BDBM267703 (R)-4-(8-amino-5-deutero-3-(1-(3-methoxypropanoyl) piperidin-3-yl)imidazo[1,5-a]pyrazin-1-yl)-N-(4-(trifluoromethyl)pyridin-2-yl)benzamide::US9718828, Example, 305

SMILES CC1(COC1)C(=O)N1CCC[C@H](C1)c1nc(-c2ccc(cc2)C(=O)Nc2cc(ccn2)C(F)(F)F)c2c(N)nccn12

InChI Key InChIKey=AHBFBRPGNOVEBK-LJQANCHMSA-N

Data  16 IC50  1 EC50

PDB links: 1 PDB ID matches this monomer.

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Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 17 hits for monomerid = 267703   

TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM267703((R)-4-(8-amino-5-deutero-3-(1-(3-methoxypropanoyl)...)
Affinity DataEC50: <10nMpH: 7.2 T: 2°CAssay Description:Btk enzyme activity is measured using the IMAP (immobilized metal ion affinity-based fluorescence polarization) assay as outlined below. Btk enzyme (...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
TargetTyrosine-protein kinase TXK(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM267703((R)-4-(8-amino-5-deutero-3-(1-(3-methoxypropanoyl)...)
Affinity DataIC50:  49nMAssay Description:Inhibition of human TXKMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM267703((R)-4-(8-amino-5-deutero-3-(1-(3-methoxypropanoyl)...)
Affinity DataIC50:  3.50E+3nMAssay Description:Inhibition of human ERG by [35S]-MK499 displacement or iKr channel assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM267703((R)-4-(8-amino-5-deutero-3-(1-(3-methoxypropanoyl)...)
Affinity DataIC50:  8nMAssay Description:Inhibition of BTK in human PBMC assessed as reduction in anti-IgM-induced MIP1betaMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM267703((R)-4-(8-amino-5-deutero-3-(1-(3-methoxypropanoyl)...)
Affinity DataIC50:  0.270nMAssay Description:Reversible inhibition of recombinant full length BTK (unknown origin) baculovirus infected Sf9 cells using biotinylated EQEDEPEGDYFEWLE-NH2 peptide a...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM267703((R)-4-(8-amino-5-deutero-3-(1-(3-methoxypropanoyl)...)
Affinity DataIC50:  8nMAssay Description:Inhibition of BTK in human PBMC assessed as reduction in cell surface CD69 expression preincubated for 1 hr followed by stimulation with goat anti-hu...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM267703((R)-4-(8-amino-5-deutero-3-(1-(3-methoxypropanoyl)...)
Affinity DataIC50:  120nMAssay Description:Inhibition of BTK in human whole blood assessed as reduction in cell surface CD69 expression preincubated for 1 hr followed by stimulation with anti-...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
TargetTyrosine-protein kinase Blk(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM267703((R)-4-(8-amino-5-deutero-3-(1-(3-methoxypropanoyl)...)
Affinity DataIC50:  84nMAssay Description:Inhibition of human BLKMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
TargetCytoplasmic tyrosine-protein kinase BMX(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM267703((R)-4-(8-amino-5-deutero-3-(1-(3-methoxypropanoyl)...)
Affinity DataIC50:  28nMAssay Description:Inhibition of human BMXMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-4(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM267703((R)-4-(8-amino-5-deutero-3-(1-(3-methoxypropanoyl)...)
Affinity DataIC50:  118nMAssay Description:Inhibition of human ERBB4More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase FRK(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM267703((R)-4-(8-amino-5-deutero-3-(1-(3-methoxypropanoyl)...)
Affinity DataIC50:  361nMAssay Description:Inhibition of human FRKMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase Lck(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM267703((R)-4-(8-amino-5-deutero-3-(1-(3-methoxypropanoyl)...)
Affinity DataIC50:  36nMAssay Description:Inhibition of human LCKMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase Lyn(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM267703((R)-4-(8-amino-5-deutero-3-(1-(3-methoxypropanoyl)...)
Affinity DataIC50:  399nMAssay Description:Inhibition of human LYNBMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
TargetProtein-tyrosine kinase 6(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM267703((R)-4-(8-amino-5-deutero-3-(1-(3-methoxypropanoyl)...)
Affinity DataIC50:  66nMAssay Description:Inhibition of human PTK6More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase Srms(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM267703((R)-4-(8-amino-5-deutero-3-(1-(3-methoxypropanoyl)...)
Affinity DataIC50:  32nMAssay Description:Inhibition of human SRMSMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase Tec(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM267703((R)-4-(8-amino-5-deutero-3-(1-(3-methoxypropanoyl)...)
Affinity DataIC50:  167nMAssay Description:Inhibition of human TECMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM267703((R)-4-(8-amino-5-deutero-3-(1-(3-methoxypropanoyl)...)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of recombinant full-length His6-tagged BTK (unknown origin) expressed in baculovirus infected Sf9 cells using biotinylated A5 peptide as s...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB