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Assay Detail

CHEMBL901565

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

Binding
Inhibition of Escherichia coli beta-lactamase
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Escherichia coli
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Beta-lactamase TEM (CHEMBL2065)
Type SINGLE PROTEIN
Organism Escherichia coli

Publication

Optimizing cell permeation of an antibiotic resistance inhibitor for improved efficacy.
Venturelli A, Tondi D, Cancian L, Morandi F, Cannazza G, Segatore B, Prati F, Amicosante G, Shoichet BK, Costi MP.
J Med Chem (2007) 50 : 5644 -5654
PubMed 17956081 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 6.90 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL396872 1 8.00
CHEMBL34964 1 7.57
CHEMBL235293 1 7.55
CHEMBL235526 1 7.55
CHEMBL238243 1 7.52
CHEMBL397522 1 7.52
CHEMBL235073 1 7.43
CHEMBL235292 1 7.43
CHEMBL395398 1 7.37
CHEMBL235308 1 7.35
CHEMBL236203 1 7.10
CHEMBL395186 1 7.09
CHEMBL237390 1 7.08
CHEMBL235951 1 6.77
CHEMBL235523 1 6.60
CHEMBL396889 1 6.60
CHEMBL396871 1 6.60
CHEMBL396390 1 6.58
CHEMBL235291 1 6.35
CHEMBL237181 1 6.22
CHEMBL391537 1 6.10
CHEMBL235097 1 6.00
CHEMBL398112 1 5.70
CHEMBL236759 1 5.60
CHEMBL235524 1 -
CHEMBL235508 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL396872 Ki = 10.0 nM 8.00
CHEMBL34964 Ki = 27.0 nM 7.57
CHEMBL235293 Ki = 28.0 nM 7.55
CHEMBL235526 Ki = 28.0 nM 7.55
CHEMBL238243 Ki = 30.0 nM 7.52
CHEMBL397522 Ki = 30.0 nM 7.52
CHEMBL235073 Ki = 37.0 nM 7.43
CHEMBL235292 Ki = 37.0 nM 7.43
CHEMBL395398 Ki = 43.0 nM 7.37
CHEMBL235308 Ki = 45.0 nM 7.35
CHEMBL236203 Ki = 80.0 nM 7.10
CHEMBL395186 Ki = 82.0 nM 7.09
CHEMBL237390 Ki = 83.0 nM 7.08
CHEMBL235951 Ki = 170.0 nM 6.77
CHEMBL235523 Ki = 250.0 nM 6.60
CHEMBL396889 Ki = 250.0 nM 6.60
CHEMBL396871 Ki = 250.0 nM 6.60
CHEMBL396390 Ki = 260.0 nM 6.58
CHEMBL235291 Ki = 450.0 nM 6.35
CHEMBL237181 Ki = 600.0 nM 6.22
CHEMBL391537 Ki = 800.0 nM 6.10
CHEMBL235097 Ki = 1000.0 nM 6.00
CHEMBL398112 Ki = 2000.0 nM 5.70
CHEMBL236759 Ki = 2500.0 nM 5.60
CHEMBL235524 Ki - -
CHEMBL235508 Ki - -