Compile Data Set for Download or QSAR
Report error Found 97 Enz. Inhib. hit(s) with Target = 'G protein-coupled receptor kinase 4'
LigandPNGBDBM130909(US8822500, Stauro- sporine | US9920060, Staurospor...)
Affinity DataIC50: 8.40nMAssay Description:Inhibition of human GRK4 using casein as substrate preincubated for 20 mins followed by [gamma-33P]-ATP addition and measured after 120 mins by radio...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM50308060(CEP-701 | 16-hydroxy-16-(hydroxymethyl)-15-methyl-...)
Affinity DataKd:  12nMAssay Description:Binding affinity to GRK4More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/11/2011
Entry Details Article
PubMed
LigandPNGBDBM50308060(CEP-701 | 16-hydroxy-16-(hydroxymethyl)-15-methyl-...)
Affinity DataKd:  12nMAssay Description:Binding constant for GRK4 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM50026612(BIBF-1120 | Nintedanib | Vargatef | US10981896, Co...)
Affinity DataKd:  17nMAssay Description:Binding constant for GRK4 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM50566949(CHEMBL4877302)
Affinity DataIC50: 22nMAssay Description:Inhibition of human GRK4 using casein as substrate in presence of [gamma33P]ATP by radiometric hotspot kinase assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/19/2022
Entry Details Article
PubMed
LigandPNGBDBM2579(CHEMBL388978 | Staurosporine, 8 | Staurosporin, 4 ...)
Affinity DataKd:  37nMAssay Description:Binding constant for GRK4 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM2579(CHEMBL388978 | Staurosporine, 8 | Staurosporin, 4 ...)
Affinity DataIC50: 69.9nMAssay Description:Inhibition of human GRK4 using casein as substrate by [gamma-33P]-ATP assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/27/2022
Entry Details Article
PubMed
LigandPNGBDBM50355496(CHEMBL1908397)
Affinity DataKd:  71nMAssay Description:Binding constant for GRK4 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM25118(4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-...)
Affinity DataKd:  97nMAssay Description:Binding constant for GRK4 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM50566946(CHEMBL4854871)
Affinity DataIC50: 97nMAssay Description:Inhibition of human GRK4 using casein as substrate in presence of [gamma33P]ATP by radiometric hotspot kinase assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/19/2022
Entry Details Article
PubMed
LigandPNGBDBM50326053(PKC-412 | CHEMBL608533 | US20240132489, Compound S...)
Affinity DataKd:  110nMAssay Description:Binding affinity to GRK4More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/11/2011
Entry Details Article
PubMed
LigandPNGBDBM50326053(PKC-412 | CHEMBL608533 | US20240132489, Compound S...)
Affinity DataKd:  110nMAssay Description:Binding constant for GRK4 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM2579(CHEMBL388978 | Staurosporine, 8 | Staurosporin, 4 ...)
Affinity DataIC50: 112nMAssay Description:Inhibition of human GRK4 using casein as substrate by [gamma-33P]-ATP assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/19/2021
Entry Details Article
PubMed
LigandPNGBDBM4814(SUNITINIB MALATE | CHEMBL535 | N-[2-(diethylamino)...)
Affinity DataKd:  140nMAssay Description:Binding constant for GRK4 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM4814(SUNITINIB MALATE | CHEMBL535 | N-[2-(diethylamino)...)
Affinity DataKd:  140nMAssay Description:Binding affinity to GRK4More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/11/2011
Entry Details Article
PubMed
LigandPNGBDBM50332294(N-tert-butyl-3-(5-methyl-2-(4-(2-(pyrrolidin-1-yl)...)
Affinity DataKd:  170nMAssay Description:Binding constant for GRK4 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM50566947(CHEMBL4847703)
Affinity DataIC50: 190nMAssay Description:Inhibition of human GRK4 using casein as substrate in presence of [gamma33P]ATP by radiometric hotspot kinase assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/19/2022
Entry Details Article
PubMed
LigandPNGBDBM50536679(CHEMBL4568087)
Affinity DataIC50: 260nMAssay Description:Inhibition of full-length recombinant human GST-tagged GRK4 expressed in baculovirus expression system by Z'-LYTE assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/2/2021
Entry Details Article
PubMed
LigandPNGBDBM3149(Acyclic Balanol Analog (-)-1 | 2-{[2,6-dihydroxy-4...)
Affinity DataIC50: 260nMAssay Description:Inhibition of GRK4-mediated bovine tubulin phosphorylation by scintillation countingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/17/2010
Entry Details Article
PubMed
LigandPNGBDBM31095(5-[(Z)-(5-fluoranyl-2-oxidanylidene-1H-indol-3-yli...)
Affinity DataKd:  370nMAssay Description:Binding constant for GRK4 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM13534(VX680 | N-[4-[[4-(4-methylpiperazino)-6-[(5-methyl...)
Affinity DataKd:  400nMAssay Description:Binding constant for GRK4 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM50242737((R,Z)-5-(2,6-dichlorobenzylsulfonyl)-3-((3,5-dimet...)
Affinity DataKd:  420nMAssay Description:Binding constant for GRK4 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM60665(US9145414, R406 | US9212178, R406 | BDBM50249542 |...)
Affinity DataKd:  450nMAssay Description:Binding constant for GRK4 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM17055((9S)-9-[(dimethylamino)methyl]-6,7,10,11-tetrahydr...)
Affinity DataKd:  590nMAssay Description:Binding constant for GRK4 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM50536681(CHEMBL4552628)
Affinity DataIC50: 670nMAssay Description:Inhibition of full-length recombinant human GST-tagged GRK4 expressed in baculovirus expression system by Z'-LYTE assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/2/2021
Entry Details Article
PubMed
LigandPNGBDBM50311017(N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyri...)
Affinity DataIC50: 1.00E+3nMAssay Description:Inhibition of GRK4 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM174948(US9096593, P-2049)
Affinity DataIC50: 1.00E+3nMAssay Description:Inhibition of GRK4 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM15138(Biochemistry 469551 Compound 11 | 5-indazolyl pyri...)
Affinity DataKd:  1.40E+3nMAssay Description:Binding constant for GRK4 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM50355499(CHEMBL1908395 | CHEMBL1908842 | US20250129067, Com...)
Affinity DataKd:  2.20E+3nMAssay Description:Binding constant for GRK4 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM25117(AG-013736 | N-methyl-2-({3-[(E)-2-(pyridin-2-yl)et...)
Affinity DataKd:  2.30E+3nMAssay Description:Binding constant for GRK4 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM50355500(CHEMBL1908394 | US9695172, GSK461364)
Affinity DataKd:  2.80E+3nMAssay Description:Binding constant for GRK4 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM50326054(CHEMBL1240703)
Affinity DataKd:  2.90E+3nMAssay Description:Binding affinity to GRK4More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/11/2011
Entry Details Article
PubMed
LigandPNGBDBM482158(TAE684 | BDBM50242742)
Affinity DataKd:  3.50E+3nMAssay Description:Binding constant for GRK4 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataKd:  4.20E+3nMAssay Description:Binding constant for GRK4 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM4552(CHEMBL288441 | SKI-606 | 4-[(2,4-Dichloro-5-methox...)
Affinity DataKd:  4.90E+3nMAssay Description:Binding constant for GRK4 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM50536675(CHEMBL4569508)
Affinity DataIC50: 5.30E+3nMAssay Description:Inhibition of full-length recombinant human GST-tagged GRK4 expressed in baculovirus expression system by Z'-LYTE assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/2/2021
Entry Details Article
PubMed
LigandPNGBDBM50355501(RUXOLITINIB PHOSPHATE | INCB-018424 | RUXOLITINIB ...)
Affinity DataKd:  6.10E+3nMAssay Description:Binding constant for GRK4 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM25084(JMC504279 Compound 6 | 3-[2,4-diamino-6-(3-hydroxy...)
Affinity DataKd:  6.20E+3nMAssay Description:Binding constant for GRK4 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM5446(Erlotinib | OSI-774 | N-(3-ethynylphenyl)-6,7-bis(...)
Affinity DataKd:  7.30E+3nMAssay Description:Binding constant for GRK4 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM31085(cid_11409972 | 1-[4-[(4-ethylpiperazin-1-yl)methyl...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for GRK4 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM12621(2,4-Diamino-5-ketopyrimidine 39 | 5-[(2,3-difluoro...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for GRK4 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM50331096(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-6-methoxy-7...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for GRK4 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM5447(ZD1839 | N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for GRK4 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM5931(cid_3025986 | CHEMBL296468 | N-(5-{[(5-tert-butyl-...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for GRK4 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM50355504(CHEMBL1908393)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for GRK4 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM4779(cid_156414 | PD0183805 | CHEMBL545315 | CHEMBL3196...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for GRK4 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM15244(cid_3038525 | 5-(2,6-dichlorophenyl)-2-[(2,4-diflu...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for GRK4 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM16673(Xarelto | BAY439006 | CHEMBL1336 | BAY 43-9006 | 4...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for GRK4 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM21079(1-[4-(3-azanyl-1H-indazol-4-yl)phenyl]-3-(2-fluora...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for GRK4 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM13530(cid_5291 | STI571 | N-(4-methyl-3-{[4-(pyridin-3-y...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for GRK4 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
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