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Assay Detail

CHEMBL5247752

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Binding
Inhibition of bacteria KPC-2 assessed as apparent inhibition constant using nitrocefin as substrate
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Strategic Approaches to Overcome Resistance against Gram-Negative Pathogens Using β-Lactamase Inhibitors and β-Lactam Enhancers: Activity of Three Novel Diazabicyclooctanes WCK 5153, Zidebactam (WCK 5107), and WCK 4234.
Papp-Wallace KM, Nguyen NQ, Jacobs MR, Bethel CR, Barnes MD, Kumar V, Bajaksouzian S, Rudin SD, Rather PN, Bhavsar S, Ravikumar T, Deshpande PK, Patil V, Yeole R, Bhagwat SS, Patel MV, van den Akker F, Bonomo RA.
J Med Chem (2018) 61 : 4067 -4086
PubMed 29627985 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 5.73 6.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4450418 1 6.50
CHEMBL2107817 AVIBACTAM SODIUM 4.0 1 6.05
CHEMBL3301605 RELEBACTAM 4.0 1 5.66
CHEMBL4533605 ZIDEBACTAM 3.0 1 5.35
CHEMBL5288189 1 5.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4450418 Ki = 320.0 nM 6.50
CHEMBL2107817 AVIBACTAM SODIUM Ki = 900.0 nM 6.05
CHEMBL3301605 RELEBACTAM Ki = 2200.0 nM 5.66
CHEMBL4533605 ZIDEBACTAM Ki = 4500.0 nM 5.35
CHEMBL5288189 Ki = 7800.0 nM 5.11