Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1960110

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

Binding
Inhibition of Pseudomonas aeruginosa LpxC using UDP-3-O-(R-hydroxydecanoyl)-N-acetylglucosamine incubated for 30 mins prior to substrate addition measured after 60 mins by mass spectrophotometry
ChEMBL ↗
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

UDP-3-O-acyl-N-acetylglucosamine deacetylase (CHEMBL3855) ↗
Type SINGLE PROTEIN
Organism Pseudomonas aeruginosa (strain ATCC 15692 / PAO1 / 1C / PRS 101 / LMG12228)

Publication

Potent inhibitors of LpxC for the treatment of Gram-negative infections.
Brown MF, Reilly U, Abramite JA, Arcari JT, Oliver R, Barham RA, Che Y, Chen JM, Collantes EM, Chung SW, Desbonnet C, Doty J, Doroski M, Engtrakul JJ, Harris TM, Huband M, Knafels JD, Leach KL, Liu S, Marfat A, Marra A, McElroy E, Melnick M, Menard CA, Montgomery JI, Mullins L, Noe MC, O'Donnell J, Penzien J, Plummer MS, Price LM, Shanmugasundaram V, Thoma C, Uccello DP, Warmus JS, Wishka DG.
J Med Chem (2012) 55 : 914 -923
PubMed 22175825 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 39 8.05 9.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1956131 — — 1 9.19
CHEMBL1956145 — — 1 8.92
CHEMBL1956104 — — 1 8.87
CHEMBL1956115 — — 1 8.86
CHEMBL1956130 — — 1 8.76
CHEMBL1956148 — — 1 8.73
CHEMBL1956125 — — 1 8.45
CHEMBL1956146 — — 1 8.43
CHEMBL1956134 — — 1 8.29
CHEMBL1956126 — — 1 8.17
CHEMBL1956105 — — 1 8.15
CHEMBL1956120 — — 1 8.04
CHEMBL1956143 — — 1 8.02
CHEMBL1956136 — — 1 8.00
CHEMBL1956121 — — 1 7.92
CHEMBL1956142 — — 1 7.90
CHEMBL1956141 — — 1 7.89
CHEMBL1956117 — — 1 7.86
CHEMBL1956137 — — 1 7.67
CHEMBL1956140 — — 1 7.67
CHEMBL1956127 — — 1 7.66
CHEMBL1956123 — — 1 7.58
CHEMBL1956128 — — 1 7.56
CHEMBL1956114 — — 1 7.53
CHEMBL1956113 — — 1 7.52
CHEMBL1956122 — — 1 7.50
CHEMBL1956139 — — 1 7.13
CHEMBL1956138 — — 1 7.03
CHEMBL1956144 — — 1 -
CHEMBL1956147 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1956131 — IC50 = 0.64 nM 9.19
CHEMBL1956145 — IC50 = 1.2 nM 8.92
CHEMBL1956104 — IC50 = 1.36 nM 8.87
CHEMBL1956115 — IC50 = 1.37 nM 8.86
CHEMBL1956130 — IC50 = 1.74 nM 8.76
CHEMBL1956148 — IC50 = 1.85 nM 8.73
CHEMBL1956125 — IC50 = 3.54 nM 8.45
CHEMBL1956146 — IC50 = 3.68 nM 8.43
CHEMBL1956134 — IC50 = 5.16 nM 8.29
CHEMBL1956126 — IC50 = 6.78 nM 8.17
CHEMBL1956105 — IC50 = 7.04 nM 8.15
CHEMBL1956120 — IC50 = 9.04 nM 8.04
CHEMBL1956143 — IC50 = 9.49 nM 8.02
CHEMBL1956136 — IC50 = 10.1 nM 8.00
CHEMBL1956121 — IC50 = 11.9 nM 7.92
CHEMBL1956142 — IC50 = 12.7 nM 7.90
CHEMBL1956141 — IC50 = 12.9 nM 7.89
CHEMBL1956117 — IC50 = 13.8 nM 7.86
CHEMBL1956140 — IC50 = 21.2 nM 7.67
CHEMBL1956137 — IC50 = 21.6 nM 7.67
CHEMBL1956127 — IC50 = 22.1 nM 7.66
CHEMBL1956123 — IC50 = 26.1 nM 7.58
CHEMBL1956128 — IC50 = 27.8 nM 7.56
CHEMBL1956114 — IC50 = 29.7 nM 7.53
CHEMBL1956113 — IC50 = 30.4 nM 7.52
CHEMBL1956122 — IC50 = 31.4 nM 7.50
CHEMBL1956139 — IC50 = 73.6 nM 7.13
CHEMBL1956138 — IC50 = 92.7 nM 7.03
CHEMBL1956118 — IC50 > 67.9 nM -
CHEMBL1956119 — IC50 > 92.5 nM -
CHEMBL1956135 — IC50 > 100.0 nM -
CHEMBL1956133 — IC50 > 100.0 nM -
CHEMBL1956116 — IC50 > 95.2 nM -
CHEMBL1956124 — IC50 > 100.0 nM -
CHEMBL1956129 — IC50 < 1.05 nM -
CHEMBL1956132 — IC50 < 2.47 nM -
CHEMBL260091 — IC50 < 2.05 nM -
CHEMBL1956147 — IC50 > 92.5 nM -
CHEMBL1956144 — IC50 < 2.13 nM -