BDBM50262079 4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline::4-[6-(4-piperazin-1-ylphenyl)pyrazolo[1,5-a]pyrimidin-3-yl]quinoline::CHEMBL513147::LDN-193189

SMILES C1CN(CCN1)c1ccc(cc1)-c1cnc2c(cnn2c1)-c1ccnc2ccccc12

InChI Key InChIKey=CDOVNWNANFFLFJ-UHFFFAOYSA-N

Data  49 IC50  4 EC50

PDB links: 4 PDB IDs match 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 53 hits for monomerid = 50262079   

TargetReceptor protein serine/threonine kinase(Zebrafish)
Vanderbilt University

LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataEC50:  3.00E+3nMAssay Description:The effects on zebrafish embryos with respect to the dorsoventral (DV) axis. For dorsalization, the EC100 (effective concentration 100%) represents t...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetActivin receptor type-2B(Human)
Baylor College of Medicine

Curated by ChEMBL
LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  9.30E+3nMAssay Description:Inhibition of ACVR2B (unknown origin) by LanthaScreen TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetReceptor protein serine/threonine kinase(Zebrafish)
Vanderbilt University

LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataEC50:  2.00E+4nMAssay Description:For nonspecific toxicity, the EC100 represents the concentration when 100% of the treated embryos exhibit either early lethality within hours of comp...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetActivin receptor type-1(Human)
Vanderbilt University

LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  40.7nMAssay Description:Shown are the IC50s (concentrations causing 50% inhibition) of DM and the analogues for the in vitro kinase assays using the following purified human...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetTGF-beta receptor type-1(Human)
Vanderbilt University

LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  565nMAssay Description:Shown are the IC50s (concentrations causing 50% inhibition) of DM and the analogues for the in vitro kinase assays using the following purified human...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  1.12E+3nMAssay Description:Shown are the IC50s (concentrations causing 50% inhibition) of DM and the analogues for the in vitro kinase assays using the following purified human...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetVascular endothelial growth factor receptor 2(Human)
Vanderbilt University

LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  215nMAssay Description:Shown are the IC50s (concentrations causing 50% inhibition) of DM and the analogues for the in vitro kinase assays using the following purified human...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetSerine/threonine-protein kinase receptor R3(Mouse)
Massachusetts Institute of Technology

LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  1.48nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetActivin receptor type-1(Mouse)
Massachusetts Institute of Technology

LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  0.670nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetBone morphogenetic protein receptor type-1A(Mouse)
Massachusetts Institute of Technology

LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  14.3nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetActivin receptor type-1B(Mouse)
Massachusetts Institute of Technology

LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  108nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetTGF-beta receptor type-1(Mouse)
Massachusetts Institute of Technology

LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  117nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetBone morphogenetic protein 4(Human)
Harvard Medical School

Curated by ChEMBL
LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  4.90nMAssay Description:Inhibition of BMP4 (unknown origin)-induced phosphorylation of SMAD 1/5/8 by cytoblot cellular ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetBone morphogenetic protein receptor type-1B(Human)
Vanderbilt University Medical Center

Curated by ChEMBL
LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  60nMAssay Description:Inhibition of ALK6 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetActivin receptor type-1(Human)
Vanderbilt University

LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  41nMAssay Description:Inhibition of ALK2 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetSerine/threonine-protein kinase receptor R3(Human)
Vanderbilt University Medical Center

Curated by ChEMBL
LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  13nMAssay Description:Inhibition of ALK1 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetBone morphogenetic protein receptor type-2(Human)
Vanderbilt University Medical Center

Curated by ChEMBL
LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  3.85E+3nMAssay Description:Inhibition of BMPR2 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetActivin receptor type-1B(Human)
Vanderbilt University Medical Center

Curated by ChEMBL
LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  1.83E+3nMAssay Description:Inhibition of ALK4 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

Target5'-AMP-activated protein kinase subunit beta-1(Human)
Vanderbilt University Medical Center

Curated by ChEMBL
LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  1.12E+3nMAssay Description:Inhibition of AMPK (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetTGF-beta receptor type-1(Human)
Vanderbilt University

LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  565nMAssay Description:Inhibition of ALK5 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetTGF-beta receptor type-2(Human)
Vanderbilt University Medical Center

Curated by ChEMBL
LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  140nMAssay Description:Inhibition of TGFBR2 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetSerine/threonine-protein kinase receptor R3(Human)
Vanderbilt University Medical Center

Curated by ChEMBL
LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  11nMAssay Description:Inhibition of human ALK1 using casein as substrate in presence of 10 uM ATP by radiometric kinase assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetActivin receptor type-1(Human)
Vanderbilt University

LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  3.30nMAssay Description:Inhibition of human ALK2 using casein as substrate in presence of 10 uM ATP by radiometric kinase assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetBone morphogenetic protein receptor type-1A(Human)
Korea University

Curated by ChEMBL
LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  2.20nMAssay Description:Inhibition of human ALK3 using casein as substrate in presence of 10 uM ATP by radiometric kinase assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetActivin receptor type-1B(Human)
Vanderbilt University Medical Center

Curated by ChEMBL
LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  43nMAssay Description:Inhibition of human ALK4 using casein as substrate in presence of 10 uM ATP by radiometric kinase assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetBone morphogenetic protein receptor type-1B(Human)
Vanderbilt University Medical Center

Curated by ChEMBL
LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  0.940nMAssay Description:Inhibition of human ALK6 using casein as substrate in presence of 10 uM ATP by radiometric kinase assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetTGF-beta receptor type-1(Human)
Vanderbilt University

LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  27nMAssay Description:Inhibition of human ALK5 using casein as substrate in presence of 10 uM ATP by radiometric kinase assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetActivin receptor type-1(Human)
Vanderbilt University

LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  17nMAssay Description:Inhibition of ALK2 (unknown origin) using Ulight topo IIa (Thr 1342) peptide as substrate preincubated for 10 mins followed by substrate addition and...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetActivin receptor type-1(Mouse)
Massachusetts Institute of Technology

LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataEC50:  14nMAssay Description:Inhibition of BMP6-induced ALK2 transcriptional activity in mouse C2C12 cells expressing BRE-Luc after 30 mins by luciferase reporter gene assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetBone morphogenetic protein receptor type-1A(Human)
Korea University

Curated by ChEMBL
LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  19nMAssay Description:Inhibition of ALK3 (unknown origin) using Ulight topo IIa (Thr 1342) peptide as substrate preincubated for 10 mins followed by substrate addition and...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetTGF-beta receptor type-1(Human)
Vanderbilt University

LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  500nMAssay Description:Inhibition of human ALK5 in presence of (33P)gamma ATPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetBone morphogenetic protein receptor type-1A(Human)
Korea University

Curated by ChEMBL
LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  23.4nMAssay Description:Inhibition of human ALK3 using casein as substrate by [gamma-33P]-ATP assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetTGF-beta receptor type-1(Human)
Vanderbilt University

LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  339nMAssay Description:Inhibition of human ALK5 using casein as substrate by [gamma-33P]-ATP assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetBone morphogenetic protein receptor type-1B(Human)
Vanderbilt University Medical Center

Curated by ChEMBL
LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  12.7nMAssay Description:Inhibition of human ALK6 using casein as substrate by [gamma-33P]-ATP assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetActivin receptor type-1(Human)
Vanderbilt University

LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  43.3nMAssay Description:Inhibition of human ALK2 using casein as substrate by [gamma-33P]-ATP assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetSerine/threonine-protein kinase receptor R3(Human)
Vanderbilt University Medical Center

Curated by ChEMBL
LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  19.6nMAssay Description:Inhibition of human ALK1 using casein as substrate by [gamma-33P]-ATP assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetActivin receptor type-1B(Human)
Vanderbilt University Medical Center

Curated by ChEMBL
LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  297nMAssay Description:Inhibition of human ALK4 using casein as substrate by [gamma-33P]-ATP assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetTGF-beta receptor type-2(Human)
Vanderbilt University Medical Center

Curated by ChEMBL
LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  156nMAssay Description:Inhibition of human TGFBR2 using MBP as substrate by [gamma-33P]-ATP assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetTGF-beta receptor type-1(Human)
Vanderbilt University

LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  468nMAssay Description:Inhibition of human ALK5 using dephosphorylated casein as substrate measured after 45 mins in presence of [gamma33P]ATP by scintillation counting met...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetTGF-beta receptor type-1(Human)
Vanderbilt University

LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  468nMAssay Description:Inhibition of human ALK5 using casein as substrate in presence of 10 uM [gamma33P] ATP by radioactive assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetActivin receptor type-1(Human)
Vanderbilt University

LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  17nMAssay Description:Inhibition of human ALK2 using dephosphorylated casein as substrate measured after 45 mins in presence of [gamma33P]ATP by scintillation counting met...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetActivin receptor type-1(Human)
Vanderbilt University

LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  17nMAssay Description:Inhibition of human ALK2 using casein as substrate in presence of 10 uM [gamma33P] ATP by radioactive assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetReceptor-interacting serine/threonine-protein kinase 2(Human)
Baylor College of Medicine

Curated by ChEMBL
LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  25nMAssay Description:Inhibition of RIPK2 (unknown origin) incubated for 30 mins in presence of [gamma33P]ATP by microplate reader analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetBone morphogenetic protein receptor type-2(Human)
Vanderbilt University Medical Center

Curated by ChEMBL
LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50: >1.00E+6nMAssay Description:Inhibition of recombinant C-terminal 6His-tagged human BMPR2 (188 to 517 residues) expressed in Escherichia coli Rosetta by LanthaScreen TR-FRET assa...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetSerine/threonine-protein kinase receptor R3(Human)
Vanderbilt University Medical Center

Curated by ChEMBL
LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  1.20E+3nMAssay Description:Inhibition of ACVRL1 (unknown origin) by LanthaScreen TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetActivin receptor type-1(Human)
Vanderbilt University

LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  1.80E+3nMAssay Description:Inhibition of ACVR1 (unknown origin) by LanthaScreen TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetBone morphogenetic protein receptor type-1A(Human)
Korea University

Curated by ChEMBL
LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  3.80E+3nMAssay Description:Inhibition of BMPR1A (unknown origin) by LanthaScreen TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetActivin receptor type-1B(Human)
Vanderbilt University Medical Center

Curated by ChEMBL
LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  2.65E+5nMAssay Description:Inhibition of ACVR1B (unknown origin) by Z'-LYTE assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetTGF-beta receptor type-1(Human)
Vanderbilt University

LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  7.80E+3nMAssay Description:Inhibition of TGFBR1 (unknown origin) by LanthaScreen TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetBone morphogenetic protein receptor type-1B(Human)
Vanderbilt University Medical Center

Curated by ChEMBL
LigandPNGBDBM50262079(4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyri...)
Affinity DataIC50:  2.30E+3nMAssay Description:Inhibition of BMPR1B (unknown origin) by LanthaScreen TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

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