BDBM50652774 Gsk-923295a::Gsk923295::GSK-295::GSK-923295::GSK-923295A::GSK923295

SMILES CC(C)Oc1ccc(C(=O)N[C@H](CNC(=O)CN(C)C)Cc2ccc(-c3cn4cccc([C@H](C)O)c4n3)cc2)cc1Cl

InChI Key

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

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 19 hits for monomerid = 50652774   

TargetCentromere protein E(Canis lupus familiaris)TBA
LigandPNGBDBM50652774(Gsk-923295a | Gsk923295 | GSK-295 | GSK-923295 | G...)
Affinity DataKi:  1.60nMAssay Description:Binding affinity to wild-type dog CENP-E assessed as inhibition constantMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM50652774(Gsk-923295a | Gsk923295 | GSK-295 | GSK-923295 | G...)
Affinity DataIC50: 2.30nMAssay Description:Inhibition of microtubule-stimulated ATPase activity of C-terminal 6-his-tagged CENP-E (2 to 340 residues)(unknown origin) expressed in Escherichia c...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM50652774(Gsk-923295a | Gsk923295 | GSK-295 | GSK-923295 | G...)
Affinity DataKi:  3.10nMAssay Description:Uncompetitive binding affinity to microtubule-stimulated ATPase activity of C-terminal 6-his-tagged CENP-E (2 to 340 residues)(unknown origin) expres...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM50652774(Gsk-923295a | Gsk923295 | GSK-295 | GSK-923295 | G...)
Affinity DataKi:  3.20nMAssay Description:Uncompetitive binding affinity to C-terminal 6-his-tagged CENP-E (2 to 340 residues)(unknown origin) expressed in Escherichia coli BL21(DE3) assessed...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM50652774(Gsk-923295a | Gsk923295 | GSK-295 | GSK-923295 | G...)
Affinity DataKi:  3.20nMAssay Description:Binding affinity to wild-type human CENP-E assessed as inhibition constantMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM50652774(Gsk-923295a | Gsk923295 | GSK-295 | GSK-923295 | G...)
Affinity DataKi:  12nMAssay Description:Binding affinity to human CENP-E K184T mutant assessed as inhibition constantMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM50652774(Gsk-923295a | Gsk923295 | GSK-295 | GSK-923295 | G...)
Affinity DataKi:  13nMAssay Description:Binding affinity to human CENP-E T183A mutant assessed as inhibition constantMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM50652774(Gsk-923295a | Gsk923295 | GSK-295 | GSK-923295 | G...)
Affinity DataKi:  14nMAssay Description:Binding affinity to human CENP-E I182L mutant assessed as inhibition constantMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM50652774(Gsk-923295a | Gsk923295 | GSK-295 | GSK-923295 | G...)
Affinity DataIC50: 17nMAssay Description:Inhibition of CENP-E in human SW48 cells assessed as decrease in cell viability after 72 hrs by Cell-titer Glo reagent assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM50652774(Gsk-923295a | Gsk923295 | GSK-295 | GSK-923295 | G...)
Affinity DataKi:  18nMAssay Description:Binding affinity to human CENP-E I182L/K184T mutant assessed as inhibition constantMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM50652774(Gsk-923295a | Gsk923295 | GSK-295 | GSK-923295 | G...)
Affinity DataIC50: 42nMAssay Description:Inhibition of CENP-E in human SW620 cells expressing KRAS mutant assessed as decrease in cell viability after 72 hrs by Cell-titer Glo reagent assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM50652774(Gsk-923295a | Gsk923295 | GSK-295 | GSK-923295 | G...)
Affinity DataIC50: 52nMAssay Description:Inhibition of CENP-E in human HCT-116 cells expressing KRAS mutant assessed as decrease in cell viability after 72 hrs by Cell-titer Glo reagent assa...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM50652774(Gsk-923295a | Gsk923295 | GSK-295 | GSK-923295 | G...)
Affinity DataIC50: 56nMAssay Description:Inhibition of CENP-E in human RKO cells expressing BRAF mutant assessed as decrease in cell viability after 72 hrs by Cell-titer Glo reagent assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM50652774(Gsk-923295a | Gsk923295 | GSK-295 | GSK-923295 | G...)
Affinity DataKi:  61nMAssay Description:Binding affinity to human CENP-E I182L/T183A mutant assessed as inhibition constantMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM50652774(Gsk-923295a | Gsk923295 | GSK-295 | GSK-923295 | G...)
Affinity DataKi:  64nMAssay Description:Binding affinity to human CENP-E I182L/T183A/K184T mutant assessed as inhibition constantMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
TBA
Entry Details
PubMed
TargetCentromere-associated protein E(Mus musculus)TBA
LigandPNGBDBM50652774(Gsk-923295a | Gsk923295 | GSK-295 | GSK-923295 | G...)
Affinity DataKi:  67nMAssay Description:Binding affinity to wild-type mouse CENP-E assessed as inhibition constantMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM50652774(Gsk-923295a | Gsk923295 | GSK-295 | GSK-923295 | G...)
Affinity DataIC50: 134nMAssay Description:Inhibition of CENP-E in human SK-N-FI cells assessed as decrease in cell viability after 72 hrs in presence of ERK1 siRNA by Cell-titer Glo reagent a...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM50652774(Gsk-923295a | Gsk923295 | GSK-295 | GSK-923295 | G...)
Affinity DataIC50: 283nMAssay Description:Inhibition of CENP-E in human SK-N-FI cells assessed as decrease in cell viability after 72 hrs by Cell-titer Glo reagent assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM50652774(Gsk-923295a | Gsk923295 | GSK-295 | GSK-923295 | G...)
Affinity DataIC50: 2.08E+3nMAssay Description:Inhibition of ATPase activity of C-terminal 6-his-tagged CENP-E (2 to 340 residues)(unknown origin) expressed in Escherichia coli BL21(DE3) in presen...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
TBA
Entry Details
PubMed