BDBM377824 (R)-5-amino-3-(4-((5-chloro-3-fluoropyridin-2-yl)oxy)phenyl)-1-(1-cyanopiperidin-3-yl)-1H-pyrazole-4-carboxamide::US10266513, Example 118::US10815213, Example 118

SMILES NC(=O)c1c(N)n(nc1-c1ccc(Oc2ncc(Cl)cc2F)cc1)[C@@H]1CCCN(C1)C#N

InChI Key InChIKey=JJICHOVZOJORFF-CQSZACIVSA-N

Data  12 IC50

  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 12 hits for monomerid = 377824   

TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM377824((R)-5-amino-3-(4-((5-chloro-3-fluoropyridin-2-yl)o...)
Affinity DataIC50:  7.60nMAssay Description:TR-FRET LanthaScreen assays were performed by incubating a dilution series of inhibitor concentrations with 50 μM ATP, 100 nM FAM-Srctide peptid...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM377824((R)-5-amino-3-(4-((5-chloro-3-fluoropyridin-2-yl)o...)
Affinity DataIC50: >5.00E+4nMAssay Description:TR-FRET LanthaScreen assays were performed by incubating a dilution series of inhibitor concentrations with 20 μM ATP, 100 nM peptide substrate ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM377824((R)-5-amino-3-(4-((5-chloro-3-fluoropyridin-2-yl)o...)
Affinity DataIC50:  230nMAssay Description:Inhibition of full-length human C-terminal His6-tagged BTK C481S mutant expressed in Sf9 insect cells using FAM-Srctide peptide as substrate preincub...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM377824((R)-5-amino-3-(4-((5-chloro-3-fluoropyridin-2-yl)o...)
Affinity DataIC50: >2.00E+4nMAssay Description:Inhibition of human EGFR cytoplasmic domain expressed in baculovirus expression system using FITC-C6-KKAEEEEYFELVAKK-NH2 as substrate preincubated fo...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM377824((R)-5-amino-3-(4-((5-chloro-3-fluoropyridin-2-yl)o...)
Affinity DataIC50:  7.60nMAssay Description:Inhibition of full-length human His-tagged BTK expressed in baculovirus expression system using FAM-Srctide peptide as substrate preincubated for 1 h...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM377824((R)-5-amino-3-(4-((5-chloro-3-fluoropyridin-2-yl)o...)
Affinity DataIC50: >5.00E+4nMAssay Description:EGFR: TR-FRET LanthaScreen assays were performed by incubating a dilution series of inhibitor concentrations with 20 μM ATP, 100 nM peptide subs...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM377824((R)-5-amino-3-(4-((5-chloro-3-fluoropyridin-2-yl)o...)
Affinity DataIC50:  50nMAssay Description:Inhibition of BTK in human whole blood assessed as reduction in anti-human IgE antibody-stimulated histamine release pretreated for 2 hrs followed by...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetProto-oncogene tyrosine-protein kinase Src(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM377824((R)-5-amino-3-(4-((5-chloro-3-fluoropyridin-2-yl)o...)
Affinity DataIC50: >2.00E+4nMAssay Description:Inhibition of full-length recombinant human C-terminal His-tagged SRC cytoplasmic domain expressed in baculovirus expression system using FAM-Srctide...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM377824((R)-5-amino-3-(4-((5-chloro-3-fluoropyridin-2-yl)o...)
Affinity DataIC50:  19nMAssay Description:Inhibition of BTK in goat anti-human IgM F(ab')2-stimulated human B cells assessed as reduction in cell proliferation pretreated for 30 mins followed...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM377824((R)-5-amino-3-(4-((5-chloro-3-fluoropyridin-2-yl)o...)
Affinity DataIC50:  89nMAssay Description:Inhibition of BTK in goat anti-human IgM F(ab')2-stimulated human whole blood assessed as suppression of CD69 expression on B cells pretreated for 1 ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM377824((R)-5-amino-3-(4-((5-chloro-3-fluoropyridin-2-yl)o...)
Affinity DataIC50:  7.60nMAssay Description:BTK: TR-FRET LanthaScreen assays were performed by incubating a dilution series of inhibitor concentrations with 50 μM ATP, 100 nM FAM-Srctide p...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM377824((R)-5-amino-3-(4-((5-chloro-3-fluoropyridin-2-yl)o...)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of BTK in anti-CD3/CD28-stimulated human CD4-positive T cells assessed as reduction in cell proliferation pretreated for 30 mins followed ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed