BDBM16018 14,15-diazatetracyclo[7.6.1.0^{2,7}.0^{13,16}]hexadeca-1(15),2(7),3,5,9(16),10,12-heptaen-8-one::CHEMBL7064::ChemBiol10705 Compound 4::JMC517015 Compound 2::SP 600125::SP-600125::SP600125::cid_8515::dibenzo[cd,g]indazol-6(2H)-one

SMILES O=C1c2ccccc2-c2n[nH]c3cccc1c23

InChI Key InChIKey=ACPOUJIDANTYHO-UHFFFAOYSA-N

Data  26 IC50  3 Kd

PDB links: 5 PDB IDs match this monomer.

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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 29 hits for monomerid = 16018   

TargetMitogen-activated protein kinase 10(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM16018(14,15-diazatetracyclo[7.6.1.0^{2,7}.0^{13,16}]hexa...)
Affinity DataIC50:  150nMpH: 7.0 T: 2°CAssay Description:HTRF relies on fluorescence resonance energy transfer (FRET) between the donor, a europium cryptate (EuK), and the acceptor, the light harvesting pro...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 9(Homo sapiens (Human))
National Clinical Research Center For Geriatrics

Curated by ChEMBL
LigandPNGBDBM16018(14,15-diazatetracyclo[7.6.1.0^{2,7}.0^{13,16}]hexa...)
Affinity DataIC50:  40nMAssay Description:Inhibition of JNK2 (unknown origin)More data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical

LigandPNGBDBM16018(14,15-diazatetracyclo[7.6.1.0^{2,7}.0^{13,16}]hexa...)
Affinity DataIC50:  957nMpH: 7.5 T: 2°CAssay Description:An ELISA assay was used to determine the ability of inhibitor to inhibit JAK3 RTK activity. The compounds were incubated with enzyme, 10 uM ATP, and ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitochondrial import inner membrane translocase subunit TIM10(Saccharomyces cerevisiae S288c)
Burnham Center For Chemical Genomics

Curated by PubChem BioAssay
LigandPNGBDBM16018(14,15-diazatetracyclo[7.6.1.0^{2,7}.0^{13,16}]hexa...)
Affinity DataIC50: >1.00E+5nMAssay Description:Data Source: Sanford-Burnham Center for Chemical Genomics (SBCCG) Source Affiliation: Sanford-Burnham Medical Research Institute(SBMRI, San Diego, CA...More data for this Ligand-Target Pair
In DepthDetails PCBioAssay
TargetMitogen-activated protein kinase 9(Homo sapiens (Human))
National Clinical Research Center For Geriatrics

Curated by ChEMBL
LigandPNGBDBM16018(14,15-diazatetracyclo[7.6.1.0^{2,7}.0^{13,16}]hexa...)
Affinity DataIC50:  110nMAssay Description:The binding results were confirmed by measuring IC50 for the inhibition of JNK kinase activity by using Z'-LYTE assay format.More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 10(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM16018(14,15-diazatetracyclo[7.6.1.0^{2,7}.0^{13,16}]hexa...)
Affinity DataIC50:  190nMAssay Description:The binding results were confirmed by measuring IC50 for the inhibition of JNK kinase activity by using Z'-LYTE assay format.More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 10(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM16018(14,15-diazatetracyclo[7.6.1.0^{2,7}.0^{13,16}]hexa...)
Affinity DataIC50:  220nMMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 8(Homo sapiens (Human))
The Scripps Research Institute

LigandPNGBDBM16018(14,15-diazatetracyclo[7.6.1.0^{2,7}.0^{13,16}]hexa...)
Affinity DataIC50:  68nMMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase/endoribonuclease IRE1 [547-977](Homo sapiens (Human))
University of Washington

LigandPNGBDBM16018(14,15-diazatetracyclo[7.6.1.0^{2,7}.0^{13,16}]hexa...)
Affinity DataIC50:  720nMpH: 7.5Assay Description:Inhibitors (initial concentration 10 or 60 μM, three-fold serial dilutions) were incubated with IRE1α* in cleavage buffer (20 mM HEPES at p...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 8(Homo sapiens (Human))
The Scripps Research Institute

LigandPNGBDBM16018(14,15-diazatetracyclo[7.6.1.0^{2,7}.0^{13,16}]hexa...)
Affinity DataIC50:  40nMAssay Description:Inhibition of JNK1More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 9(Homo sapiens (Human))
National Clinical Research Center For Geriatrics

Curated by ChEMBL
LigandPNGBDBM16018(14,15-diazatetracyclo[7.6.1.0^{2,7}.0^{13,16}]hexa...)
Affinity DataIC50:  40nMAssay Description:Inhibition of JNK2More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 10(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM16018(14,15-diazatetracyclo[7.6.1.0^{2,7}.0^{13,16}]hexa...)
Affinity DataIC50:  90nMAssay Description:Inhibition of JNK3More data for this Ligand-Target Pair
TargetInterferon-induced, double-stranded RNA-activated protein kinase(Homo sapiens (Human))
Weill Cornell Medical College

Curated by ChEMBL
LigandPNGBDBM16018(14,15-diazatetracyclo[7.6.1.0^{2,7}.0^{13,16}]hexa...)
Affinity DataIC50:  8.00E+3nMAssay Description:Inhibition of human recombinant PKR autophosphorylation using poly[I:C] after 10 mins by luminescent assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 8(Homo sapiens (Human))
The Scripps Research Institute

LigandPNGBDBM16018(14,15-diazatetracyclo[7.6.1.0^{2,7}.0^{13,16}]hexa...)
Affinity DataIC50:  1.40E+4nMAssay Description:Inhibition of JNK1 using ATF2 substrate by TR-FRET assayMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 8(Homo sapiens (Human))
The Scripps Research Institute

LigandPNGBDBM16018(14,15-diazatetracyclo[7.6.1.0^{2,7}.0^{13,16}]hexa...)
Affinity DataIC50:  110nMAssay Description:Inhibition of human JNK1 by radiometric assayMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 10(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM16018(14,15-diazatetracyclo[7.6.1.0^{2,7}.0^{13,16}]hexa...)
Affinity DataIC50:  1.00E+4nMAssay Description:Inhibition of JNK3 in human PBMCs assessed as decrease in LPS-induced TNFalpha mRNA level after 4 hrs by real-time reverse transcription-PCR analysisMore data for this Ligand-Target Pair
TargetDual specificity protein kinase TTK(Homo sapiens (Human))
Jilin University

Curated by ChEMBL
LigandPNGBDBM16018(14,15-diazatetracyclo[7.6.1.0^{2,7}.0^{13,16}]hexa...)
Affinity DataIC50:  98nMAssay Description:Inhibition of MPS1 (unknown origin)More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 8(Homo sapiens (Human))
The Scripps Research Institute

LigandPNGBDBM16018(14,15-diazatetracyclo[7.6.1.0^{2,7}.0^{13,16}]hexa...)
Affinity DataKd:  100nMAssay Description:Binding affinity to human full-length JNK1 (M1 to Q384 residues) expressed in HEK293 cells measured after 1 hr by Kinomescan methodMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 10/8/9(Homo sapiens (Human))
Montana State University

Curated by ChEMBL
LigandPNGBDBM16018(14,15-diazatetracyclo[7.6.1.0^{2,7}.0^{13,16}]hexa...)
Affinity DataIC50:  5.20E+3nMAssay Description:Inhibition of JNK in human MONO-MAC-6 cells assessed as reduction in LPS-induced IL6 production preincubated for 30 mins followed by LPS-stimulation ...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 9(Homo sapiens (Human))
National Clinical Research Center For Geriatrics

Curated by ChEMBL
LigandPNGBDBM16018(14,15-diazatetracyclo[7.6.1.0^{2,7}.0^{13,16}]hexa...)
Affinity DataKd:  84nMAssay Description:Binding affinity to human full-length JNK2 (M1 to Q382 residues) expressed in HEK293 cells measured after 1 hr by Kinomescan methodMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 10(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM16018(14,15-diazatetracyclo[7.6.1.0^{2,7}.0^{13,16}]hexa...)
Affinity DataKd:  22nMAssay Description:Binding affinity to human partial length JNK3 (V28 to Q422 residues) expressed in HEK293 cells measured after 1 hr by Kinomescan methodMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 10/8/9(Homo sapiens (Human))
Montana State University

Curated by ChEMBL
LigandPNGBDBM16018(14,15-diazatetracyclo[7.6.1.0^{2,7}.0^{13,16}]hexa...)
Affinity DataIC50:  3.40E+3nMAssay Description:Inhibition of JNK in human THP1-Blue cells assessed as reduction in LPS-induced NFkappaB/AP1 activation preincubated for 30 mins followed by LPS-stim...More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 10(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM16018(14,15-diazatetracyclo[7.6.1.0^{2,7}.0^{13,16}]hexa...)
Affinity DataIC50:  90nMAssay Description:Inhibition of human JNK3 after 40 mins by [gamma-33ATP] radiometric assay relative to controlMore data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 8/9(Homo sapiens (Human))
Centro De Investigaciones Biol�Gicas Margarita Salas (Csic)

Curated by ChEMBL
LigandPNGBDBM16018(14,15-diazatetracyclo[7.6.1.0^{2,7}.0^{13,16}]hexa...)
Affinity DataIC50:  40nMAssay Description:Inhibition of JNK1/2 (unknown origin)More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 10(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM16018(14,15-diazatetracyclo[7.6.1.0^{2,7}.0^{13,16}]hexa...)
Affinity DataIC50:  90nMAssay Description:Inhibition of JNK3 (unknown origin)More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 10(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM16018(14,15-diazatetracyclo[7.6.1.0^{2,7}.0^{13,16}]hexa...)
Affinity DataIC50:  91nMAssay Description:Inhibition of JNK3 (unknown origin)More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 8(Homo sapiens (Human))
The Scripps Research Institute

LigandPNGBDBM16018(14,15-diazatetracyclo[7.6.1.0^{2,7}.0^{13,16}]hexa...)
Affinity DataIC50:  40nMAssay Description:Inhibition of JNK1 (unknown origin)More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 10(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM16018(14,15-diazatetracyclo[7.6.1.0^{2,7}.0^{13,16}]hexa...)
Affinity DataIC50:  90nMAssay Description:Inhibition of JNK3 (unknown origin)More data for this Ligand-Target Pair
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM16018(14,15-diazatetracyclo[7.6.1.0^{2,7}.0^{13,16}]hexa...)
Affinity DataIC50: >3.00E+4nMpH: 7.0 T: 2°CAssay Description:HTRF relies on fluorescence resonance energy transfer (FRET) between the donor, a europium cryptate (EuK), and the acceptor, the light harvesting pro...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed