BindingDB PrimarySearch_ki

Found 229 with Last Name = 'coyle' and Initial = 'je'

Platelet-activating factor acetylhydrolase(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM50125265(CHEMBL204021 | N-(2-Diethylamino-ethyl)-2-[2-(4-fl...)

IC50: 0.0350nMAssay Description:Inhibition of Lp-PLA2 in whole human plasma pre-incubated for 15 mins before 2-thio-PAF substrate additionMore data for this Ligand-Target Pair

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3D Structure (crystal)

Platelet-activating factor acetylhydrolase(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM50125265(CHEMBL204021 | N-(2-Diethylamino-ethyl)-2-[2-(4-fl...)

IC50: 0.0490nMAssay Description:Inhibition of recombinant human Lp-PLA2 pre-incubated for 30 mins before PED6 fluorogenic substrateMore data for this Ligand-Target Pair

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3D Structure (crystal)

Platelet-activating factor acetylhydrolase(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM50125265(CHEMBL204021 | N-(2-Diethylamino-ethyl)-2-[2-(4-fl...)

IC50: 0.0490nMAssay Description:Inhibition of human recombinant Lp-PLA2 using 2-thio-PAF as substrate after 20 mins by CPM-based fluorescence assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

Platelet-activating factor acetylhydrolase(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM50125265(CHEMBL204021 | N-(2-Diethylamino-ethyl)-2-[2-(4-fl...)

IC50: 0.0490nMAssay Description:Inhibition of recombinant human Lp-PLA2 incubated for 20 mins by Thio-PAF assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

Mitogen-activated protein kinase 1(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM50573875(CHEMBL4869086)

IC50: 1.10nMAssay Description:Inhibition of full-length human N-terminal MAHHHHHH tagged-ERK2 expressed in Escherichia coli BL21 (DE3) using ATF2-GFP as substrate incubated for 30...More data for this Ligand-Target Pair

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Mitogen-activated protein kinase 1(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM418177(2-[(1R)-5-{5-chloro-2-[(oxan-4- yl)amino]pyrimidin...)

IC50: 1.10nMAssay Description:Inhibition of full-length human N-terminal MAHHHHHH tagged-ERK2 expressed in Escherichia coli BL21 (DE3) using ATF2-GFP as substrate incubated for 30...More data for this Ligand-Target Pair

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Mitogen-activated protein kinase 1(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM417999(US10457669, Example 675 | US11001575, Example 675)

IC50: 1.30nMAssay Description:Inhibition of full-length human N-terminal MAHHHHHH tagged-ERK2 expressed in Escherichia coli BL21 (DE3) using ATF2-GFP as substrate incubated for 30...More data for this Ligand-Target Pair

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Platelet-activating factor acetylhydrolase(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM50182422(CHEMBL3818650)

IC50: 1.40nMAssay Description:Inhibition of human recombinant Lp-PLA2 using 2-thio-PAF as substrate after 20 mins by CPM-based fluorescence assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

Mitogen-activated protein kinase 1(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM50573874(CHEMBL4873851)

IC50: 1.80nMAssay Description:Inhibition of full-length human N-terminal MAHHHHHH tagged-ERK2 expressed in Escherichia coli BL21 (DE3) using ATF2-GFP as substrate incubated for 30...More data for this Ligand-Target Pair

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Mitogen-activated protein kinase 1(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM418019(US10457669, Example 698 | US11001575, Example 698)

IC50: 1.80nMAssay Description:Inhibition of full-length human N-terminal MAHHHHHH tagged-ERK2 expressed in Escherichia coli BL21 (DE3) using ATF2-GFP as substrate incubated for 30...More data for this Ligand-Target Pair

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3D Structure (crystal)

Mitogen-activated protein kinase 1(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM418270((2R)-2-(6-{5-chloro-2-[(oxan-4- yl)amino]pyrimidin...)

IC50: 1.80nMAssay Description:Inhibition of full-length human N-terminal MAHHHHHH tagged-ERK2 expressed in Escherichia coli BL21 (DE3) using ATF2-GFP as substrate incubated for 30...More data for this Ligand-Target Pair

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Discoidin domain-containing receptor 2(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM13216(BMS-354825 | CHEMBL1421 | DASATINIB | N-(2-Chloro-...)

IC50: 2nMAssay Description:Inhibition of DDR2 (unknown origin) after 1 hr by time resolved fluorescence methodMore data for this Ligand-Target Pair

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Mitogen-activated protein kinase 1(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM418018(US10457669, Example 697 | US11001575, Example 697)

IC50: 2nMAssay Description:Inhibition of full-length human N-terminal MAHHHHHH tagged-ERK2 expressed in Escherichia coli BL21 (DE3) using ATF2-GFP as substrate incubated for 30...More data for this Ligand-Target Pair

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3D Structure (crystal)

Platelet-activating factor acetylhydrolase(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM50182421(CHEMBL3817896)

IC50: 2.40nMAssay Description:Inhibition of human recombinant Lp-PLA2 using 2-thio-PAF as substrate after 20 mins by CPM-based fluorescence assayMore data for this Ligand-Target Pair

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Mitogen-activated protein kinase 1(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM50573872(CHEMBL4868536)

IC50: 2.60nMAssay Description:Inhibition of full-length human N-terminal MAHHHHHH tagged-ERK2 expressed in Escherichia coli BL21 (DE3) using ATF2-GFP as substrate incubated for 30...More data for this Ligand-Target Pair

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Mitogen-activated protein kinase 1(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM418007(US10457669, Example 1083 | US10457669, Example 685...)

IC50: 2.70nMAssay Description:Inhibition of full-length human N-terminal MAHHHHHH tagged-ERK2 expressed in Escherichia coli BL21 (DE3) using ATF2-GFP as substrate incubated for 30...More data for this Ligand-Target Pair

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3D Structure (crystal)

Mitogen-activated protein kinase 1(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM418315((2R)-2-(3-{5-chloro-2-[(oxan-4- yl)amino]pyrimidin...)

IC50: 2.80nMAssay Description:Inhibition of full-length human N-terminal MAHHHHHH tagged-ERK2 expressed in Escherichia coli BL21 (DE3) using ATF2-GFP as substrate incubated for 30...More data for this Ligand-Target Pair

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Mitogen-activated protein kinase 1(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM50456348(CHEMBL4212211 | US11001575, Example 683)

IC50: 3nMAssay Description:Inhibition of full-length human N-terminal MAHHHHHH tagged-ERK2 expressed in Escherichia coli BL21 (DE3) using ATF2-GFP as substrate incubated for 30...More data for this Ligand-Target Pair

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3D Structure (crystal)

Mitogen-activated protein kinase 1(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM418226((2R)-2-(6-{5-chloro-2-[(oxan-4- yl)amino]pyrimidin...)

IC50: 3.10nMAssay Description:Inhibition of full-length human N-terminal MAHHHHHH tagged-ERK2 expressed in Escherichia coli BL21 (DE3) using ATF2-GFP as substrate incubated for 30...More data for this Ligand-Target Pair

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3D Structure (crystal)

Discoidin domain-containing receptor 2(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM50112617(CHEMBL3608786)

IC50: 3.30nMAssay Description:Inhibition of DDR2 (unknown origin) after 1 hr by time resolved fluorescence methodMore data for this Ligand-Target Pair

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3D Structure (crystal)

Mitogen-activated protein kinase 1(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM50573873(CHEMBL4870176)

IC50: 3.5nMAssay Description:Inhibition of full-length human N-terminal MAHHHHHH tagged-ERK2 expressed in Escherichia coli BL21 (DE3) using ATF2-GFP as substrate incubated for 30...More data for this Ligand-Target Pair

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Platelet-activating factor acetylhydrolase(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM50182420(CHEMBL3819600)

IC50: 3.60nMAssay Description:Inhibition of human recombinant Lp-PLA2 using 2-thio-PAF as substrate after 20 mins by CPM-based fluorescence assayMore data for this Ligand-Target Pair

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Discoidin domain-containing receptor 2(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM50112628(CHEMBL3608789)

IC50: 4.5nMAssay Description:Inhibition of DDR2 (unknown origin) after 1 hr by time resolved fluorescence methodMore data for this Ligand-Target Pair

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Discoidin domain-containing receptor 2(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM50112631(CHEMBL3608790)

IC50: 5.80nMAssay Description:Inhibition of DDR2 (unknown origin) after 1 hr by time resolved fluorescence methodMore data for this Ligand-Target Pair

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Mitogen-activated protein kinase 1(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM417431(6-{5-chloro-2-[(oxan-4- yl)amino]pyrimidin-4- yl}-...)

IC50: 5.80nMAssay Description:Inhibition of full-length human N-terminal MAHHHHHH tagged-ERK2 expressed in Escherichia coli BL21 (DE3) using ATF2-GFP as substrate incubated for 30...More data for this Ligand-Target Pair

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3D Structure (crystal)

Epithelial discoidin domain-containing receptor 1(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM50112618(CHEMBL3608787)

IC50: 6nMAssay Description:Inhibition of DDR1 (unknown origin) after 1 hr by time resolved fluorescence methodMore data for this Ligand-Target Pair

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Discoidin domain-containing receptor 2(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM50112634(CHEMBL3608791)

IC50: 6.10nMAssay Description:Inhibition of DDR2 (unknown origin) after 1 hr by time resolved fluorescence methodMore data for this Ligand-Target Pair

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Maternal embryonic leucine zipper kinase(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM50043378(CHEMBL3355064)

IC50: 7.60nMAssay Description:Inhibition of MELK (unknown origin) using KKLNRTLSFAEPG substrate by Millipore/scintillation counting analysisMore data for this Ligand-Target Pair

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Discoidin domain-containing receptor 2(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM50112618(CHEMBL3608787)

IC50: 8.10nMAssay Description:Inhibition of DDR2 (unknown origin) after 1 hr by time resolved fluorescence methodMore data for this Ligand-Target Pair

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Discoidin domain-containing receptor 2(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM50112615(CHEMBL3608785)

IC50: 8.20nMAssay Description:Inhibition of DDR2 (unknown origin) after 1 hr by time resolved fluorescence methodMore data for this Ligand-Target Pair

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Platelet-activating factor acetylhydrolase(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM50182419(CHEMBL3819444)

IC50: 9.5nMAssay Description:Inhibition of human recombinant Lp-PLA2 using 2-thio-PAF as substrate after 20 mins by CPM-based fluorescence assayMore data for this Ligand-Target Pair

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Mast/stem cell growth factor receptor Kit(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM50112615(CHEMBL3608785)

IC50: 9.80nMAssay Description:Inhibition of c-Kit (unknown origin) using biotinylated HER2 peptide as substrate by time resolved fluorescence methodMore data for this Ligand-Target Pair

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Proto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM50043380(CHEMBL3355065)

IC50: 10nMAssay Description:Inhibition of RET (unknown origin)More data for this Ligand-Target Pair

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Kelch-like ECH-associated protein 1(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM304727(3-(7-methoxy-1-methyl-1H-benzo[d][1,2,3]triazol-5-...)

IC50: 10nMAssay Description:Displacement of 5'-TAMRA-labelled NRF2 peptide from human N-terminal His6-tagged KEAP1 Kelch domain (321 to 609 residues) expressed in baculovirus in...More data for this Ligand-Target Pair

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Mitogen-activated protein kinase 1(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM418281((2R)-2-[6-(5-chloro-2-{[(2S)-1- hydroxypropan-2-yl...)

IC50: 12nMAssay Description:Inhibition of full-length human N-terminal MAHHHHHH tagged-ERK2 expressed in Escherichia coli BL21 (DE3) using ATF2-GFP as substrate incubated for 30...More data for this Ligand-Target Pair

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Mitogen-activated protein kinase 1(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM417432(6-{5-chloro-2-[(oxan-4- yl)amino]pyrimidin-4- yl}-...)

IC50: 14nMAssay Description:Inhibition of full-length human N-terminal MAHHHHHH tagged-ERK2 expressed in Escherichia coli BL21 (DE3) using ATF2-GFP as substrate incubated for 30...More data for this Ligand-Target Pair

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3D Structure (crystal)

Platelet-activating factor acetylhydrolase(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM50182422(CHEMBL3818650)

IC50: 18nMAssay Description:Inhibition of Lp-PLA2 in human whole plasma using 2-thio-PAF as substrate preincubated for 15 mins followed by substrate addition measured after 3 mi...More data for this Ligand-Target Pair

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3D Structure (crystal)

Maternal embryonic leucine zipper kinase(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM50043380(CHEMBL3355065)

IC50: 19nMAssay Description:Inhibition of MELK (unknown origin) using KKLNRTLSFAEPG substrate by Millipore/scintillation counting analysisMore data for this Ligand-Target Pair

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Mast/stem cell growth factor receptor Kit(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM50112617(CHEMBL3608786)

IC50: 19nMAssay Description:Inhibition of c-Kit (unknown origin) using biotinylated HER2 peptide as substrate by time resolved fluorescence methodMore data for this Ligand-Target Pair

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Vascular endothelial growth factor receptor 1(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM50043380(CHEMBL3355065)

IC50: 20nMAssay Description:Inhibition of Flt1 (unknown origin)More data for this Ligand-Target Pair

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Maternal embryonic leucine zipper kinase(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM50043380(CHEMBL3355065)

IC50: 20nMAssay Description:Inhibition of MELK (unknown origin)More data for this Ligand-Target Pair

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Kelch-like ECH-associated protein 1(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM304721(3-(7-methoxy-1-methyl-1H-benzo[d][1,2,3]triazol-5-...)

IC50: 20nMAssay Description:Displacement of 5'-TAMRA-labelled NRF2 peptide from human N-terminal His6-tagged KEAP1 Kelch domain (321 to 609 residues) expressed in baculovirus in...More data for this Ligand-Target Pair

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3D Structure (crystal)

Kelch-like ECH-associated protein 1(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM304748(BDBM304749 | US10144731, Example 34a)

IC50: 24nMAssay Description:Displacement of 5'-TAMRA-labelled NRF2 peptide from human N-terminal His6-tagged KEAP1 Kelch domain (321 to 609 residues) expressed in baculovirus in...More data for this Ligand-Target Pair

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Mitogen-activated protein kinase 1(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM417517(N-benzyl-2-(6-{5-chloro- 2-[(oxan-4-yl)amino] pyri...)

IC50: 25nMAssay Description:Inhibition of full-length human N-terminal MAHHHHHH tagged-ERK2 expressed in Escherichia coli BL21 (DE3) using ATF2-GFP as substrate incubated for 30...More data for this Ligand-Target Pair

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Mitogen-activated protein kinase 1(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM50456358(CHEMBL4213466 | US11001575, Example 77)

IC50: 26nMAssay Description:Inhibition of full-length human N-terminal MAHHHHHH tagged-ERK2 expressed in Escherichia coli BL21 (DE3) using ATF2-GFP as substrate incubated for 30...More data for this Ligand-Target Pair

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Platelet-activating factor acetylhydrolase(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM50182421(CHEMBL3817896)

IC50: 28nMAssay Description:Inhibition of Lp-PLA2 in human whole plasma using 2-thio-PAF as substrate preincubated for 15 mins followed by substrate addition measured after 3 mi...More data for this Ligand-Target Pair

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Tyrosine-protein kinase Yes(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM50043380(CHEMBL3355065)

IC50: 30nMAssay Description:Inhibition of Yes1 (unknown origin)More data for this Ligand-Target Pair

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Vascular endothelial growth factor receptor 3(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM50043380(CHEMBL3355065)

IC50: 30nMAssay Description:Inhibition of Flt4 (unknown origin)More data for this Ligand-Target Pair

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Platelet-activating factor acetylhydrolase(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM50197673(CHEMBL3922315)

IC50: 32nMAssay Description:Inhibition of Lp-PLA2 in whole human plasma pre-incubated for 15 mins before 2-thio-PAF substrate additionMore data for this Ligand-Target Pair

PDB MMDB NCI pathway Reactome pathway KEGG
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3D Structure (crystal)

Platelet-activating factor acetylhydrolase(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL

PNG

BDBM50125265(CHEMBL204021 | N-(2-Diethylamino-ethyl)-2-[2-(4-fl...)

IC50: 35nMAssay Description:Inhibition of Lp-PLA2 in human whole plasma using 2-thio-PAF as substrate preincubated for 15 mins followed by substrate addition measured after 3 mi...More data for this Ligand-Target Pair

PDB MMDB NCI pathway Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD DrugBank antibodypedia GoogleScholar

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PC cid PC sid PDB Patents Similars

Details Article PubMed PDB

3D Structure (crystal)

Displayed 1 to 50 (of 229 total ) | Next | Last >>

Filter my 229 hits

Targets 25▿
- Platelet-activating factor acetylhydrolase 76
- Kelch-like ECH-associated protein 1 31
- Heat shock protein HSP 90-alpha/90-beta 29
- Maternal embryonic leucine zipper kinase 19
- Mitogen-activated protein kinase 1 18
- Nuclear factor erythroid 2-related factor 2 15
- Discoidin domain-containing receptor 2 11
- Mast/stem cell growth factor receptor Kit 6
- Epithelial discoidin domain-containing receptor 1 4
- Cytochrome P450 3A4 4
- Receptor-type tyrosine-protein kinase FLT3 2
- Calcium/calmodulin-dependent protein kinase type II subunit delta 1
- Macrophage colony-stimulating factor 1 receptor 1
- Solute carrier organic anion transporter family member 1B1 1
- Calcium/calmodulin-dependent protein kinase type II subunit gamma 1
- MAP kinase-interacting serine/threonine-protein kinase 2 1
- cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A 1
- Proto-oncogene tyrosine-protein kinase receptor Ret 1
- Tyrosine-protein kinase Yes 1
- Myosin light chain kinase, smooth muscle 1
- BDNF/NT-3 growth factors receptor 1
- Fibroblast growth factor receptor 1 1
- Vascular endothelial growth factor receptor 3 1
- Bile salt export pump 1
- Vascular endothelial growth factor receptor 1 1
- ...
Publications 9▿
- J Med Chem 59: 10738-10749 (2016) 55
- J Med Chem 62: 4683-4702 (2019) 33
- J Med Chem 53: 5942-55 (2010) 29
- J Med Chem 59: 5356-67 (2016) 25
- ACS Med Chem Lett 6: 798-803 (2015) 20
- ACS Med Chem Lett 6: 31-6 (2015) 20
- J Med Chem 64: 12286-12303 (2021) 18
- J Med Chem 59: 3991-4006 (2016) 16
- ACS Med Chem Lett 6: 25-30 (2015) 13
Institutions 2▿
- Astex Pharmaceuticals 200
- Astex Therapeutics 29
Affinity: 0.035 to 3.4E+6 nM▿
- IC50 175
- Kd 38
- EC50 16
- Affinity ≤ nM
Xtal structures: 48
Docked structures: 0
Catalog Cmpds: 26