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Assay Detail

CHEMBL649554

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Binding
Inhibitory activity against Escherichia coli AmpC beta-lactamase.
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Beta-lactamase (CHEMBL2026)
Type SINGLE PROTEIN
Organism Escherichia coli K-12

Publication

Structure-based enhancement of boronic acid-based inhibitors of AmpC beta-lactamase.
Weston GS, Blázquez J, Baquero F, Shoichet BK.
J Med Chem (1998) 41 : 4577 -4586
PubMed 9804697 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 37 5.53 7.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL34964 1 7.57
CHEMBL109227 1 6.70
CHEMBL143399 1 6.66
CHEMBL142592 1 6.39
CHEMBL334931 1 6.30
CHEMBL342173 1 6.11
CHEMBL336239 1 5.96
CHEMBL140740 M(DANSYLAMIDOPHENYL)BORONIC ACID 1 5.89
CHEMBL140723 1 5.85
CHEMBL139713 1 5.80
CHEMBL20945 1 5.77
CHEMBL141272 1 5.60
CHEMBL82324 1 5.54
CHEMBL140254 1 5.54
CHEMBL143654 1 5.52
CHEMBL20866 1 5.44
CHEMBL334932 1 5.42
CHEMBL140916 1 5.41
CHEMBL139928 1 5.38
CHEMBL140780 TOLYL BORONIC ACID 1 5.27
CHEMBL140747 1 5.23
CHEMBL21427 1 5.23
CHEMBL344890 1 5.19
CHEMBL140467 1 5.16
CHEMBL20852 1 5.14
CHEMBL141079 1 5.07
CHEMBL21485 PHENYLBORONIC ACID 1 4.98
CHEMBL342460 1 4.96
CHEMBL415532 1 4.92
CHEMBL143927 1 4.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL34964 Ki = 27.0 nM 7.57
CHEMBL109227 Ki = 200.0 nM 6.70
CHEMBL143399 Ki = 220.0 nM 6.66
CHEMBL142592 Ki = 410.0 nM 6.39
CHEMBL334931 Ki = 500.0 nM 6.30
CHEMBL342173 Ki = 780.0 nM 6.11
CHEMBL336239 Ki = 1100.0 nM 5.96
CHEMBL140740 M(DANSYLAMIDOPHENYL)BORONIC ACID Ki = 1300.0 nM 5.89
CHEMBL140723 Ki = 1400.0 nM 5.85
CHEMBL139713 Ki = 1600.0 nM 5.80
CHEMBL20945 Ki = 1700.0 nM 5.77
CHEMBL141272 Ki = 2500.0 nM 5.60
CHEMBL82324 Ki = 2900.0 nM 5.54
CHEMBL140254 Ki = 2900.0 nM 5.54
CHEMBL143654 Ki = 3000.0 nM 5.52
CHEMBL20866 Ki = 3600.0 nM 5.44
CHEMBL334932 Ki = 3800.0 nM 5.42
CHEMBL140916 Ki = 3900.0 nM 5.41
CHEMBL139928 Ki = 4200.0 nM 5.38
CHEMBL140780 TOLYL BORONIC ACID Ki = 5400.0 nM 5.27
CHEMBL140747 Ki = 5900.0 nM 5.23
CHEMBL21427 Ki = 5900.0 nM 5.23
CHEMBL344890 Ki = 6400.0 nM 5.19
CHEMBL140467 Ki = 7000.0 nM 5.16
CHEMBL20852 Ki = 7300.0 nM 5.14
CHEMBL141079 Ki = 8500.0 nM 5.07
CHEMBL21485 PHENYLBORONIC ACID Ki = 10500.0 nM 4.98
CHEMBL342460 Ki = 10900.0 nM 4.96
CHEMBL415532 Ki = 12000.0 nM 4.92
CHEMBL143927 Ki = 15800.0 nM 4.80
CHEMBL341722 Ki = 22100.0 nM 4.66
CHEMBL139725 Ki = 25300.0 nM 4.60
CHEMBL141313 Ki = 53400.0 nM 4.27
CHEMBL31962 BUTYL BORONIC ACID Ki > 100000.0 nM -
CHEMBL421765 Ki > 100000.0 nM -
CHEMBL81556 DIPHENYL BORINIC ACID Ki > 100000.0 nM -
CHEMBL142083 Ki > 100000.0 nM -