BDBM142598 US10238658, Example Reference::US10813932, Reference Compound::US8933228, Ref 2::US9242960, 1::US9249125, Reference Compound::US9701670, Reference Compound::US9724347, Example Reference::US9993478, Example Reference

SMILES COCC(=O)Nc1cc(Oc2ccc(NC(=O)Nc3cc(nn3-c3ccc(C)cc3)C(C)(C)C)c3ccccc23)ccn1

InChI Key InChIKey=AVUUHIYJPTWYNX-UHFFFAOYSA-N

Data  32 IC50  21 Kd

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
   Substructure
Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 53 hits for monomerid = 142598   

TargetGlycogen synthase kinase-3 beta(Human)
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US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataKd:  24nMAssay Description:The inhibitory activities of compounds of the invention against c-Src and Syk enzymes (Invitrogen), were evaluated in a similar fashion to that descr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2019
Entry Details
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TargetGlycogen synthase kinase-3 alpha(Human)
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US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataIC50: 45nMAssay Description:GSK 3α: The enzyme inhibitory activities of compounds disclosed herein were determined by FRET using synthetic peptides labelled with both donor...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/5/2020
Entry Details
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TargetMitogen-activated protein kinase 14(Human)
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US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataIC50: 12nMAssay Description:p38 MAPKα: The enzyme inhibitory activities of compounds disclosed herein were determined by FRET using synthetic peptides labelled with both do...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/5/2020
Entry Details
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TargetMitogen-activated protein kinase 12(Human)
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US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataIC50: 344nMAssay Description:The inhibitory activities of compounds of the invention against p38MAPKγ (MAPK12: Invitrogen), were evaluated in a similar fashion to that descr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2019
Entry Details
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TargetMitogen-activated protein kinase 14(Human)
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US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataIC50: 12nMAssay Description:The inhibitory activities of test compounds against the p38 MAPKα isoform (MAPK14: Invitrogen), were evaluated indirectly by determining the lev...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2019
Entry Details
Go to US Patent

TargetGlycogen synthase kinase-3 alpha(Human)
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US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataIC50: 45nMAssay Description:The inhibitory activities of test compounds against the GSK 3α enzyme isoform (Invitrogen), were evaluated by determining the level of activatio...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2019
Entry Details
Go to US Patent

TargetProto-oncogene tyrosine-protein kinase Src(Human)
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US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataIC50: 5nMAssay Description:The inhibitory activities of compounds of the invention against c-Src and Syk enzymes (Invitrogen), were evaluated in a similar fashion to that descr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2019
Entry Details
Go to US Patent

TargetTyrosine-protein kinase SYK(Human)
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US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataIC50: 42nMAssay Description:The inhibitory activities of compounds of the invention against c-Src and Syk enzymes (Invitrogen), were evaluated in a similar fashion to that descr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2019
Entry Details
Go to US Patent

TargetMitogen-activated protein kinase 14(Human)
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US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataKd:  1nMAssay Description:The inhibitory activities of test compounds against the p38 MAPKα isoform (MAPK14: Invitrogen), were evaluated indirectly by determining the lev...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2019
Entry Details
Go to US Patent

TargetMitogen-activated protein kinase 12(Human)
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US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataKd:  5nMAssay Description:The inhibitory activities of compounds of the invention against p38MAPKγ (MAPK12: Invitrogen), were evaluated in a similar fashion to that descr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2019
Entry Details
Go to US Patent

TargetTyrosine-protein kinase HCK(Human)
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US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataKd:  5nMAssay Description:The inhibitory activities of compounds of the invention against c-Src and Syk enzymes (Invitrogen), were evaluated in a similar fashion to that descr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2019
Entry Details
Go to US Patent

TargetProto-oncogene tyrosine-protein kinase Src(Human)
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US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataKd:  4nMAssay Description:The inhibitory activities of compounds of the invention against c-Src and Syk enzymes (Invitrogen), were evaluated in a similar fashion to that descr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2019
Entry Details
Go to US Patent

TargetTyrosine-protein kinase SYK(Human)
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US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataKd:  9nMAssay Description:The inhibitory activities of compounds of the invention against c-Src and Syk enzymes (Invitrogen), were evaluated in a similar fashion to that descr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2019
Entry Details
Go to US Patent

TargetGlycogen synthase kinase-3 alpha(Human)
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US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataKd:  180nMAssay Description:The inhibitory activities of test compounds against the GSK 3α enzyme isoform (Invitrogen), were evaluated by determining the level of activatio...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2019
Entry Details
Go to US Patent

TargetMitogen-activated protein kinase 12(Human)
Respivert

US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataIC50: 344nMAssay Description:p38 MAPKγ: The enzyme inhibitory activities of compounds disclosed herein were determined by FRET using synthetic peptides labelled with both do...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/5/2020
Entry Details
Go to US Patent

TargetMitogen-activated protein kinase 14(Human)
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US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataIC50: 12nMAssay Description:p38 MAPKα: The inhibitory activities of test compounds against the p38 MAPKα isoform (MAPK14: Invitrogen), were evaluated indirectly by det...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/13/2021
Entry Details
Go to US Patent

TargetMitogen-activated protein kinase 12(Human)
Respivert

US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataIC50: 344nMAssay Description:p38 MAPKγ: The inhibitory activities of compounds of the invention against p38MAPKγ (MAPK12: Invitrogen), were evaluated in a similar fashi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/13/2021
Entry Details
Go to US Patent

TargetGlycogen synthase kinase-3 alpha(Human)
Respivert

US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataIC50: 45nMAssay Description:GSK 3α: The inhibitory activities of test compounds against the GSK 3α enzyme isoform (Invitrogen), were evaluated by determining the level...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/13/2021
Entry Details
Go to US Patent

TargetProto-oncogene tyrosine-protein kinase Src(Human)
Respivert

US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataIC50: 5nMAssay Description:c-Src and Syk: The inhibitory activities of compounds of the invention against c-Src and Syk enzymes (Invitrogen), were evaluated in a similar fashio...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/13/2021
Entry Details
Go to US Patent

TargetTyrosine-protein kinase SYK(Human)
Respivert

US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataIC50: 42nMAssay Description:c-Src and Syk: The inhibitory activities of compounds of the invention against c-Src and Syk enzymes (Invitrogen), were evaluated in a similar fashio...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/13/2021
Entry Details
Go to US Patent

TargetMitogen-activated protein kinase 14(Human)
Respivert

US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataKd:  1nMAssay Description:p38 MAPKα: The inhibitory activities of test compounds against the p38 MAPKα isoform (MAPK14: Invitrogen), were evaluated indirectly by det...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/13/2021
Entry Details
Go to US Patent

TargetMitogen-activated protein kinase 12(Human)
Respivert

US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataKd:  5nMAssay Description:p38 MAPKγ: The inhibitory activities of compounds of the invention against p38MAPKγ (MAPK12: Invitrogen), were evaluated in a similar fashi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/13/2021
Entry Details
Go to US Patent

TargetCysteine protease ATG4B(Human)
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US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
In Depth
Date in BDB:
6/13/2021
Entry Details
Go to US Patent

TargetProto-oncogene tyrosine-protein kinase Src(Human)
Respivert

US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataKd:  4nMAssay Description:c-Src and Syk: The inhibitory activities of compounds of the invention against c-Src and Syk enzymes (Invitrogen), were evaluated in a similar fashio...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/13/2021
Entry Details
Go to US Patent

TargetTyrosine-protein kinase SYK(Human)
Respivert

US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataKd:  9nMAssay Description:c-Src and Syk: The inhibitory activities of compounds of the invention against c-Src and Syk enzymes (Invitrogen), were evaluated in a similar fashio...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/13/2021
Entry Details
Go to US Patent

TargetGlycogen synthase kinase-3 alpha(Human)
Respivert

US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataKd:  180nMAssay Description:GSK 3α: The inhibitory activities of test compounds against the GSK 3α enzyme isoform (Invitrogen), were evaluated by determining the level...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/13/2021
Entry Details
Go to US Patent

TargetGlycogen synthase kinase-3 beta(Human)
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US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataKd:  24nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/13/2021
Entry Details
Go to US Patent

TargetGlycogen synthase kinase-3 alpha(Human)
Respivert

US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataIC50: 45nMAssay Description:The inhibitory activities of compounds of the invention against the GSK 3α enzyme isoform (Invitrogen), are evaluated by determining the level o...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
Go to US Patent

TargetMitogen-activated protein kinase 12(Human)
Respivert

US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataIC50: 344nMAssay 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
In Depth
Date in BDB:
6/8/2015
Entry Details
Go to US Patent

TargetTyrosine-protein kinase HCK(Human)
Respivert

US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataIC50: 3nMAssay 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
In Depth
Date in BDB:
6/8/2015
Entry Details
Go to US Patent

TargetProto-oncogene tyrosine-protein kinase Src(Human)
Respivert

US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataIC50: 5nMAssay 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
In Depth
Date in BDB:
6/8/2015
Entry Details
Go to US Patent

TargetProto-oncogene tyrosine-protein kinase Src(Human)
Respivert

US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataIC50: 5nMAssay Description:The inhibitory activities of compounds of the invention against c-Src and Syk enzymes (Invitrogen), are evaluated in a similar fashion to that descri...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/12/2016
Entry Details
Go to US Patent

TargetTyrosine-protein kinase SYK(Human)
Respivert

US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataIC50: 42nMAssay Description:The inhibitory activities of compounds of the invention against c-Src and Syk enzymes (Invitrogen), are evaluated in a similar fashion to that descri...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/12/2016
Entry Details
Go to US Patent

TargetGlycogen synthase kinase-3 alpha(Human)
Respivert

US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataIC50: 45nMAssay Description:The inhibitory activities of compounds of the invention against the GSK 3α enzyme isoform (Invitrogen), are evaluated by determining the level ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/12/2016
Entry Details
Go to US Patent

TargetMitogen-activated protein kinase 14(Human)
Respivert

US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
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-LYTE...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/28/2016
Entry Details
Go to US Patent

TargetMitogen-activated protein kinase 12(Human)
Respivert

US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataIC50: 344nMT: 2°CAssay Description:The enzyme inhibitory activity of compound was determined by FRET using synthetic peptides labelled with both donor and acceptor fluorophores (Z-LYTE...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/28/2016
Entry Details
Go to US Patent

TargetMitogen-activated protein kinase 14(Human)
Respivert

US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataIC50: 12nMAssay Description:The inhibitory activities of test compounds against the p38 MAPKα isoform (MAPK14: Invitrogen), are evaluated indirectly by determining the lev...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/12/2016
Entry Details
Go to US Patent

TargetMitogen-activated protein kinase 14(Human)
Respivert

US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataIC50: 12nMAssay Description:The inhibitory activities of test compounds against the p38 MAPKα isoform (MAPK14: Invitrogen), are evaluated indirectly by determining the leve...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
Go to US Patent

TargetProto-oncogene tyrosine-protein kinase Src(Human)
Respivert

US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataIC50: 5nMAssay Description:The inhibitory activities of compounds of the invention against c-Src and Syk enzymes (Invitrogen), are evaluated in a similar fashion to that descri...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
Go to US Patent

TargetTyrosine-protein kinase SYK(Human)
Respivert

US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataIC50: 42nMAssay Description:The inhibitory activities of compounds of the invention against Syk enzymes (Invitrogen), are evaluated in a similar fashion to that described herein...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/30/2018
Entry Details
Go to US Patent

TargetMitogen-activated protein kinase 14(Human)
Respivert

US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
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
In Depth
Date in BDB:
6/8/2015
Entry Details
Go to US Patent

Target5-hydroxytryptamine receptor 2A(Human)
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US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataIC50: 12nMAssay Description:The inhibitory activities of test compounds against the p38 MAPKα isoform (MAPK14: Invitrogen), were evaluated indirectly by determining the lev...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/12/2019
Entry Details
Go to US Patent

TargetMitogen-activated protein kinase 12(Human)
Respivert

US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataIC50: 344nMAssay Description:The inhibitory activities of compounds of the invention against p38MAPKγ (MAPK12: Invitrogen), were evaluated in a similar fashion to that descr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/12/2019
Entry Details
Go to US Patent

TargetGlycogen synthase kinase-3 alpha(Human)
Respivert

US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataIC50: 45nMAssay Description:The GSK3-α protein (500 ng/mL, 2.5 μL) was mixed with the test compound (2.5 μL at either 4 μg/mL, 0.4 μg/mL, 0.04 μg/m...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/12/2019
Entry Details
Go to US Patent

TargetProto-oncogene tyrosine-protein kinase Src(Human)
Respivert

US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataIC50: 5nMAssay Description:The inhibitory activities of compounds of the invention against c-Src and Syk enzymes (Invitrogen), were evaluated in a similar fashion to that descr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/12/2019
Entry Details
Go to US Patent

TargetTyrosine-protein kinase SYK(Human)
Respivert

US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataIC50: 42nMAssay Description:The inhibitory activities of compounds of the invention against c-Src and Syk enzymes (Invitrogen), were evaluated in a similar fashion to that descr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/12/2019
Entry Details
Go to US Patent

Target5-hydroxytryptamine receptor 2A(Human)
Respivert

US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataKd:  1nMAssay Description:The inhibitory activities of test compounds against the p38 MAPKα isoform (MAPK14: Invitrogen), were evaluated indirectly by determining the lev...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/12/2019
Entry Details
Go to US Patent

TargetMitogen-activated protein kinase 12(Human)
Respivert

US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataKd:  5nMAssay Description:The inhibitory activities of compounds of the invention against p38MAPKγ (MAPK12: Invitrogen), were evaluated in a similar fashion to that descr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/12/2019
Entry Details
Go to US Patent

TargetTyrosine-protein kinase HCK(Human)
Respivert

US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataKd:  5nMAssay Description:The inhibitory activities of compounds of the invention against c-Src and Syk enzymes (Invitrogen), were evaluated in a similar fashion to that descr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/12/2019
Entry Details
Go to US Patent

TargetProto-oncogene tyrosine-protein kinase Src(Human)
Respivert

US Patent
LigandPNGBDBM142598(US8933228, Ref 2 | US9249125, Reference Compound |...)
Affinity DataKd:  4nMAssay Description:The inhibitory activities of compounds of the invention against c-Src and Syk enzymes (Invitrogen), were evaluated in a similar fashion to that descr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/12/2019
Entry Details
Go to US Patent

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