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Assay Detail

CHEMBL2150722

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Antagonist activity at Pseudomonas aeruginosa LasB using Abz-Ala-Gly-Leu-Ala-p-Nitro-Benzyl-Amide as substrate incubated for 30 mins prior to substrate addition by FRET assay
19
Total Activities
13
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Pseudomonas aeruginosa
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Elastase (CHEMBL1075146)
Type SINGLE PROTEIN
Organism Pseudomonas aeruginosa (strain ATCC 15692 / PAO1 / 1C / PRS 101 / LMG12228)

Publication

3-Hydroxy-1-alkyl-2-methylpyridine-4(1H)-thiones: Inhibition of the Pseudomonas aeruginosa Virulence Factor LasB.
Garner AL, Struss AK, Fullagar JL, Agrawal A, Moreno AY, Cohen SM, Janda KD.
ACS Med Chem Lett (2012) 3 : 668 -672
PubMed 23181168 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.01 5.56
Activity 6 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2146996 1 5.56
CHEMBL2146995 1 5.48
CHEMBL2146997 1 5.45
CHEMBL2146998 1 5.33
CHEMBL2147001 1 5.28
CHEMBL2146999 1 5.17
CHEMBL2147000 1 5.07
CHEMBL152665 PHENYLACETOHYDROXAMIC ACID 2 4.87
CHEMBL2146994 2 4.79
CHEMBL1650620 2 4.09
CHEMBL1650624 2 4.05
CHEMBL1650623 2 -
CHEMBL1650621 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2146996 IC50 = 2730.0 nM 5.56
CHEMBL2146995 IC50 = 3340.0 nM 5.48
CHEMBL2146997 IC50 = 3580.0 nM 5.45
CHEMBL2146998 IC50 = 4650.0 nM 5.33
CHEMBL2147001 IC50 = 5270.0 nM 5.28
CHEMBL2146999 IC50 = 6720.0 nM 5.17
CHEMBL2147000 IC50 = 8580.0 nM 5.07
CHEMBL152665 PHENYLACETOHYDROXAMIC ACID IC50 = 13600.0 nM 4.87
CHEMBL2146994 IC50 = 16400.0 nM 4.79
CHEMBL1650620 IC50 = 80600.0 nM 4.09
CHEMBL1650624 IC50 = 88500.0 nM 4.05
CHEMBL1650621 IC50 = 220000.0 nM -
CHEMBL1650623 IC50 = 392000.0 nM -
CHEMBL152665 PHENYLACETOHYDROXAMIC ACID Activity - -
CHEMBL2146994 Activity - -
CHEMBL1650620 Activity - -
CHEMBL1650624 Activity - -
CHEMBL1650623 Activity - -
CHEMBL1650621 Activity - -