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Assay Detail

CHEMBL3117139

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

Binding
Inhibition of beta-lactamase AmpC in Pseudomonas aeruginosa assessed as inhibition of hydrolysis of nitrocefin
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Pseudomonas aeruginosa
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of MK-7655, a β-lactamase inhibitor for combination with Primaxin®.
Blizzard TA, Chen H, Kim S, Wu J, Bodner R, Gude C, Imbriglio J, Young K, Park YW, Ogawa A, Raghoobar S, Hairston N, Painter RE, Wisniewski D, Scapin G, Fitzgerald P, Sharma N, Lu J, Ha S, Hermes J, Hammond ML.
Bioorg Med Chem Lett (2014) 24 : 780 -785
PubMed 24433862 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.29 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3112748 1 8.92
CHEMBL3112749 1 8.52
CHEMBL3112746 1 8.22
CHEMBL3112591 1 8.10
CHEMBL3112745 1 8.02
CHEMBL3112752 1 7.96
CHEMBL3112751 1 7.96
CHEMBL3112753 1 7.52
CHEMBL3112747 1 7.43
CHEMBL3112756 1 7.16
CHEMBL3112742 1 6.85
CHEMBL3112755 1 6.77
CHEMBL3112750 1 6.68
CHEMBL3112754 1 6.54
CHEMBL3301605 RELEBACTAM 4.0 1 6.33
CHEMBL3112744 1 6.30
CHEMBL3112757 1 6.28
CHEMBL3112743 1 5.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3112748 IC50 = 1.2 nM 8.92
CHEMBL3112749 IC50 = 3.0 nM 8.52
CHEMBL3112746 IC50 = 6.0 nM 8.22
CHEMBL3112591 IC50 = 8.0 nM 8.10
CHEMBL3112745 IC50 = 9.5 nM 8.02
CHEMBL3112752 IC50 = 11.0 nM 7.96
CHEMBL3112751 IC50 = 11.0 nM 7.96
CHEMBL3112753 IC50 = 30.0 nM 7.52
CHEMBL3112747 IC50 = 37.0 nM 7.43
CHEMBL3112756 IC50 = 69.0 nM 7.16
CHEMBL3112742 IC50 = 140.0 nM 6.85
CHEMBL3112755 IC50 = 170.0 nM 6.77
CHEMBL3112750 IC50 = 210.0 nM 6.68
CHEMBL3112754 IC50 = 290.0 nM 6.54
CHEMBL3301605 RELEBACTAM IC50 = 465.0 nM 6.33
CHEMBL3112744 IC50 = 500.0 nM 6.30
CHEMBL3112757 IC50 = 520.0 nM 6.28
CHEMBL3112743 IC50 = 1900.0 nM 5.72