BDBM50277889 CARFILZOMIB::CHEMBL451887
SMILES CC(C)C[C@H](NC(=O)[C@H](CCc1ccccc1)NC(=O)CN1CCOCC1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)[C@@]1(C)CO1
InChI Key InChIKey=BLMPQMFVWMYDKT-NZTKNTHTSA-N
Data 44 IC50
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 44 hits for monomerid = 50277889
Affinity DataIC50: 8.60nMAssay Description:The assay was carried out in 50 uL volume, where 1 uL compound was added to 10 uL purified human proteasome (25 ug/mL) and incubated for 15 min and t...More data for this Ligand-Target Pair
Affinity DataIC50: 2.10nMAssay 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
Affinity DataIC50: >3.00E+4nMAssay Description:Inhibition of recombinant cathepsin G (unknown origin) using Suc-Ala-Ala-Pro-Phe-AMC as substrate by spectrofluorometer analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 1.10E+4nMAssay Description:Inhibition of recombinant cathepsin B (unknown origin) using Z-Leu-Arg-AMC as substrate by spectrofluorometer analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 8.60nMAssay Description:Inhibition of chymotrypsin-like enzyme activity of purified human 20S proteasome using Suc-Leu-Leu-Val-Tyr-AMC as substrate by fluorescence methodMore data for this Ligand-Target Pair
Affinity DataIC50: 14nMAssay Description:Inhibition of chymotrypsin-like activity of LMP7 immunoproteasome by proteasome active site ELISAMore data for this Ligand-Target Pair
Affinity DataIC50: 8.40nMAssay Description:Inhibition of chymotrypsin-like activity of human 20S proteasome preincubated for 15 mins followed by addition of Suc-Leu-Leu-Val-Tyr-AMC as substrat...More data for this Ligand-Target Pair
Affinity DataIC50: 8.40nMAssay Description:Inhibition of chymotrypsin-like activity of human 20S proteasome pretreated for 15 mins followed by Suc-Leu-Leu-Val-Tyr-AMC substrate addition by flu...More data for this Ligand-Target Pair
Affinity DataIC50: 150nMAssay Description:Inhibition of GSTO1-1 (unknown origin) pre-incubated for 1 hr before GSH addition by CDNB-GSH conjugation assayMore data for this Ligand-Target Pair
TargetA5LHX3/O14818/P20618/P25786/P25787/P25788/P25789/P28062/P28065/P28066/P28070/P28072/P28074/P40306/P49720/P49721/P60900/Q8TAA3/Q99436(Homo sapiens (Human))
Monash University
Curated by ChEMBL
Monash University
Curated by ChEMBL
Affinity DataIC50: <10nMAssay Description:Inhibition of 20S proteasome activity in human ANBL-6 cellsMore data for this Ligand-Target Pair
Affinity DataIC50: 9.60nMAssay Description:Inhibition of 20S proteasome beta5 subunit in human Jurkat cell lysate using Suc-LLVY-AMC as substrate pretreated for 30 mins followed by substrate a...More data for this Ligand-Target Pair
TargetProteasome subunit beta type-2(Homo sapiens (Human))
New Mexico Institute Of Mining And Technology
Curated by ChEMBL
New Mexico Institute Of Mining And Technology
Curated by ChEMBL
Affinity DataIC50: 203nMAssay Description:Inhibition of 20S proteasome beta2 subunit in human Jurkat cell lysate using Suc-RLR-AMC as substrate pretreated for 30 mins followed by substrate ad...More data for this Ligand-Target Pair
Affinity DataIC50: 33nMAssay Description:Inhibition of human immunoproteasome beta5 subunit using Suc-RLR-AMC as substrate pretreated for 30 mins followed by substrate addition and measured ...More data for this Ligand-Target Pair
TargetmRNA cap guanine-N7 methyltransferase(Homo sapiens)
New Mexico Institute Of Mining And Technology
Curated by ChEMBL
New Mexico Institute Of Mining And Technology
Curated by ChEMBL
Affinity DataIC50: >1.00E+3nMAssay Description:Inhibition of yeast 20S proteasome beta2 subunit using SUC-RLR-AMC as substrate pretreated for 30 mins followed by substrate addition and measured af...More data for this Ligand-Target Pair
TargetmRNA cap guanine-N7 methyltransferase(Homo sapiens)
New Mexico Institute Of Mining And Technology
Curated by ChEMBL
New Mexico Institute Of Mining And Technology
Curated by ChEMBL
Affinity DataIC50: >1.00E+3nMAssay Description:Inhibition of yeast 20S proteasome beta1 subunit using fluorescent substrate pretreated for 30 mins followed by substrate addition and measured after...More data for this Ligand-Target Pair
Affinity DataIC50: 2.70nMAssay Description:Inhibition of 20S proteasome beta5 subunit in human RPMI8226 cell lysate using Suc-LLVY-AMC as substrate pretreated for 1 hr followed by substrate ad...More data for this Ligand-Target Pair
Affinity DataIC50: 2.94E+3nMAssay Description:Inhibition of purified human 20S immunoproteasome beta1 subunit using Ac-Pro-Ala-Leu-AMC as substrate pretreated for 1 hr followed by substrate addit...More data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Nanjing Forestry University
Curated by ChEMBL
Nanjing Forestry University
Curated by ChEMBL
Affinity DataIC50: 9.21E+4nMAssay Description:Inhibition of human ERG in HEK293 cells assessed as effect on QT intervalMore data for this Ligand-Target Pair
Affinity DataIC50: 24nMAssay Description:Inhibition of human chymotrypsin-like activity of 20S proteasome using Suc-LLVY-AMC as substrate pre-incubated for 10 mins followed by substrate addi...More data for this Ligand-Target Pair
TargetProteasome subunit beta type-2(Homo sapiens (Human))
New Mexico Institute Of Mining And Technology
Curated by ChEMBL
New Mexico Institute Of Mining And Technology
Curated by ChEMBL
Affinity DataIC50: 825nMAssay Description:Inhibition of human trypsin-like activity of 20S constitutive proteasome using Z-VLR-AMC as substrate preincubated for 15 mins followed by substrate ...More data for this Ligand-Target Pair
Affinity DataIC50: 1.45E+3nMAssay Description:Inhibition of human caspase-like activity of 20S constitutive proteasome preincubated for 15 mins followed by substrate addition by fluorescence assa...More data for this Ligand-Target Pair
Affinity DataIC50: 27nMAssay Description:Inhibition of 20S immunoproteasome LMP7 (unknown origin) using Ac-ANW-AMC as substrate preincubated for 15 mins followed by substrate addition by flu...More data for this Ligand-Target Pair
Affinity DataIC50: 5nMAssay Description:Inhibition of human chymotrypsin-like activity of 20S constitutive proteasome using Suc-LLVY-AMC as substrate preincubated for 15 mins followed by su...More data for this Ligand-Target Pair
TargetProteasome subunit beta type-2(Homo sapiens (Human))
New Mexico Institute Of Mining And Technology
Curated by ChEMBL
New Mexico Institute Of Mining And Technology
Curated by ChEMBL
Affinity DataIC50: 1.81E+3nMAssay Description:Inhibition of human 20s proteasome subunit beta2 caspase-like activity using Z-LLE-AMC as substrate preincubated for 15 mins followed by substrate ad...More data for this Ligand-Target Pair
Affinity DataIC50: 34nMAssay Description:Inhibition of human 20s immunoproteasome beta5i activity using Suc-LLVY-AMC as substrate preincubated for 15 mins followed by substrate additionMore data for this Ligand-Target Pair
Affinity DataIC50: 8.60nMAssay Description:Inhibition of human 20s constitutive proteasome beta5 chymotrypsin-like activity using Suc-LLVY-AMC as substrate preincubated for 15 mins followed by...More data for this Ligand-Target Pair
TargetA5LHX3/O14818/P20618/P25786/P25787/P25788/P25789/P28062/P28065/P28066/P28070/P28072/P28074/P40306/P49720/P49721/P60900/Q8TAA3/Q99436(Homo sapiens (Human))
Monash University
Curated by ChEMBL
Monash University
Curated by ChEMBL
Affinity DataIC50: 8.60nMAssay Description:Inhibition of human 20S proteasome preincubated for 15 mins followed by substrate additionMore data for this Ligand-Target Pair
Affinity DataIC50: 2.40E+3nMAssay Description:Inhibition of 20S proteasome beta 1c (unknown origin) after 1 hr by fluorescence based assayMore data for this Ligand-Target Pair
Affinity DataIC50: 2.42E+3nMAssay Description:Inhibition of 20S proteasome beta 1i (unknown origin) after 1 hr by fluorescence based assayMore data for this Ligand-Target Pair
TargetProteasome subunit beta type-2(Homo sapiens (Human))
New Mexico Institute Of Mining And Technology
Curated by ChEMBL
New Mexico Institute Of Mining And Technology
Curated by ChEMBL
Affinity DataIC50: 3.60E+3nMAssay Description:Inhibition of 20S proteasome beta 2c (unknown origin) after 1 hr by fluorescence based assayMore data for this Ligand-Target Pair
Affinity DataIC50: 7nMAssay Description:Inhibition of human hepatic cell derived 20s constitutive proteasome beta5 chymotrypsin-like activity using Suc-WLA-AMC as substrate preincubated for...More data for this Ligand-Target Pair
Affinity DataIC50: 7nMAssay Description:Inhibition of human hepatic cell derived 20s constitutive proteasome beta5 chymotrypsin-like activity using Suc-WLA-AMC as substrate preincubated for...More data for this Ligand-Target Pair
Affinity DataIC50: 6nMAssay Description:Inhibition of 20S proteasome beta 5c (unknown origin) after 1 hr by fluorescence based assayMore data for this Ligand-Target Pair
Affinity DataIC50: 620nMAssay Description:Inhibition of 20S proteasome beta 2i (unknown origin) after 1 hr by fluorescence based assayMore data for this Ligand-Target Pair
Affinity DataIC50: 33nMAssay Description:Inhibition of 20S proteasome beta 5i (unknown origin) after 1 hr by fluorescence based assayMore data for this Ligand-Target Pair
Affinity DataIC50: 8.40nMAssay Description:Inhibition of chymotrypsin-like activity of human 20S proteasome using Suc-Leu-Leu-Val-Tyr-AMC as substrate preincubated for 15 mins followed by subs...More data for this Ligand-Target Pair
TargetA5LHX3/O14818/P20618/P25786/P25787/P25788/P25789/P28062/P28065/P28066/P28070/P28072/P28074/P40306/P49720/P49721/P60900/Q8TAA3/Q99436(Homo sapiens (Human))
Monash University
Curated by ChEMBL
Monash University
Curated by ChEMBL
Affinity DataIC50: 7nMAssay Description:Inhibition of human 20S proteasome chymotrypsin-like activity in human RPMI-8226 cells using Suc-LLVY-AMC as fluorogenic substrate incubated for 3 hr...More data for this Ligand-Target Pair
TargetA5LHX3/O14818/P20618/P25786/P25787/P25788/P25789/P28062/P28065/P28066/P28070/P28072/P28074/P40306/P49720/P49721/P60900/Q8TAA3/Q99436(Homo sapiens (Human))
Monash University
Curated by ChEMBL
Monash University
Curated by ChEMBL
Affinity DataIC50: 270nMAssay Description:Inhibition of human 20S proteasome chymotrypsin-like activity in human RPMI-8226 cells overexpressing ABCB1 using Suc-LLVY-AMC as fluorogenic substra...More data for this Ligand-Target Pair
Affinity DataIC50: 69nMAssay Description:Inhibition of human 20S immunoproteasome beta-1i subunit using (Ac-PAL)2R110 as substrate preincubated for 2 hrs followed by substrate addition and m...More data for this Ligand-Target Pair
Affinity DataIC50: 13nMAssay Description:Inhibition of human 20S immunoproteasome beta-2i subunit using Ac-RLR-AMC as substrate preincubated for 2 hrs followed by substrate addition and meas...More data for this Ligand-Target Pair
Affinity DataIC50: 3.20nMAssay 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
Affinity DataIC50: 890nMAssay Description:Inhibition of human 20S immunoproteasome beta1 subunit using Ac-nLPnLD-AMC as substrate preincubated for 2 hrs followed by substrate addition and mea...More data for this Ligand-Target Pair
Affinity DataIC50: 43nMAssay Description:Inhibition of human 20S proteasome beta2 subunit using Ac-RLR-AMC as substrate preincubated for 2 hrs followed by substrate addition and measured aft...More data for this Ligand-Target Pair
Affinity DataIC50: >3.00E+4nMAssay Description:Inhibition of recombinant cathepsin A (unknown origin) using Mca-Arg-Pro-Pro-Gly-Phe-Ser-Ala-Phe-Lys(Dnp)-OH as substrate incubated with enzyme for 5...More data for this Ligand-Target Pair