BDBM178085 US10307413, Compound 188::US10391089, Compound 188::US10980794, Cmpd No 188::US9675614, 188

SMILES c1ccc2c(c1)CCN(C2)C[C@H](CNC(=O)c3ccnc(c3)NC4CCC4)O

InChI Key InChIKey=TWKYXZSXXXKKJU-UHFFFAOYSA-N

Data  6 IC50

PDB links: 1 PDB ID matches this monomer.

  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 = 178085   

LigandPNGBDBM178085(US9675614, 188 | US10307413, Compound 188 | US1039...)
Affinity DataEC50:  2.10nMAssay Description:Inhibition of PRMT5 in human Z138 cells assessed as effect on SDMA level incubated for 3 days by ELISA analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM178085(US9675614, 188 | US10307413, Compound 188 | US1039...)
Affinity DataKi:  2.40nMAssay Description:Inhibition of Flag-tagged human PRMT5/his-tagged MEP50 (unknown origin) expressed in baculovirus expression system using Sm3d as substrate assessed a...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM178085(US9675614, 188 | US10307413, Compound 188 | US1039...)
Affinity DataKi:  2.80nMAssay Description:Inhibition of Flag-tagged human PRMT5/his-tagged MEP50 (unknown origin) expressed in baculovirus expression system using H4 as substrate assessed as ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM178085(US9675614, 188 | US10307413, Compound 188 | US1039...)
Affinity DataIC50: 3nMAssay Description:Inhibition of PRMT5 in human Z138 cells assessed as reduction in symmetrical dimethylation of arginine containing substrate using SmD3 as substrate i...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM178085(US9675614, 188 | US10307413, Compound 188 | US1039...)
Affinity DataKi:  3.10nMAssay Description:Inhibition of Flag-tagged human PRMT5/his-tagged MEP50 (unknown origin) expressed in baculovirus expression system using H2A as substrate assessed as...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM178085(US9675614, 188 | US10307413, Compound 188 | US1039...)
Affinity DataIC50: 4nMAssay Description:Inhibition of human full length FLAG-tagged PRMT5/human His6-tagged MEP50 expressed in baculovirus-infected Sf9 cells assessed as reduction in tritiu...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM178085(US9675614, 188 | US10307413, Compound 188 | US1039...)
Affinity DataIC50: 4.80nMAssay Description:Inhibition of Flag-tagged human PRMT5/his-tagged MEP50 (unknown origin) expressed in baculovirus expression system using Sm3d as substrate preincubat...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM178085(US9675614, 188 | US10307413, Compound 188 | US1039...)
Affinity DataIC50: 5.5nMAssay Description:Inhibition of Flag-tagged human PRMT5/his-tagged MEP50 (unknown origin) expressed in baculovirus expression system using H4 as substrate preincubated...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM178085(US9675614, 188 | US10307413, Compound 188 | US1039...)
Affinity DataIC50: 6.10nMAssay Description:Inhibition of Flag-tagged human PRMT5/his-tagged MEP50 (unknown origin) expressed in baculovirus expression system using H2A as substrate preincubate...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM178085(US9675614, 188 | US10307413, Compound 188 | US1039...)
Affinity DataKi:  9.80nMAssay Description:Inhibition of Flag-tagged human PRMT5/his-tagged MEP50 (unknown origin) expressed in baculovirus expression system using HNRNPH1 as substrate assesse...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM178085(US9675614, 188 | US10307413, Compound 188 | US1039...)
Affinity DataIC50: 11nMAssay Description:Inhibition of PRMT5 (unknown origin) assessed as inhibition of PRMT5/MEP50 complex from methylating histone 4 (H4)More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM178085(US9675614, 188 | US10307413, Compound 188 | US1039...)
Affinity DataIC50: 20nMAssay Description:Inhibition of Flag-tagged human PRMT5/his-tagged MEP50 (unknown origin) expressed in baculovirus expression system using HNRNPH1 as substrate preincu...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM178085(US9675614, 188 | US10307413, Compound 188 | US1039...)
Affinity DataKi:  46nMAssay Description:Inhibition of Flag-tagged human PRMT5/his-tagged MEP50 (unknown origin) expressed in baculovirus expression system using FUBP1 as substrate assessed ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM178085(US9675614, 188 | US10307413, Compound 188 | US1039...)
Affinity DataIC50: 46nMAssay Description:Inhibition of Flag-tagged human PRMT5/his-tagged MEP50 (unknown origin) expressed in baculovirus expression system using FUBP1 as substrate preincuba...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMed
LigandPNGBDBM178085(US9675614, 188 | US10307413, Compound 188 | US1039...)
Affinity DataEC50:  56nMAssay Description:Inhibition of PRMT5 (unknown origin) assessed as inhibition of PRMT5/MEP50 complex from methylating SmD3More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM178085(US9675614, 188 | US10307413, Compound 188 | US1039...)
Affinity DataIC50: 100nMAssay Description:The assays were all performed in a buffer consisting of 20 mM Bicine (pH=7.6), 1 mM TCEP, 0.005% BSG, and 0.002% Tween20, prepared on the day of use....More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/20/2020
Entry Details
US Patent
PDB3D3D Structure (crystal)
TargetProtein arginine N-methyltransferase 5(Human)
Epizyme

US Patent
LigandPNGBDBM178085(US9675614, 188 | US10307413, Compound 188 | US1039...)
Affinity DataIC50: 100nMAssay Description:The assays were all performed in a buffer consisting of 20 mM Bicine (pH=7.6), 1 mM TCEP, 0.005% BSG, and 0.002% Tween20, prepared on the day of use....More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/15/2020
Entry Details
US Patent
PDB3D3D Structure (crystal)
TargetProtein arginine N-methyltransferase 5(Human)
Epizyme

US Patent
LigandPNGBDBM178085(US9675614, 188 | US10307413, Compound 188 | US1039...)
Affinity DataIC50: 100nMAssay Description:The assays were all performed in a buffer consisting of 20 mM Bicine (pH=7.6), 1 mM TCEP, 0.005% BSG, and 0.002% Tween20, prepared on the day of use....More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/26/2021
Entry Details
US Patent
PDB3D3D Structure (crystal)
TargetProtein arginine N-methyltransferase 5(Human)
Epizyme

US Patent
LigandPNGBDBM178085(US9675614, 188 | US10307413, Compound 188 | US1039...)
Affinity DataIC50: 100nMAssay Description:The assays were all performed in a buffer consisting of 20 mM Bicine (pH=7.6), 1 mM TCEP, 0.005% BSG, and 0.002% Tween20, prepared on the day of use....More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/12/2018
Entry Details
US Patent
PDB3D3D Structure (crystal)