BDBM264139 4-(3-(R)-(5-Chloro-1,3-dioxo-1H-pyrido[1,2-c]pyrimidin-2(3H)-yl)-2-methylphenyl)-7-(2-hydroxypropan-2-yl)-9H-carbazole-1-carboxamide (14), and::US9714234, 14

SMILES Cc1c(cccc1-n1c(=O)cc2c(Cl)cccn2c1=O)-c1ccc(C(N)=O)c2[nH]c3cc(ccc3c12)C(C)(C)O

InChI Key InChIKey=RXHAROKPHMWUME-UHFFFAOYSA-N

Data  11 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 11 hits for monomerid = 264139   

TargetTyrosine-protein kinase BTK(Human)
Bristol Myers Squibb Research

Curated by ChEMBL
LigandPNGBDBM264139(4-(3-(R)-(5-Chloro-1,3-dioxo-1H-pyrido[1,2-c]pyrim...)
Affinity DataIC50: 0.940nMAssay Description:Inhibition of recombinant full-length His-tagged human BTK expressed in baculovirus expression system using fluoresceinated peptide as substrate incu...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/22/2022
Entry Details Article
PubMed
TargetTyrosine-protein kinase BTK(Human)
Bristol Myers Squibb Research

Curated by ChEMBL
LigandPNGBDBM264139(4-(3-(R)-(5-Chloro-1,3-dioxo-1H-pyrido[1,2-c]pyrim...)
Affinity DataIC50: 1nMAssay Description:Inhibition of recombinant full-length His-tagged human BTK expressed in baculovirus expression system using fluoresceinated peptide as substrate incu...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/22/2022
Entry Details Article
PubMed
TargetTyrosine-protein kinase BTK(Human)
Bristol Myers Squibb Research

Curated by ChEMBL
LigandPNGBDBM264139(4-(3-(R)-(5-Chloro-1,3-dioxo-1H-pyrido[1,2-c]pyrim...)
Affinity DataIC50: 1nMAssay Description:Inhibition of recombinant full-length His-tagged human BTK expressed in baculovirus expression system using fluoresceinated peptide as substrate incu...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/22/2022
Entry Details Article
PubMed
TargetTyrosine-protein kinase BTK(Human)
Bristol Myers Squibb Research

Curated by ChEMBL
LigandPNGBDBM264139(4-(3-(R)-(5-Chloro-1,3-dioxo-1H-pyrido[1,2-c]pyrim...)
Affinity DataIC50: 1nMpH: 7.4 T: 2°CAssay Description:To V-bottom 384-well plates were added test compounds, human recombinant Btk (1 nM, INVITROGEN Corporation), fluoresceinated peptide (1.5 μM), A...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/15/2018
Entry Details
US Patent

TargetTyrosine-protein kinase BTK(Human)
Bristol Myers Squibb Research

Curated by ChEMBL
LigandPNGBDBM264139(4-(3-(R)-(5-Chloro-1,3-dioxo-1H-pyrido[1,2-c]pyrim...)
Affinity DataIC50: 12nMAssay Description:Inhibition of BTK in human Ramos B cells assessed as reduction in goat anti human IgM-stimulated calcium flux preincubated for 1 hr followed by goat ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/22/2022
Entry Details Article
PubMed
TargetTyrosine-protein kinase BTK(Human)
Bristol Myers Squibb Research

Curated by ChEMBL
LigandPNGBDBM264139(4-(3-(R)-(5-Chloro-1,3-dioxo-1H-pyrido[1,2-c]pyrim...)
Affinity DataIC50: 12nMAssay Description:Inhibition of BTK in human Ramos B cells assessed as reduction in goat anti human IgM-stimulated calcium flux preincubated for 1 hr followed by goat ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/22/2022
Entry Details Article
PubMed
TargetTyrosine-protein kinase BTK(Human)
Bristol Myers Squibb Research

Curated by ChEMBL
LigandPNGBDBM264139(4-(3-(R)-(5-Chloro-1,3-dioxo-1H-pyrido[1,2-c]pyrim...)
Affinity DataIC50: 13nMAssay Description:Inhibition of BTK in human Ramos B cells assessed as reduction in goat anti human IgM-stimulated calcium flux preincubated for 1 hr followed by goat ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/22/2022
Entry Details Article
PubMed
TargetTyrosine-protein kinase BTK(Human)
Bristol Myers Squibb Research

Curated by ChEMBL
LigandPNGBDBM264139(4-(3-(R)-(5-Chloro-1,3-dioxo-1H-pyrido[1,2-c]pyrim...)
Affinity DataIC50: 78nMAssay Description:Inhibition of BTK in human whole blood assessed as reduction in goat anti human IgM/human IL4-stimulated CD69 cell surface expression on peripheral B...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/22/2022
Entry Details Article
PubMed
TargetTyrosine-protein kinase BTK(Human)
Bristol Myers Squibb Research

Curated by ChEMBL
LigandPNGBDBM264139(4-(3-(R)-(5-Chloro-1,3-dioxo-1H-pyrido[1,2-c]pyrim...)
Affinity DataIC50: 120nMAssay Description:Inhibition of BTK in human whole blood assessed as reduction in goat anti human IgM/human IL4-stimulated CD69 cell surface expression on peripheral B...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/22/2022
Entry Details Article
PubMed
TargetTyrosine-protein kinase BTK(Human)
Bristol Myers Squibb Research

Curated by ChEMBL
LigandPNGBDBM264139(4-(3-(R)-(5-Chloro-1,3-dioxo-1H-pyrido[1,2-c]pyrim...)
Affinity DataIC50: 120nMAssay Description:Inhibition of BTK in human whole blood assessed as reduction in goat anti human IgM/human IL4-stimulated CD69 cell surface expression on peripheral B...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/22/2022
Entry Details Article
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Bristol-Myers Squibb

US Patent
LigandPNGBDBM264139(4-(3-(R)-(5-Chloro-1,3-dioxo-1H-pyrido[1,2-c]pyrim...)
Affinity DataIC50: 1.10E+3nMpH: 7.4 T: 2°CAssay Description:Compounds with activity against Jak2 tyrosine kinase have been observed to cause thrombocytopenia, anemia and neutropenia in human patients in clinic...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/15/2018
Entry Details
US Patent