BDBM276743 US10071991, Compound (P)::US10800764, Compound (P)::US11214566, Compound (P)::US9611259, Compound (P)

SMILES CC1(C)CCC(=CC1)c1nc(ccc1NC(=O)c1nc(c[nH]1)C#N)C1CC(C)(C)OC(C)(C)C1

InChI Key InChIKey=BNVPFDRNGHMRJS-UHFFFAOYSA-N

Data  16 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 23 hits for monomerid = 276743   

LigandPNGBDBM276743(US10071991, Compound (P) | US9611259, Compound (P)...)
Affinity DataIC50: 3.20nMAssay Description:Inhibition of CSF1-induced CSF1R signalling in mouse BMDM cells assessed as reduction in ERK1/2 phosphorylation preincubated for 30 mins followed by ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetMacrophage colony-stimulating factor 1 receptor(Human)
University of Sharjah

Curated by ChEMBL
LigandPNGBDBM276743(US10071991, Compound (P) | US9611259, Compound (P)...)
Affinity DataIC50: 3.20nMAssay Description:Inhibition of CSF1R (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/16/2020
Entry Details Article
PubMed
TargetMacrophage colony-stimulating factor 1 receptor(Human)
University of Sharjah

Curated by ChEMBL
LigandPNGBDBM276743(US10071991, Compound (P) | US9611259, Compound (P)...)
Affinity DataIC50: 3.20nMAssay Description:Inhibition of human CSF1R using pEY as substrate incubated for 40 mins in presence of [gamma33P]-ATP by scintillation countingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetMacrophage colony-stimulating factor 1 receptor(Human)
University of Sharjah

Curated by ChEMBL
LigandPNGBDBM276743(US10071991, Compound (P) | US9611259, Compound (P)...)
Affinity DataIC50: 3.20nMAssay Description:Inhibition of CSF1R (unknown origin) (538 to 972 residues) expressed in baculovirus expression system using SYEGNSYTFIDPTQ as substrate incubated for...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/20/2022
Entry Details Article
PubMed
TargetMacrophage colony-stimulating factor 1 receptor(Human)
University of Sharjah

Curated by ChEMBL
LigandPNGBDBM276743(US10071991, Compound (P) | US9611259, Compound (P)...)
Affinity DataIC50: 10nMAssay Description:In this assay, recombinant human, dog or rat c-fms catalyzed the phosphorylation of the FMS peptide substrate, SYEGNSYTFIDPTQ, with the phosphorylate...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/8/2022
Entry Details
US Patent

TargetMacrophage colony-stimulating factor 1 receptor(Human)
University of Sharjah

Curated by ChEMBL
LigandPNGBDBM276743(US10071991, Compound (P) | US9611259, Compound (P)...)
Affinity DataIC50: 10nMAssay Description:Materials:Human c-fms protein (N-terminal 6His-tagged, amino acids 538-972), dog c-fms protein (N-terminal 6His-tagged, amino acids 535-967) and rat ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/1/2021
Entry Details
US Patent

TargetMacrophage colony-stimulating factor 1 receptor(Human)
University of Sharjah

Curated by ChEMBL
LigandPNGBDBM276743(US10071991, Compound (P) | US9611259, Compound (P)...)
Affinity DataIC50: 10nMpH: 7.0 T: 2°CAssay Description:In this assay, recombinant human, dog or rat c-fms catalyzed the phosphorylation of the FMS peptide substrate, SYEGNSYTFIDPTQ, with the phosphorylate...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/21/2018
Entry Details
US Patent

TargetMacrophage colony-stimulating factor 1 receptor(Rat)
Janssen Pharmaceutica

US Patent
LigandPNGBDBM276743(US10071991, Compound (P) | US9611259, Compound (P)...)
Affinity DataIC50: 11nMpH: 7.0 T: 2°CAssay Description:In this assay, recombinant human, dog or rat c-fms catalyzed the phosphorylation of the FMS peptide substrate, SYEGNSYTFIDPTQ, with the phosphorylate...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/21/2018
Entry Details
US Patent

TargetMacrophage colony-stimulating factor 1 receptor(Rat)
Janssen Pharmaceutica

US Patent
LigandPNGBDBM276743(US10071991, Compound (P) | US9611259, Compound (P)...)
Affinity DataIC50: 11nMAssay Description:In this assay, recombinant human, dog or rat c-fms catalyzed the phosphorylation of the FMS peptide substrate, SYEGNSYTFIDPTQ, with the phosphorylate...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/8/2022
Entry Details
US Patent

TargetMacrophage colony-stimulating factor 1 receptor(Rat)
Janssen Pharmaceutica

US Patent
LigandPNGBDBM276743(US10071991, Compound (P) | US9611259, Compound (P)...)
Affinity DataIC50: 11nMAssay Description:Materials:Human c-fms protein (N-terminal 6His-tagged, amino acids 538-972), dog c-fms protein (N-terminal 6His-tagged, amino acids 535-967) and rat ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/1/2021
Entry Details
US Patent

TargetColony stimulating factor 1 receptor(Dog)
Janssen Pharmaceutica

US Patent
LigandPNGBDBM276743(US10071991, Compound (P) | US9611259, Compound (P)...)
Affinity DataIC50: 16nMpH: 7.0 T: 2°CAssay Description:In this assay, recombinant human, dog or rat c-fms catalyzed the phosphorylation of the FMS peptide substrate, SYEGNSYTFIDPTQ, with the phosphorylate...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/21/2018
Entry Details
US Patent

TargetReceptor protein-tyrosine kinase(Dog)
Janssen Pharmaceutica

US Patent
LigandPNGBDBM276743(US10071991, Compound (P) | US9611259, Compound (P)...)
Affinity DataIC50: 16nMAssay Description:In this assay, recombinant human, dog or rat c-fms catalyzed the phosphorylation of the FMS peptide substrate, SYEGNSYTFIDPTQ, with the phosphorylate...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/8/2022
Entry Details
US Patent

TargetReceptor protein-tyrosine kinase(Dog)
Janssen Pharmaceutica

US Patent
LigandPNGBDBM276743(US10071991, Compound (P) | US9611259, Compound (P)...)
Affinity DataIC50: 16nMAssay Description:Materials:Human c-fms protein (N-terminal 6His-tagged, amino acids 538-972), dog c-fms protein (N-terminal 6His-tagged, amino acids 535-967) and rat ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/1/2021
Entry Details
US Patent

TargetMacrophage colony-stimulating factor 1 receptor(Human)
University of Sharjah

Curated by ChEMBL
LigandPNGBDBM276743(US10071991, Compound (P) | US9611259, Compound (P)...)
Affinity DataIC50: 18nMAssay Description:c-fms(h) was incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 250 μM KKKSPGEYVNIEFG, 10 mM MgAcetate and [γ-33P-ATP] (specific activity approx...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/29/2019
Entry Details
US Patent

TargetMacrophage colony-stimulating factor 1 receptor(Human)
University of Sharjah

Curated by ChEMBL
LigandPNGBDBM276743(US10071991, Compound (P) | US9611259, Compound (P)...)
Affinity DataIC50: 18nMpH: 7.0 T: 2°CAssay Description:c-fms(h) was incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 250 μM KKKSPGEYVNIEFG, 10 mM MgAcetate and [γ-33P-ATP] (specific activity approx...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/21/2018
Entry Details
US Patent

TargetMacrophage colony-stimulating factor 1 receptor(Human)
University of Sharjah

Curated by ChEMBL
LigandPNGBDBM276743(US10071991, Compound (P) | US9611259, Compound (P)...)
Affinity DataIC50: 18nMAssay Description:c-fms(h) was incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 250 μM KKKSPGEYVNIEFG, 10 mM MgAcetate and [γ-33P-ATP] (specific activity approx...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/8/2022
Entry Details
US Patent

TargetMacrophage colony-stimulating factor 1 receptor(Human)
University of Sharjah

Curated by ChEMBL
LigandPNGBDBM276743(US10071991, Compound (P) | US9611259, Compound (P)...)
Affinity DataIC50: 18nMAssay Description:c-fms(h) was incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 250 μM KKKSPGEYVNIEFG, 10 mM MgAcetate and [γ-33P-ATP] (specific activity approx...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/1/2021
Entry Details
US Patent

LigandPNGBDBM276743(US10071991, Compound (P) | US9611259, Compound (P)...)
Affinity DataIC50: 20nMAssay Description:Inhibition of KIT (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM276743(US10071991, Compound (P) | US9611259, Compound (P)...)
Affinity DataIC50: 20nMAssay Description:Inhibition of c-KIT (unknown origin) using TK as substrate incubated for 50 mins in presence of ATP by HTRF methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM276743(US10071991, Compound (P) | US9611259, Compound (P)...)
Affinity DataIC50: 190nMAssay Description:Inhibition of FLT3 (unknown origin) by enzymatic assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM276743(US10071991, Compound (P) | US9611259, Compound (P)...)
Affinity DataIC50: 190nMAssay Description:Inhibition of FLT3-ITD mutant phosphorylation in human HEK-293T cells incubated for 2 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM276743(US10071991, Compound (P) | US9611259, Compound (P)...)
Affinity DataIC50: 1.00E+3nMAssay Description:Inhibition of CSF-1R autophosphorylation in mouse RAW264.7 cells preincubated for 6 hrs followed by CSF-1 addition and measured after 20 mins by ELIS...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetMacrophage colony-stimulating factor 1 receptor(Human)
University of Sharjah

Curated by ChEMBL
LigandPNGBDBM276743(US10071991, Compound (P) | US9611259, Compound (P)...)
Affinity DataIC50: 1.25E+3nMAssay Description:Representative compounds of the present invention were additionally tested in an in vitro assay measuring inhibition of CSF-1 induced monocyte MCP-1 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/1/2021
Entry Details
US Patent