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Assay Detail

CHEMBL1177097

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

Binding
Inhibition of Stenotrophomonas maltophilia beta lactamase L1 in presence of Zn+ chelator
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Stenotrophomonas maltophilia
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Beta-lactamase L1 (CHEMBL3326)
Type SINGLE PROTEIN
Organism Stenotrophomonas maltophilia

Publication

Mercaptophosphonate compounds as broad-spectrum inhibitors of the metallo-beta-lactamases.
Lassaux P, Hamel M, Gulea M, Delbrück H, Mercuri PS, Horsfall L, Dehareng D, Kupper M, Frère JM, Hoffmann K, Galleni M, Bebrone C.
J Med Chem (2010) 53 : 4862 -4876
PubMed 20527888 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 5.30 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1173797 1 6.40
CHEMBL1173800 1 6.16
CHEMBL1173799 1 5.77
CHEMBL1170425 1 5.40
CHEMBL1173798 1 5.40
CHEMBL1173336 1 4.92
CHEMBL1173337 1 4.85
CHEMBL1170023 DIISOPROPYL MERCAPTO(PHENYL)METHYLPHOSPHONATE 1 4.80
CHEMBL1172743 1 4.75
CHEMBL1170424 1 4.50
CHEMBL1172387 1 -
CHEMBL1173338 1 -
CHEMBL1173339 1 -
CHEMBL1172388 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1173797 Ki = 400.0 nM 6.40
CHEMBL1173800 Ki = 700.0 nM 6.16
CHEMBL1173799 Ki = 1700.0 nM 5.77
CHEMBL1170425 Ki = 4000.0 nM 5.40
CHEMBL1173798 Ki = 4000.0 nM 5.40
CHEMBL1173336 Ki = 12000.0 nM 4.92
CHEMBL1173337 Ki = 14000.0 nM 4.85
CHEMBL1170023 DIISOPROPYL MERCAPTO(PHENYL)METHYLPHOSPHONATE Ki = 16000.0 nM 4.80
CHEMBL1172743 Ki = 18000.0 nM 4.75
CHEMBL1170424 Ki = 32000.0 nM 4.50
CHEMBL1172387 Ki > 250000.0 nM -
CHEMBL1173338 Ki > 50000.0 nM -
CHEMBL1173339 Ki > 40000.0 nM -
CHEMBL1172388 Ki > 40000.0 nM -