BDBM388378 US10294246, Compound No. 75

SMILES Cc1cccc2c(C[C@H](NC(=O)Cc3ccccc3)B(O)O)coc12

InChI Key InChIKey=BOTOTAFWXOQROJ-UHFFFAOYSA-N

Data  6 IC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 6 hits for monomerid = 388378   

TargetProteasome subunit beta type-8(Human)
Merck

Curated by ChEMBL
LigandPNGBDBM388378(US10294246, Compound No. 75)
Affinity DataIC50: 4.5nMAssay Description:Inhibition of human 20S immunoproteasome beta-5i subunit using Suc-LLVY-AMC as substrate preincubated for 2 hrs followed by substrate addition and me...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/24/2023
Entry Details
PubMed
TargetProteasome subunit beta type-8(Human)
Merck

Curated by ChEMBL
LigandPNGBDBM388378(US10294246, Compound No. 75)
Affinity DataIC50: 29nMAssay Description:Inhibition of 20S immunoproteasome beta-5i subunit in human PBMC using Ac-ANW-luciferin substrate preincubated for 2 hrs followed by substrate additi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/24/2023
Entry Details
PubMed
TargetProteasome subunit beta type-8(Human)
Merck

Curated by ChEMBL
LigandPNGBDBM388378(US10294246, Compound No. 75)
Affinity DataIC50: 50nMAssay Description:Measurement of LMP7 inhibition is performed in 384 well format based on fluorescence intensity assay.Purified human immunoproteasome (0.25 nM) and se...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/10/2020
Entry Details
US Patent

TargetProteasome subunit beta type-5(Human)
Merck

Curated by ChEMBL
LigandPNGBDBM388378(US10294246, Compound No. 75)
Affinity DataIC50: 1.20E+3nMAssay Description:Inhibition of human 20S proteasome beta5 subunit using Suc-LLVY-AMC as substrate preincubated for 2 hrs followed by substrate addition and measured a...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/24/2023
Entry Details
PubMed
TargetProteasome subunit beta type-5(Human)
Merck

Curated by ChEMBL
LigandPNGBDBM388378(US10294246, Compound No. 75)
Affinity DataIC50: 2.10E+3nMAssay Description:Inhibition of 20S proteasome beta5 subunit in human A549 cells using Suc-LLVY-luciferin substrate preincubated for 2 hrs followed by substrate additi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/24/2023
Entry Details
PubMed
TargetProteasome subunit beta type-5(Human)
Merck

Curated by ChEMBL
LigandPNGBDBM388378(US10294246, Compound No. 75)
Affinity DataIC50: 2.75E+3nMAssay Description:Measurement of Beta5 inhibition is performed in 384 well format based on fluorescence intensity assay.Purified human constitutive proteasome (1.25 nM...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/10/2020
Entry Details
US Patent