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Found 41 Enz. Inhib. hit(s) for PDB: 5N66
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataKi:  0.100nMAssay Description:Inhibition of p38alphaMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataKi:  6.40nMAssay Description:Displacement of rhodamine-green labeled (2-(6-amino-3-imino-3H-xanthen-9-yl)-5-{[({4-[4-(4-Cl-3-hydroxyphenyl)-5-(4-pyridinyl)-1H-imidazol-2yl]phenyl...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataKi:  22nMAssay Description:Binding affinity to full-length GST-tagged p38alpha after 2.5 hrs by TR-FRET competition binding assayMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataIC50:  0.100nMAssay Description:Inhibition of p38alpha (unknown origin)More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataIC50:  4nMAssay Description:Inhibition of human recombinant full-length N-terminal GST-tagged p38alpha expressed in Escherichia coli by radiometric kinase assayMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 11/12/13/14(Homo sapiens (Human))
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataIC50:  8nMAssay Description:Inhibition of human p38-MAPKMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataIC50:  8nMAssay Description:Inhibition of N-terminus His-tagged human p38alpha expressed in Escherichia coli BL21 DE3 using GST-tagged ATF2 as substrate after 90 mins by HTRF as...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 11/12/13/14(Homo sapiens (Human))
Vu University Amsterdam

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataIC50:  9nMAssay Description:Inhibition of MAPK p38More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataIC50:  10nMAssay Description:Inhibition of human recombinant P38alpha-mediated ATF2 phosphorylation after 1 hrMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataIC50:  12nMT: 2°CAssay Description:The enzyme inhibitory activity of compound was determined by FRET using synthetic peptides labelled with both donor and acceptor fluorophores (Z-LY...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataIC50:  12nMAssay Description:The enzyme inhibitory activities of compounds disclosed herein were determined by fluorescence resonance energy transfer (FRET) using synthetic pepti...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataIC50:  12nMAssay Description:The enzyme inhibitory activity of test compounds was determined by fluorescence resonance energy transfer (FRET) using synthetic peptides labelled wi...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataIC50:  17nMAssay Description:Inhibition of phospho-p38 alpha activity by ELISAMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataIC50:  17nMAssay Description:Inhibition of human p38-alpha kinase phosphorylationMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataIC50:  20nMAssay Description:Inhibition of P38alphaMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataIC50:  20nMAssay Description:Inhibition of human recombinant p38 alpha assessed as phosphorylation of MAPKAP-K2 preincubated for 2 hrs followed by FRET peptide and MAPKAP-K2 addi...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataIC50:  44nMAssay Description:Inhibition of p38 alpha activity by ELISAMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataIC50:  44nMAssay Description:Inhibition of human p38-alpha kinaseMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataIC50:  47nMAssay Description:Inhibition of p38alpha phosphorylation in IL1alpha-stimulated HLF cellsMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataIC50:  89nMAssay Description:Inhibition of p38 alphaMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataIC50:  220nMAssay Description:Displacemnt of N,N'-(2,2'-(3,3'-disulfanediylbis(2,5-dioxopyrrolidine-3,1-diyl))bis(ethane-2,1-diyl))bis(2-(3-(3-tert-butyl-5-(3-naphthalen-1-ylureid...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataIC50:  250nMAssay Description:Inhibition of p38alpha active form expressed in Escherichia coli BL21(DE3) cells by HTRF assayMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataKd:  1nMAssay Description:Binding affinity to wild type human biotin labelled p38 alpha (9 to 352 residues) expressed in sf21 insect cells assessed as dissociation rate consta...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataKd:  0.123nMAssay Description:Binding affinity to wild type human biotin labelled p38 alpha (9 to 352 residues) expressed in sf21 insect cells SPR analysisMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataKd:  12nMAssay Description:Binding affinity to p38alpha MAP kinase (unknown origin) by FLiK assayMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for TGFBR1 kinase domainMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataKd:  0.370nMAssay Description:Binding constant for full-length p38-alphaMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataKon:  0.00000800M-1s-1Assay Description:Rate of dissociation from Mitogen-activated protein kinase p38 alphaMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataKoff:  8.49E+4s-1Assay Description:Rate of association to Mitogen-activated protein kinase p38 alphaMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataKd:  7.5nMAssay Description:Binding affinity to N-terminus His-tagged human p38alpha expressed in Escherichia coli BL21 DE3 after 5 hrs by fluorescence analysisMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataKd:  1nMAssay Description:Binding affinity to p38alpha MAPK by surface plasmon resonance methodMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for TGFBR1 kinase domainMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataKd:  0.450nMAssay Description:Binding constant for p38-alpha kinase domainMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataKd:  0.160nMAssay Description:Inhibition of p38alphaMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataKd:  0.0980nMAssay Description:Binding affinity to full-length GST-tagged p38alpha by surface plasmon resonance assayMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataKd:  0.100nMAssay Description:Binding affinity to p38alpha (unknown origin) by exchange curve binding kinetic analysisMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataKd:  0.240nMAssay Description:Average Binding Constant for p38-alpha; NA=Not Active at 10 uMMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataKd:  0.0980nMAssay Description:Binding affinity for Mitogen-activated protein kinase p38 alphaMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Mus musculus (mouse))
Boehringer Ingelheim Pharmaceuticals

LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataKd:  0.0460nMpH: 7.0 T: 2°CAssay Description:UV thermal melt experiments were carried out in a quartz cuvette loaded with sample containing enzyme and each test compound using a spectrophotomete...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataKd:  0.100nMpH: 7.0 T: 2°CAssay Description:The exchange curve assays were run as two half-reactions using an SLM Aminco Bowman Series 2 model SQ-340 fluorescence detector. In the first half re...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM13533(1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3...)
Affinity DataKd:  0.100nMpH: 7.0 T: 2°CAssay Description:The exchange curve assays were run as two half-reactions using an SLM Aminco Bowman Series 2 model SQ-340 fluorescence detector. In the first half re...More data for this Ligand-Target Pair