BDBM50285607 MLN-4924::MLN-4924003::Pevonedistat

SMILES [H][C@]1(O)C[C@@]([H])(C[C@@]1([H])COS(N)(=O)=O)n1ccc2c(N[C@@]3([H])CCc4ccccc34)ncnc12

InChI Key InChIKey=MPUQHZXIXSTTDU-QXGSTGNESA-N

Data  14 IC50  2 EC50

PDB links: 1 PDB ID matches this monomer.

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
   Substructure
Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 16 hits for monomerid = 50285607   

TargetNEDD8-activating enzyme E1 catalytic/regulatory subunit(Human)
University of Macau

Curated by ChEMBL
LigandPNGBDBM50285607(MLN-4924 | MLN-4924003 | Pevonedistat)
Affinity DataEC50:  3.40E+3nMAssay Description:Inhibition of NAE-mediated Ubcl2-NEDD8 conjugation in human Caco2 cells after 16 hrs by Western blot analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetPotassium voltage-gated channel subfamily H member 2(Human)
Shanghai Institute of Materia Medica (Simm)

Curated by ChEMBL
LigandPNGBDBM50285607(MLN-4924 | MLN-4924003 | Pevonedistat)
Affinity DataIC50: >4.00E+4nMAssay Description:Inhibition of hERG channelMore data for this Ligand-Target Pair
In DepthDetails PubMed

TargetUbiquitin-like modifier-activating enzyme ATG7(Human)
Temple University

Curated by ChEMBL
LigandPNGBDBM50285607(MLN-4924 | MLN-4924003 | Pevonedistat)
Affinity DataIC50: >1.00E+3nMAssay Description:Inhibition of ATG7 (unknown origin) assessed as decrease in formation of E2-UBL thioester reaction productMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetUbiquitin-like modifier-activating enzyme 6(Human)
Temple University

Curated by ChEMBL
LigandPNGBDBM50285607(MLN-4924 | MLN-4924003 | Pevonedistat)
Affinity DataIC50: >1.00E+3nMAssay Description:Inhibition of UBA6 (unknown origin) assessed as decrease in formation of E2-UBL thioester reaction productMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetNEDD8(Human)
Temple University

Curated by ChEMBL
LigandPNGBDBM50285607(MLN-4924 | MLN-4924003 | Pevonedistat)
Affinity DataIC50:  4.70nMAssay Description:Inhibition of NEDD8 (unknown origin) assessed as decrease in formation of E2-UBL thioester reaction productMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetNEDD8-activating enzyme E1 catalytic subunit(Human)
St. Jude Children'S Research Hospital

Curated by ChEMBL
LigandPNGBDBM50285607(MLN-4924 | MLN-4924003 | Pevonedistat)
Affinity DataIC50:  5nMAssay Description:Inhibition of human recombinant His-tagged NAE1 expressed in baculovirus expression system after 90 mins in presence of FLAG-tagged NEDD8 by TR-FRET ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetNEDD8-activating enzyme E1 regulatory subunit(Human)
East China University of Science and Technology

Curated by ChEMBL
LigandPNGBDBM50285607(MLN-4924 | MLN-4924003 | Pevonedistat)
Affinity DataIC50:  180nMAssay Description:Inhibition of NAE (unknown origin)-mediated neddylation assessed as suppression of cullin1-Nedd8 adduct formation preincubated for 10 mins followed b...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetNEDD8-activating enzyme E1 catalytic subunit(Human)
St. Jude Children'S Research Hospital

Curated by ChEMBL
LigandPNGBDBM50285607(MLN-4924 | MLN-4924003 | Pevonedistat)
Affinity DataIC50:  4nMAssay Description:Inhibition of NAE1/UBA3 in human HCT-116 cells assessed as reduction in Ubc12-NEDD8 level incubated for 24 hrs by immunoblot analysisMore data for this Ligand-Target Pair
In DepthDetails PubMed

TargetSUMO-activating enzyme subunit 1/2(Human)
Southwest Jiaotong University

Curated by ChEMBL
LigandPNGBDBM50285607(MLN-4924 | MLN-4924003 | Pevonedistat)
Affinity DataIC50:  8.20E+3nMAssay Description:Inhibition of SAE1/UBA2 in human HCT-116 cells assessed as reduction in Ubc9-SUMO level incubated for 24 hrs by immunoblot analysisMore data for this Ligand-Target Pair
In DepthDetails PubMed

TargetUbiquitin-like modifier-activating enzyme 1(Mouse)
Southwest Jiaotong University

Curated by ChEMBL
LigandPNGBDBM50285607(MLN-4924 | MLN-4924003 | Pevonedistat)
Affinity DataIC50:  1.50E+3nMAssay Description:Inhibition of mouse UAE1 in human HCT-116 cells assessed as reduction in Ubc10-Ub thioester level incubated for 24 hrs by immunoblot analysisMore data for this Ligand-Target Pair
In DepthDetails PubMed

TargetUbiquitin-like modifier-activating enzyme 6(Human)
Temple University

Curated by ChEMBL
LigandPNGBDBM50285607(MLN-4924 | MLN-4924003 | Pevonedistat)
Affinity DataIC50:  1.80E+3nMAssay Description:Inhibition of His-tagged UBA6 (unknown origin) expressed in sf9 insect cellsMore data for this Ligand-Target Pair
In DepthDetails PubMed

TargetUbiquitin-like modifier-activating enzyme ATG7(Human)
Temple University

Curated by ChEMBL
LigandPNGBDBM50285607(MLN-4924 | MLN-4924003 | Pevonedistat)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of His-tagged ATG7 (unknown origin) expressed in sf9 insect cellsMore data for this Ligand-Target Pair
In DepthDetails PubMed

TargetNEDD8-activating enzyme E1 catalytic subunit(Human)
St. Jude Children'S Research Hospital

Curated by ChEMBL
LigandPNGBDBM50285607(MLN-4924 | MLN-4924003 | Pevonedistat)
Affinity DataIC50:  0.260nMAssay Description:Inhibition of NAE (unknown origin) mediated neddylation assessed as decrease in NEDD8-Ubcl2 adduct formation incubated for 2 hrs in presence of L-glu...More data for this Ligand-Target Pair
In DepthDetails PubMed

TargetNEDD8-activating enzyme E1 catalytic subunit(Human)
St. Jude Children'S Research Hospital

Curated by ChEMBL
LigandPNGBDBM50285607(MLN-4924 | MLN-4924003 | Pevonedistat)
Affinity DataIC50:  4nMAssay Description:Inhibition of NAE (unknown origin)More data for this Ligand-Target Pair
In DepthDetails PubMed

TargetNEDD8-activating enzyme E1 catalytic subunit(Human)
St. Jude Children'S Research Hospital

Curated by ChEMBL
LigandPNGBDBM50285607(MLN-4924 | MLN-4924003 | Pevonedistat)
Affinity DataEC50:  30nMAssay Description:Inhibition of NAE in human HCT-116 cells incubated for 1 hr by Western blot analysisMore data for this Ligand-Target Pair
In DepthDetails PubMed

TargetSUMO-activating enzyme subunit 1/2(Human)
Southwest Jiaotong University

Curated by ChEMBL
LigandPNGBDBM50285607(MLN-4924 | MLN-4924003 | Pevonedistat)
Affinity DataIC50: >1.00E+3nMAssay Description:Inhibition of SAE (unknown origin) assessed as decrease in formation of E2-UBL thioester reaction productMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed