BDBM50076185 CHEMBL3416026::US9290481, 1.1

SMILES c1cc2cc[nH]c2c(c1)Nc3c(nnc(n3)N[C@@H]4CCCC[C@@H]4N)C(=O)N

InChI Key InChIKey=FPQNRXITKTZFMF-UHFFFAOYSA-N

Data  14 IC50  13 Kd

PDB links: 1 PDB ID matches this monomer.

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 27 hits for monomerid = 50076185   

TargetTyrosine-protein kinase JAK2(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50076185(CHEMBL3416026 | US9290481, 1.1)
Affinity DataKd:  53nMAssay Description:Competitive binding affinity to human JAK2More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2016
Entry Details Article
PubMed
TargetTyrosine-protein kinase SYK(Human)
Universita Degli Studi Di Palermo

Curated by ChEMBL
LigandPNGBDBM50076185(CHEMBL3416026 | US9290481, 1.1)
Affinity DataIC50: 14nMAssay Description:Inhibition of SYK in human Ramos cells assessed as reduction in anti IgM-induced phosphorylation of BLNK by flow cytometry assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase SYK(Human)
Universita Degli Studi Di Palermo

Curated by ChEMBL
LigandPNGBDBM50076185(CHEMBL3416026 | US9290481, 1.1)
Affinity DataIC50: 0.800nMAssay Description:Inhibition of human SYK using 5-Fluo-Ahx-GAPDYENLQELNKK-Amid as substrate in presence of ATP by microfluidic mobility shift assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase SYK(Human)
Universita Degli Studi Di Palermo

Curated by ChEMBL
LigandPNGBDBM50076185(CHEMBL3416026 | US9290481, 1.1)
Affinity DataIC50: 367nMAssay Description:Inhibition of Syk in anti-CD32 stimulated CD14+ human monocytes in presence of 90% human blood assessed as phospho-SLP76 level preincubated for 30 mi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/9/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase SYK(Human)
Universita Degli Studi Di Palermo

Curated by ChEMBL
LigandPNGBDBM50076185(CHEMBL3416026 | US9290481, 1.1)
Affinity DataIC50: 99nMAssay Description:Inhibition of Syk in anti-igM stimulated human Ramos B cells assessed as phospho-BLNK level preincubated for 30 mins followed by anti-IgM stimulation...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/9/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50076185(CHEMBL3416026 | US9290481, 1.1)
Affinity DataIC50: 2.80E+4nMAssay Description:Inhibition of human ERG by automated patch clamp assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/9/2016
Entry Details Article
PubMed
TargetTyrosine-protein kinase SYK(Human)
Universita Degli Studi Di Palermo

Curated by ChEMBL
LigandPNGBDBM50076185(CHEMBL3416026 | US9290481, 1.1)
Affinity DataIC50: 35nMAssay Description:Inhibition of Syk (unknown origin) using 5-Fluo-Ahx-GAPDYENLQELNKK-Amide as substrate after 60 mins by microfluidic mobility shift assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/9/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase SYK(Human)
Universita Degli Studi Di Palermo

Curated by ChEMBL
LigandPNGBDBM50076185(CHEMBL3416026 | US9290481, 1.1)
Affinity DataIC50: 35nMAssay Description:Inhibition of Syk (unknown origin) using 5-Fluo-Ahx-GAPDYENLQELNKK-Amide as substrate after 60 mins by microfluidic mobility shift assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase SYK(Human)
Universita Degli Studi Di Palermo

Curated by ChEMBL
LigandPNGBDBM50076185(CHEMBL3416026 | US9290481, 1.1)
Affinity DataIC50: 99nMAssay Description:Inhibition of Syk in anti-igM stimulated human Ramos B cells assessed as phospho-BLNK level preincubated for 30 mins followed by anti-IgM stimulation...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase SYK(Human)
Universita Degli Studi Di Palermo

Curated by ChEMBL
LigandPNGBDBM50076185(CHEMBL3416026 | US9290481, 1.1)
Affinity DataIC50: 367nMAssay Description:Inhibition of Syk in anti-CD32 stimulated CD14+ human monocytes assessed as phospho-SLP76 level preincubated for 30 mins followed by anti-CD32 stimul...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50076185(CHEMBL3416026 | US9290481, 1.1)
Affinity DataIC50: 2.59E+4nMAssay Description:Inhibition of human ERG expressed in CHO cells by automated Qpatch clamp assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2016
Entry Details Article
PubMed
TargetTyrosine-protein kinase receptor UFO(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50076185(CHEMBL3416026 | US9290481, 1.1)
Affinity DataKd:  71nMAssay Description:Competitive binding affinity to human AXLMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2016
Entry Details Article
PubMed
TargetMitotic checkpoint serine/threonine-protein kinase BUB1(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50076185(CHEMBL3416026 | US9290481, 1.1)
Affinity DataKd:  240nMAssay Description:Competitive binding affinity to human BUB1More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2016
Entry Details Article
PubMed
TargetInterleukin-1 receptor-associated kinase 1(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50076185(CHEMBL3416026 | US9290481, 1.1)
Affinity DataKd:  67nMAssay Description:Competitive binding affinity to human IRAK1More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2016
Entry Details Article
PubMed
TargetTyrosine-protein kinase SYK [2-635](Human)
Novartis

US Patent
LigandPNGBDBM50076185(CHEMBL3416026 | US9290481, 1.1)
Affinity DataIC50: 23nMpH: 7.5 T: 2°CAssay Description:All assays were performed in 384 well microtiter plates. Each assay plate contained 8-point serial dilutions for 40 test compounds, as well as four 8...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/6/2017
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetMitogen-activated protein kinase kinase kinase 2(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50076185(CHEMBL3416026 | US9290481, 1.1)
Affinity DataKd:  140nMAssay Description:Competitive binding affinity to human MAP3K2More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2016
Entry Details Article
PubMed
TargetTyrosine-protein kinase Mer(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50076185(CHEMBL3416026 | US9290481, 1.1)
Affinity DataKd:  150nMAssay Description:Competitive binding affinity to human MERTKMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2016
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase PAK 4(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50076185(CHEMBL3416026 | US9290481, 1.1)
Affinity DataKd:  17nMAssay Description:Competitive binding affinity to human PAK4More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2016
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase PAK 6(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50076185(CHEMBL3416026 | US9290481, 1.1)
Affinity DataKd:  110nMAssay Description:Competitive binding affinity to human PAK6More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2016
Entry Details Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50076185(CHEMBL3416026 | US9290481, 1.1)
Affinity DataIC50: 5.00E+3nMAssay Description:Inhibition of human ERG by GLP studyMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2016
Entry Details Article
PubMed
TargetTyrosine-protein kinase ZAP-70(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50076185(CHEMBL3416026 | US9290481, 1.1)
Affinity DataIC50: 2.53E+3nMAssay Description:Inhibition of ZAP70 in anti-CD3 stimulated human Jurkat T cells assessed as SLP76 phosphorylation at Y128 preincubated for 30 mins followed by anti-C...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2016
Entry Details Article
PubMed
TargetTyrosine-protein kinase ZAP-70(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50076185(CHEMBL3416026 | US9290481, 1.1)
Affinity DataIC50: 251nMAssay Description:Inhibition of human ZAP70More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2016
Entry Details Article
PubMed
TargetTyrosine-protein kinase ZAP-70(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50076185(CHEMBL3416026 | US9290481, 1.1)
Affinity DataKd:  65nMAssay Description:Competitive binding affinity to human ZAP70More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2016
Entry Details Article
PubMed
TargetTyrosine-protein kinase SYK(Human)
Universita Degli Studi Di Palermo

Curated by ChEMBL
LigandPNGBDBM50076185(CHEMBL3416026 | US9290481, 1.1)
Affinity DataKd:  0.640nMAssay Description:Competitive binding affinity to human SYKMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetSTE20-like serine/threonine-protein kinase(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50076185(CHEMBL3416026 | US9290481, 1.1)
Affinity DataKd:  380nMAssay Description:Competitive binding affinity to human SLKMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2016
Entry Details Article
PubMed
TargetProto-oncogene tyrosine-protein kinase ROS(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50076185(CHEMBL3416026 | US9290481, 1.1)
Affinity DataKd:  120nMAssay Description:Competitive binding affinity to human ROS1More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2016
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase PAK 5(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50076185(CHEMBL3416026 | US9290481, 1.1)
Affinity DataKd:  12nMAssay Description:Competitive binding affinity to human PAK7More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/24/2016
Entry Details Article
PubMed