubMed
TargetTyrosine-protein kinase SYK(Human)
Merck

Curated by ChEMBL
LigandPNGBDBM50075744(CHEMBL3415594)
Affinity DataIC50: 0.100nMAssay Description:Inhibition of full-length GST-tagged human Syk preincubated for 10 mins followed by peptide substrate/ATP addition measured after 45 mins by TR-FRET ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2016
Entry Details Article
PubMed
TargetTyrosine-protein kinase SYK(Human)
Merck

Curated by ChEMBL
LigandPNGBDBM50075922(CHEMBL3415606)
Affinity DataIC50: 0.100nMAssay Description:Inhibition of full-length GST-tagged human Syk preincubated for 10 mins followed by peptide substrate/ATP addition measured after 45 mins by TR-FRET ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2016
Entry Details Article
PubMed
LigandPNGBDBM50630443(CHEMBL5422978)
Affinity DataIC50: 0.110nMAssay Description:Inhibition of recombinant N-terminal GST-fused LRRK2 G2109S mutant (970 to 2527 residues) (unknown origin) using LRRKtide peptide as substrate assess...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/20/2024
Entry Details
PubMed
LigandPNGBDBM50630444(CHEMBL5396547)
Affinity DataIC50: 0.200nMAssay Description:Inhibition of recombinant N-terminal GST-fused LRRK2 G2109S mutant (970 to 2527 residues) (unknown origin) using LRRKtide peptide as substrate assess...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/20/2024
Entry Details
PubMed
TargetTyrosine-protein kinase SYK(Human)
Merck

Curated by ChEMBL
LigandPNGBDBM50075747(CHEMBL3415597)
Affinity DataIC50: 0.200nMAssay Description:Inhibition of full-length GST-tagged human Syk preincubated for 10 mins followed by peptide substrate/ATP addition measured after 45 mins by TR-FRET ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2016
Entry Details Article
PubMed
LigandPNGBDBM50095475(CHEMBL3590479)
Affinity DataIC50: 0.200nMAssay Description:Inhibition of human IRAK4 assessed as phosphorylation of fluorescent peptide substrate after 30 mins by fluorescent polarization readerMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/17/2016
Entry Details Article
PubMed
LigandPNGBDBM50609728(CHEMBL5267350)
Affinity DataIC50: 0.300nMAssay Description:Inhibition of GST20-tagged human LRRK2 G2019S mutant using LRRKtide peptide preincubated for 15 mins followed by substrate addition and measured afte...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM50609742(CHEMBL5286106)
Affinity DataIC50: 0.300nMAssay Description:Inhibition of GST20-tagged LRRK2 in human SH-SY5Y cells assessed as reduction in pSer935 phosphorylation incubated for 90 mins by MSD assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM50609742(CHEMBL5286106)
Affinity DataIC50: 0.300nMAssay Description:Inhibition of LRRK2 in human PBMCs assessed as reduction in Ser95 phosphorylationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM50095470(CHEMBL3590474 | US10155765, Example 9)
Affinity DataIC50: 0.300nMAssay Description:Inhibition of human IRAK4 assessed as phosphorylation of fluorescent peptide substrate after 30 mins by fluorescent polarization readerMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/17/2016
Entry Details Article
PubMed
LigandPNGBDBM50095474(CHEMBL3590478 | US10329294, Example 2)
Affinity DataIC50: 0.300nMAssay Description:Inhibition of human IRAK4 assessed as phosphorylation of fluorescent peptide substrate after 30 mins by fluorescent polarization readerMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/17/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50609741(CHEMBL5284341)
Affinity DataIC50: 0.400nMAssay Description:Inhibition of GST20-tagged LRRK2 in human SH-SY5Y cells assessed as reduction in pSer935 phosphorylation incubated for 90 mins by MSD assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM548467(WO2022093881, Ex-7.4)
Affinity DataIC50: 0.400nMAssay Description:Inhibition of recombinant N-terminal GST-fused LRRK2 G2109S mutant (970 to 2527 residues) (unknown origin) using LRRKtide peptide as substrate assess...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/20/2024
Entry Details
PubMed
TargetTyrosine-protein kinase SYK(Human)
Merck

Curated by ChEMBL
LigandPNGBDBM50075819(CHEMBL3415604)
Affinity DataIC50: 0.400nMAssay Description:Inhibition of full-length GST-tagged human Syk preincubated for 10 mins followed by peptide substrate/ATP addition measured after 45 mins by TR-FRET ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2016
Entry Details Article
PubMed
LigandPNGBDBM257207(US9493440, 51)
Affinity DataIC50: 0.5nMAssay Description:Inhibition of GST20-tagged human LRRK2 G2019S mutant using LRRKtide peptide preincubated for 15 mins followed by substrate addition and measured afte...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
LigandPNGBDBM50630437(CHEMBL5419587)
Affinity DataIC50: 0.5nMAssay Description:Inhibition of recombinant N-terminal GST-fused LRRK2 G2109S mutant (970 to 2527 residues) (unknown origin) using LRRKtide peptide as substrate assess...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/20/2024
Entry Details
PubMed
TargetTyrosine-protein kinase SYK(Human)
Merck

Curated by ChEMBL
LigandPNGBDBM50075738(CHEMBL3415587)
Affinity DataIC50: 0.5nMAssay Description:Inhibition of full-length GST-tagged human Syk preincubated for 10 mins followed by peptide substrate/ATP addition measured after 45 mins by TR-FRET ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2016
Entry Details Article
PubMed
TargetTyrosine-protein kinase SYK(Human)
Merck

Curated by ChEMBL
LigandPNGBDBM50075742(CHEMBL3415592)
Affinity DataIC50: 0.5nMAssay Description:Inhibition of full-length GST-tagged human Syk preincubated for 10 mins followed by peptide substrate/ATP addition measured after 45 mins by TR-FRET ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2016
Entry Details Article
PubMed
TargetTyrosine-protein kinase SYK(Human)
Merck

Curated by ChEMBL
LigandPNGBDBM50075732(CHEMBL3414584 | US9775839, 2.1)
Affinity DataIC50: 0.5nMAssay Description:Inhibition of full-length GST-tagged human Syk preincubated for 10 mins followed by peptide substrate/ATP addition measured after 45 mins by TR-FRET ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2016
Entry Details Article
PubMed
LigandPNGBDBM50095532(CHEMBL3590515 | US10329294, Example 173)
Affinity DataIC50: 0.5nMAssay Description:Inhibition of human IRAK4 assessed as phosphorylation of fluorescent peptide substrate after 30 mins by fluorescent polarization readerMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/17/2016
Entry Details Article
PubMed
LigandPNGBDBM50095534(CHEMBL3590516 | US10329294, Example 252)
Affinity DataIC50: 0.5nMAssay Description:Inhibition of human IRAK4 assessed as phosphorylation of fluorescent peptide substrate after 30 mins by fluorescent polarization readerMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/17/2016
Entry Details Article
PubMed
LigandPNGBDBM50630438(CHEMBL5428129)
Affinity DataIC50: 0.600nMAssay Description:Inhibition of recombinant N-terminal GST-fused LRRK2 G2109S mutant (970 to 2527 residues) (unknown origin) using LRRKtide peptide as substrate assess...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/20/2024
Entry Details
PubMed
LigandPNGBDBM50630439(CHEMBL5400861)
Affinity DataIC50: 0.600nMAssay Description:Inhibition of recombinant N-terminal GST-fused LRRK2 G2109S mutant (970 to 2527 residues) (unknown origin) using LRRKtide peptide as substrate assess...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/20/2024
Entry Details
PubMed
TargetTyrosine-protein kinase SYK(Human)
Merck

Curated by ChEMBL
LigandPNGBDBM50075730(CHEMBL3415599)
Affinity DataIC50: 0.600nMAssay Description:Inhibition of full-length GST-tagged human Syk preincubated for 10 mins followed by peptide substrate/ATP addition measured after 45 mins by TR-FRET ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2016
Entry Details Article
PubMed
LigandPNGBDBM50609741(CHEMBL5284341)
Affinity DataIC50: 0.700nMAssay Description:Inhibition of GST20-tagged human LRRK2 G2019S mutant using LRRKtide peptide preincubated for 15 mins followed by substrate addition and measured afte...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
TargetTyrosine-protein kinase SYK(Human)
Merck

Curated by ChEMBL
LigandPNGBDBM50075733(CHEMBL3415610 | US9775839, 8.5)
Affinity DataIC50: 0.700nMAssay Description:Inhibition of full-length GST-tagged human Syk preincubated for 10 mins followed by peptide substrate/ATP addition measured after 45 mins by TR-FRET ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2016
Entry Details Article
PubMed
LigandPNGBDBM50630436(CHEMBL5411697)
Affinity DataIC50: 0.800nMAssay Description:Inhibition of recombinant N-terminal GST-fused LRRK2 G2109S mutant (970 to 2527 residues) (unknown origin) using LRRKtide peptide as substrate assess...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/20/2024
Entry Details
PubMed
TargetTyrosine-protein kinase SYK(Human)
Merck

Curated by ChEMBL
LigandPNGBDBM50075739(CHEMBL3415588)
Affinity DataIC50: 0.800nMAssay Description:Inhibition of full-length GST-tagged human Syk preincubated for 10 mins followed by peptide substrate/ATP addition measured after 45 mins by TR-FRET ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2016
Entry Details Article
PubMed
TargetTyrosine-protein kinase SYK(Human)
Merck

Curated by ChEMBL
LigandPNGBDBM50075743(CHEMBL3415593)
Affinity DataIC50: 0.800nMAssay Description:Inhibition of full-length GST-tagged human Syk preincubated for 10 mins followed by peptide substrate/ATP addition measured after 45 mins by TR-FRET ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2016
Entry Details Article
PubMed
LigandPNGBDBM50095473(CHEMBL3590477 | US10329294, Example 282)
Affinity DataIC50: 0.800nMAssay Description:Inhibition of human IRAK4 assessed as phosphorylation of fluorescent peptide substrate after 30 mins by fluorescent polarization readerMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/17/2016
Entry Details Article
PubMed
LigandPNGBDBM50609742(CHEMBL5286106)
Affinity DataIC50: 0.900nMAssay Description:Inhibition of GST20-tagged human LRRK2 G2019S mutant using LRRKtide peptide preincubated for 15 mins followed by substrate addition and measured afte...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/20/2024
Entry Details
PubMed
TargetTyrosine-protein kinase SYK(Human)
Merck

Curated by ChEMBL
LigandPNGBDBM50075745(CHEMBL3415595)
Affinity DataIC50: 0.900nMAssay Description:Inhibition of full-length GST-tagged human Syk preincubated for 10 mins followed by peptide substrate/ATP addition measured after 45 mins by TR-FRET ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2016
Entry Details Article
PubMed
TargetNuclear receptor ROR-gamma(Human)
Merck

Curated by ChEMBL
LigandPNGBDBM329724(US9663522, 6B | (3S,4R)-1-(1-(2-chloro-6-cycloprop...)
Affinity DataIC50: 1nMAssay Description:Allosteric inhibition of recombinant His6-tagged RORgammat LBD (unknown origin) expressed in Escherichia coli BL21(DE3) assessed as inhibition of bio...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/20/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase SYK(Human)
Merck

Curated by ChEMBL
LigandPNGBDBM50075821(CHEMBL3415605)
Affinity DataIC50: 1nMAssay Description:Inhibition of full-length GST-tagged human Syk preincubated for 10 mins followed by peptide substrate/ATP addition measured after 45 mins by TR-FRET ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2016
Entry Details Article
PubMed
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