Compile Data Set for Download or QSAR
Report error Found 218 Enz. Inhib. hit(s) with Target = 'A5LHX3/O14818/P20618/P25786/P25787/P25788/P25789/P28062/P28065/P28066/P28070/P28072/P28074/P40306/P49720/P49721/P60900/Q8TAA3/Q99436'
LigandPNGBDBM50518761(CHEMBL4573271)
Affinity DataEC50:  2.40E+4nMAssay Description:Stimulation of human 20S proteasome using 11 amino acid FRET peptide as substrate measured every 2 mins over 1 hr by FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50518762(CHEMBL4561568)
Affinity DataEC50:  3.50E+4nMAssay Description:Stimulation of human 20S proteasome using 11 amino acid FRET peptide as substrate measured every 2 mins over 1 hr by FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50054471(cid_6604822 | (5Z,8Z)-Icosa-5,8,11,14-tetraenoic a...)
Affinity DataEC50:  2.80E+4nMAssay Description:Stimulation of human 20S proteasome using 11 amino acid FRET peptide as substrate measured every 2 mins over 1 hr by FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
LigandPNGBDBM50476098(Cinnabaramide G)
Affinity DataIC50: 0.600nMAssay Description:Inhibition of human 20S proteasomeMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2020
Entry Details Article
PubMed
LigandPNGBDBM50234982(CHEMBL4102324)
Affinity DataIC50: 0.920nMAssay 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
In Depth
Date in BDB:
6/25/2023
Entry Details
PubMed
LigandPNGBDBM50476095(CINNABARAMIDE A)
Affinity DataIC50: 1nMAssay Description:Inhibition of human 20S proteasomeMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2020
Entry Details Article
PubMed
LigandPNGBDBM50398608(MARIZOMIB)
Affinity DataIC50: 1.30nMAssay Description:Inhibition of 20S proteasome (unknown origin) by fluorescence based assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/19/2023
Entry Details
PubMed
LigandPNGBDBM50531806(CHEMBL4460323)
Affinity DataIC50: 1.5nMAssay Description:Inhibition of human 20S proteasome preincubated for 15 mins followed by substrate additionMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
LigandPNGBDBM50031442(Alpha-ketocarbonyl derivative | 1N-[4-amino(nitroi...)
Affinity DataIC50: 2nMAssay Description:Compound was evaluated for inhibitory activity against 20S proteasome from human liver and brainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/21/2020
Entry Details Article
PubMed
LigandPNGBDBM50531814(CHEMBL4517600)
Affinity DataIC50: 2.40nMAssay Description:Inhibition of human 20S proteasome preincubated for 15 mins followed by substrate additionMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
LigandPNGBDBM50514365(CHEMBL4587036)
Affinity DataIC50: 2.5nMAssay Description:Inhibition of human 20S proteasome using Suc-LLVY-AMC as substrate measured every 5 mins for 120 mins by fluorescence based assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/21/2021
Entry Details Article
PubMed
LigandPNGBDBM50531815(CHEMBL4444107)
Affinity DataIC50: 3.40nMAssay Description:Inhibition of human 20S proteasome preincubated for 15 mins followed by substrate additionMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
LigandPNGBDBM50603962(CHEMBL5197285)
Affinity DataIC50: 3.40nMAssay 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
In Depth
Date in BDB:
6/25/2023
Entry Details
PubMed
LigandPNGBDBM50531807(CHEMBL4541038)
Affinity DataIC50: 3.60nMAssay Description:Inhibition of human 20S proteasome preincubated for 15 mins followed by substrate additionMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
LigandPNGBDBM50531812(CHEMBL4547405)
Affinity DataIC50: 3.90nMAssay Description:Inhibition of human 20S proteasome preincubated for 15 mins followed by substrate additionMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
LigandPNGBDBM50603940(CHEMBL5171225)
Affinity DataIC50: 4nMAssay 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
In Depth
Date in BDB:
6/25/2023
Entry Details
PubMed
LigandPNGBDBM50514367(CHEMBL4581126)
Affinity DataIC50: 4.30nMAssay Description:Inhibition of human 20S proteasome using Suc-LLVY-AMC as substrate measured every 5 mins for 120 mins by fluorescence based assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/21/2021
Entry Details Article
PubMed
LigandPNGBDBM50531813(CHEMBL4542373)
Affinity DataIC50: 4.60nMAssay Description:Inhibition of human 20S proteasome preincubated for 15 mins followed by substrate additionMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
LigandPNGBDBM50531826(CHEMBL4558648)
Affinity DataIC50: 4.60nMAssay Description:Inhibition of human 20S proteasome preincubated for 15 mins followed by substrate additionMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
LigandPNGBDBM50531808(CHEMBL4467618)
Affinity DataIC50: 4.80nMAssay Description:Inhibition of human 20S proteasome preincubated for 15 mins followed by substrate additionMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
LigandPNGBDBM50603963(CHEMBL5186240)
Affinity DataIC50: 5.20nMAssay 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
In Depth
Date in BDB:
6/25/2023
Entry Details
PubMed
LigandPNGBDBM50031440(Alpha-ketocarbonyl derivative | 1N-[4-amino(nitroi...)
Affinity DataIC50: 6nMAssay Description:Compound was evaluated for inhibitory activity against 20S proteasome from human liver and brainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/21/2020
Entry Details Article
PubMed
LigandPNGBDBM50476097(Cinnabaramide F)
Affinity DataIC50: 6nMAssay Description:Inhibition of human 20S proteasomeMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2020
Entry Details Article
PubMed
LigandPNGBDBM50514366(CHEMBL4447701)
Affinity DataIC50: 6.40nMAssay Description:Inhibition of human 20S proteasome using Suc-LLVY-AMC as substrate measured every 5 mins for 120 mins by fluorescence based assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/21/2021
Entry Details Article
PubMed
LigandPNGBDBM50531825(CHEMBL4435814)
Affinity DataIC50: 6.40nMAssay Description:Inhibition of human 20S proteasome preincubated for 15 mins followed by substrate additionMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
LigandPNGBDBM50531816(CHEMBL4436430)
Affinity DataIC50: 6.5nMAssay Description:Inhibition of human 20S proteasome preincubated for 15 mins followed by substrate additionMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
LigandPNGBDBM50069989(CHEMBL325041 | (R)-3-methyl-1-((S)-3-phenyl-2-(pyr...)
Affinity DataIC50: 6.90nMAssay 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
In Depth
Date in BDB:
6/25/2023
Entry Details
PubMed
LigandPNGBDBM50469762(CHEMBL432281)
Affinity DataIC50: 7nMAssay Description:Tested in vitro for inhibition of chymotrypsin like activity of purified human 20S proteasomeMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/20/2020
Entry Details Article
PubMed
LigandPNGBDBM50475041(CHEMBL181131 | TP-104)
Affinity DataIC50: 7nMAssay Description:Inhibitory concentration to inhibit chymotrypsin-like activity of 20S proteasome prepared from human leukemia HL-60 cells was determinedMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2020
Entry Details Article
PubMed
LigandPNGBDBM50277889(CHEMBL451887 | CARFILZOMIB)
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
In Depth
Date in BDB:
8/23/2022
Entry Details Article
PubMed
LigandPNGBDBM50603953(CHEMBL5202627)
Affinity DataIC50: 7nMAssay 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
In Depth
Date in BDB:
6/25/2023
Entry Details
PubMed
LigandPNGBDBM50603957(CHEMBL5208573)
Affinity DataIC50: 7.20nMAssay 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
In Depth
Date in BDB:
6/25/2023
Entry Details
PubMed
LigandPNGBDBM50531811(CHEMBL4559271)
Affinity DataIC50: 7.70nMAssay Description:Inhibition of human 20S proteasome preincubated for 15 mins followed by substrate additionMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
LigandPNGBDBM50603956(CHEMBL5172645)
Affinity DataIC50: 8.10nMAssay 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
In Depth
Date in BDB:
6/25/2023
Entry Details
PubMed
LigandPNGBDBM50603952(CHEMBL5179570)
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
In Depth
Date in BDB:
6/25/2023
Entry Details
PubMed
LigandPNGBDBM50277889(CHEMBL451887 | CARFILZOMIB)
Affinity DataIC50: 8.60nMAssay Description:Inhibition of human 20S proteasome preincubated for 15 mins followed by substrate additionMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
LigandPNGBDBM50603941(CHEMBL5209077)
Affinity DataIC50: 8.60nMAssay 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
In Depth
Date in BDB:
6/25/2023
Entry Details
PubMed
LigandPNGBDBM50603960(CHEMBL5173459)
Affinity DataIC50: 8.90nMAssay 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
In Depth
Date in BDB:
6/25/2023
Entry Details
PubMed
LigandPNGBDBM50603951(CHEMBL5188065)
Affinity DataIC50: 9.30nMAssay 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
In Depth
Date in BDB:
6/25/2023
Entry Details
PubMed
LigandPNGBDBM50603961(CHEMBL5196378)
Affinity DataIC50: 9.30nMAssay 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
In Depth
Date in BDB:
6/25/2023
Entry Details
PubMed
LigandPNGBDBM50531833(CHEMBL4572638)
Affinity DataIC50: 9.40nMAssay Description:Inhibition of human 20S proteasome preincubated for 15 mins followed by substrate additionMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
LigandPNGBDBM50603954(CHEMBL5201055)
Affinity DataIC50: 9.40nMAssay 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
In Depth
Date in BDB:
6/25/2023
Entry Details
PubMed
LigandPNGBDBM50531832(CHEMBL4441018)
Affinity DataIC50: 9.5nMAssay Description:Inhibition of human 20S proteasome preincubated for 15 mins followed by substrate additionMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
LigandPNGBDBM50277889(CHEMBL451887 | CARFILZOMIB)
Affinity DataIC50: 10nMAssay Description:Inhibition of 20S proteasome activity in human ANBL-6 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/16/2020
Entry Details Article
PubMed
LigandPNGBDBM50069989(CHEMBL325041 | (R)-3-methyl-1-((S)-3-phenyl-2-(pyr...)
Affinity DataIC50: 11nMAssay Description:Inhibition of human 20S proteasome preincubated for 15 mins followed by substrate additionMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
LigandPNGBDBM50476096(Cinnabaramide C)
Affinity DataIC50: 12nMAssay Description:Inhibition of human 20S proteasomeMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2020
Entry Details Article
PubMed
LigandPNGBDBM50475039(CHEMBL181025 | TP-103)
Affinity DataIC50: 14nMAssay Description:Inhibitory concentration to inhibit chymotrypsin-like activity of 20S proteasome prepared from human leukemia HL-60 cells was determinedMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2020
Entry Details Article
PubMed
LigandPNGBDBM50531809(CHEMBL4578081)
Affinity DataIC50: 14nMAssay Description:Inhibition of human 20S proteasome preincubated for 15 mins followed by substrate additionMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
LigandPNGBDBM50398609(CHEMBL2141296 | MLN2238 | Ixazomib | NINLARO | IXA...)
Affinity DataIC50: 15nMAssay Description:Inhibition of human 20S proteasome using Suc-LLVY-AMC as substrate measured every 5 mins for 120 mins by fluorescence based assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/21/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50531822(CHEMBL4443333)
Affinity DataIC50: 15nMAssay Description:Inhibition of human 20S proteasome preincubated for 15 mins followed by substrate additionMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
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