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Assay Detail

CHEMBL4706278

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

Binding
Inhibition of beta lactamase TEM-1 in Enterobacter cloacae assessed as decrease in enzyme activity using nitrocefin as substrate preincubated for 10 mins followed by substrate addition measured for 10 mins by fluorescence plate reader analysis
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of ANT3310, a Novel Broad-Spectrum Serine β-Lactamase Inhibitor of the Diazabicyclooctane Class, Which Strongly Potentiates Meropenem Activity against Carbapenem-Resistant Enterobacterales and Acinetobacter baumannii.
Davies DT,Leiris S,Zalacain M,Sprynski N,Castandet J,Bousquet J,Lozano C,Llanos A,Alibaud L,Vasa S,Pattipati R,Valige R,Kummari B,Pothukanuri S,De Piano C,Morrissey I,Holden K,Warn P,Marcoccia F,Benvenuti M,Pozzi C,Tassone G,Mangani S,Docquier JD,Pallin D,Elliot R,Lemonnier M,Everett M
J Med Chem (2020) 63 : 15802 -15820
PubMed 33306385 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.26 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4747858 1 9.00
CHEMBL4747415 1 9.00
CHEMBL4753698 1 9.00
CHEMBL1689063 AVIBACTAM 4.0 1 8.30
CHEMBL4760205 1 7.58
CHEMBL4450418 1 7.17
CHEMBL4751955 1 6.93
CHEMBL4758199 1 6.87
CHEMBL4783595 1 6.68
CHEMBL4743152 1 6.67
CHEMBL4784410 1 6.57
CHEMBL4754954 1 6.39
CHEMBL4762743 1 6.31
CHEMBL4784710 1 6.29
CHEMBL4753560 1 6.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4747858 IC50 = 1.0 nM 9.00
CHEMBL4747415 IC50 = 1.0 nM 9.00
CHEMBL4753698 IC50 = 1.0 nM 9.00
CHEMBL1689063 AVIBACTAM IC50 = 5.0 nM 8.30
CHEMBL4760205 IC50 = 26.0 nM 7.58
CHEMBL4450418 IC50 = 67.0 nM 7.17
CHEMBL4751955 IC50 = 117.0 nM 6.93
CHEMBL4758199 IC50 = 135.0 nM 6.87
CHEMBL4783595 IC50 = 208.0 nM 6.68
CHEMBL4743152 IC50 = 216.0 nM 6.67
CHEMBL4784410 IC50 = 267.0 nM 6.57
CHEMBL4754954 IC50 = 403.0 nM 6.39
CHEMBL4762743 IC50 = 492.0 nM 6.31
CHEMBL4784710 IC50 = 511.0 nM 6.29
CHEMBL4753560 IC50 = 810.0 nM 6.09