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Assay Detail

CHEMBL1216774

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Binding
Activity at Escherichia coli DH10B beta-lactamase KPC-2 by diode array spectrophotometry
8
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Escherichia coli str. K-12 substr. DH10B
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Inhibitor resistance in the KPC-2 beta-lactamase, a preeminent property of this class A beta-lactamase.
Papp-Wallace KM, Bethel CR, Distler AM, Kasuboski C, Taracila M, Bonomo RA.
Antimicrob Agents Chemother (2010) 54 : 890 -897
PubMed 20008772 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kcat 4 - -
Ki 4 4.94 5.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL480517 NITROCEFIN -1.0 2 5.30
CHEMBL702 PIPERACILLIN 4.0 2 4.80
CHEMBL148 IMIPENEM ANHYDROUS 4.0 2 4.72
CHEMBL1730 CEFOTAXIME 4.0 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL480517 NITROCEFIN Ki = 5000.0 nM 5.30
CHEMBL702 PIPERACILLIN Ki = 16000.0 nM 4.80
CHEMBL148 IMIPENEM ANHYDROUS Ki = 19000.0 nM 4.72
CHEMBL480517 NITROCEFIN Kcat = 30.0 /s -
CHEMBL148 IMIPENEM ANHYDROUS Kcat = 19.0 /s -
CHEMBL1730 CEFOTAXIME Kcat = 78.0 /s -
CHEMBL702 PIPERACILLIN Kcat = 17.0 /s -
CHEMBL1730 CEFOTAXIME Ki = 120000.0 nM -