BDBM50315769 3-(4-(4-(2-(3-((dimethylamino)methyl)phenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl)-1-ethyl-1H-pyrazol-3-yl)phenyl)-1,1-dimethylurea::4-[3-(4-N,N-Dimethylcarbamylaminophenyl)-1-ethyl-1H-pyrazol-4-yl]-2-[3-(dimethylaminomethyl)phenyl]-1H-pyrrolo[2,3-b]-pyridine::CHEMBL1090479::GSK-1070916

SMILES CCn1cc(c(n1)-c1ccc(NC(=O)N(C)C)cc1)-c1ccnc2[nH]c(cc12)-c1cccc(CN(C)C)c1

InChI Key InChIKey=QTBWCSQGBMPECM-UHFFFAOYSA-N

Data  8 KI  19 IC50  1 Kd

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
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Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 52 hits for monomerid = 50315769   

TargetAurora kinase A(Human)TBA
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataEC50:  0.00800nMAssay Description:Inhibition of Aurora A in human COLO 205 cells using pHH-S10 as substrate incubated for 2 hrs by ELISA methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetAurora kinase A(Human)TBA
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataEC50:  0.0120nMAssay Description:Inhibition of Aurora A in human MX1 cells using pHH-S10 as substrate incubated for 2 hrs by ELISA methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetAurora kinase A(Human)TBA
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataEC50:  0.0200nMAssay Description:Inhibition of Aurora A in human HCT-116 cells using pHH-S10 as substrate incubated for 2 hrs by ELISA methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetAurora kinase A(Human)TBA
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataEC50:  0.0460nMAssay Description:Inhibition of Aurora A in human A549 cells using pHH-S10 as substrate incubated for 2 hrs by ELISA methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetAurora kinase A(Human)TBA
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataEC50:  0.118nMAssay Description:Inhibition of Aurora A in human HeLa cells using pHH-S10 as substrate incubated for 2 hrs by ELISA methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetAurora kinase B(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataKi:  0.380nMAssay Description:Competitive inhibition of Aurora B ATP binding siteMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2012
Entry Details Article
PubMed
TargetAurora kinase B(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataKi:  0.380nMAssay Description:Competitive inhibition of human Aurora B ATP binding site by rapid dilution methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2012
Entry Details Article
PubMed
TargetAurora kinase B/Inner centromere protein(Human)
Nirma University

Curated by ChEMBL
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataKi:  0.380nMAssay Description:Inhibition of human Aurora B/INCENP pre-incubated for 30 mins before 5-FAM-PKAtide substrate addition and measured after 120 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/18/2020
Entry Details Article
PubMed
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataKi:  0.380nMAssay Description:Binding affinity to human AurB/INCENP assessed as inhibition constant using aurora sox peptide as substrate incubated for 60 mins in presence of ATP ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataKi:  0.390nMAssay Description:Binding affinity to AurB/INCENP (unknown origin) assessed as inhibition constantMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetAurora kinase C/Inner centromere protein(Human)
Nirma University

Curated by ChEMBL
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataKi:  1.5nMAssay Description:Inhibition of human Aurora C/human GST-tagged INCENP pre-incubated for 30 mins before 5-FAM-PKAtide substrate addition and measured after 60 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/18/2020
Entry Details Article
PubMed
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataKi:  1.5nMAssay Description:Binding affinity to AurC/INCENP (unknown origin) assessed as inhibition constantMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetAurora kinase C(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataKi:  1.5nMAssay Description:Competitive inhibition of human Aurora C ATP binding siteMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2012
Entry Details Article
PubMed
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataKi:  1.5nMAssay Description:Binding affinity to human AurC/INCENP assessed as inhibition constant using aurora sox peptide as substrate incubated for 60 mins in presence of ATP ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataIC50: 3.5nMAssay Description:Inhibition of human AurB/INCENP in PBS using Biotin-Ahx-RARRRLSFFFFAKKK-NH2 as substrate incubated for 30 mins in presence of ATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetAurora kinase B(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataIC50: 3.5nMAssay Description:Inhibition of recombinant aurora B (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/18/2020
Entry Details Article
PubMed
TargetAurora kinase B(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataIC50: 5nMAssay Description:Inhibition of AURB (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/25/2023
Entry Details
PubMed
TargetAurora kinase B(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataIC50: 5nMAssay Description:Inhibition of human Aurora B by rapid dilution methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2012
Entry Details Article
PubMed
TargetAurora kinase C(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataIC50: 6.5nMAssay Description:Inhibition of AURC (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/25/2023
Entry Details
PubMed
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataIC50: 6.5nMAssay Description:Inhibition of human AurC/INCENP in PBS using Biotin-Ahx-RARRRLSFFFFAKKK-NH2 as substrate incubated for 30 mins in presence of ATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetAurora kinase C(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataIC50: 6.5nMAssay Description:Competitive inhibition of Aurora C ATP binding siteMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2012
Entry Details Article
PubMed
TargetAurora kinase C(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataIC50: 6.5nMAssay Description:Inhibition of Aurora C kinase (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/18/2020
Entry Details Article
PubMed
TargetAurora kinase B(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataIC50: 32nMAssay Description:Inhibition of aurora B assessed as inhibition of histone H3 phosphorylation by ELISA based cellular mechanistic assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/18/2010
Entry Details Article
PubMed
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataIC50: 42nMAssay Description:Inhibition of FLT1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataIC50: 42nMAssay Description:Inhibition of FLT1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataIC50: 42nMAssay Description:Inhibition of FLT1More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2012
Entry Details Article
PubMed
TargetAngiopoietin-1 receptor(Human)TBA
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataIC50: 59nMAssay Description:Inhibition of TIE2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetAngiopoietin-1 receptor(Human)TBA
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataIC50: 59nMAssay Description:Inhibition of TIE2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetAngiopoietin-1 receptor(Human)TBA
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataIC50: 59nMAssay Description:Inhibition of TIE2More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2012
Entry Details Article
PubMed
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataIC50: 70nMAssay Description:Inhibition of SIK (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataIC50: 70nMAssay Description:Inhibition of SIKMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2012
Entry Details Article
PubMed
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataIC50: 70nMAssay Description:Inhibition of SIK (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetVascular endothelial growth factor receptor 3(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataIC50: 74nMAssay Description:Inhibition of FLT4More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2012
Entry Details Article
PubMed
TargetVascular endothelial growth factor receptor 3(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataIC50: 74nMAssay Description:Inhibition of FLT4 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetVascular endothelial growth factor receptor 3(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataIC50: 74nMAssay Description:Inhibition of FLT4 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetFibroblast growth factor receptor 1(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataIC50: 76nMAssay Description:Inhibition of FGFR1More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2012
Entry Details Article
PubMed
TargetFibroblast growth factor receptor 1(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataIC50: 76nMAssay Description:Inhibition of FGFR1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetFibroblast growth factor receptor 1(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataIC50: 78nMAssay Description:Inhibition of FGFR1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetAurora kinase A(Human)TBA
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataIC50: 200nMAssay Description:Inhibition of AURA (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/25/2023
Entry Details
PubMed
TargetAurora kinase A(Human)TBA
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataKi:  490nMAssay Description:Competitive inhibition of human Aurora A ATP binding siteMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2012
Entry Details Article
PubMed
TargetTargeting protein for Xklp2(Human)
Nirma University

Curated by ChEMBL
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataKi:  490nMAssay Description:Inhibition of human Aurora A/TPX2 (unknown origin) pre-incubated for 30 mins before Biotin-Ahx-RARRRLSFFFFAKKK-NH2 substrate addition and measured af...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/18/2020
Entry Details Article
PubMed
TargetAurora kinase A(Human)TBA
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataKi:  492nMAssay Description:Inhibition of Aurora AMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2012
Entry Details Article
PubMed
TargetTargeting protein for Xklp2(Human)
Nirma University

Curated by ChEMBL
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataKi:  492nMAssay Description:Binding affinity to Aura/TPX2 (unknown origin) assessed as inhibition constantMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetTargeting protein for Xklp2(Human)
Nirma University

Curated by ChEMBL
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataKi:  492nMAssay Description:Binding affinity to human AurA/TPX2 assessed as inhibition constant using aurora sox peptide as substrate incubated for 60 mins in presence of ATP by...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetTargeting protein for Xklp2(Human)
Nirma University

Curated by ChEMBL
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataIC50: 1.10E+3nMAssay Description:Inhibition of human AurA/TPX2 in PBS using Biotin-Ahx-RARRRLSFFFFAKKK-NH2 as substrate incubated for 30 mins in presence of ATP by LEADseeker assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetAurora kinase A(Human)TBA
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataIC50: 1.26E+3nMAssay Description:Inhibition of human Aurora AMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2012
Entry Details Article
PubMed
TargetFerrochelatase, mitochondrial [R115L](Human)
Technical University of Munich

LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataKd:  1.70E+3nMAssay Description:Briefly, 5 mg of a protein mixture of the four cell lines or a single cell line were incubated with compound dilution series in DMSO (3 nM, 10 nM, 30...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/30/2016
Entry Details Article
PubMed
TargetCytochrome P450 2D6(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataIC50: 1.20E+4nMAssay Description:Inhibition of CYP2D6 in human liver microsomes using bufuralol as substrateMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2012
Entry Details Article
PubMed
TargetCytochrome P450 3A4(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataIC50: 1.50E+4nMAssay Description:Inhibition of CYP3A4 in human liver microsomes using nifedipine as substrateMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2012
Entry Details Article
PubMed
TargetCytochrome P450 1A2(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50315769(GSK-1070916 | 4-[3-(4-N,N-Dimethylcarbamylaminophe...)
Affinity DataIC50: 3.30E+4nMAssay Description:Inhibition of CYP1A2 in human liver microsomes using phenacetin as substrateMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2012
Entry Details Article
PubMed
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