Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1004728

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

Binding
Inhibition of Escherichia coli DNA gyrase
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Novel dual-targeting benzimidazole urea inhibitors of DNA gyrase and topoisomerase IV possessing potent antibacterial activity: intelligent design and evolution through the judicious use of structure-guided design and structure-activity relationships.
Charifson PS, Grillot AL, Grossman TH, Parsons JD, Badia M, Bellon S, Deininger DD, Drumm JE, Gross CH, LeTiran A, Liao Y, Mani N, Nicolau DP, Perola E, Ronkin S, Shannon D, Swenson LL, Tang Q, Tessier PR, Tian SK, Trudeau M, Wang T, Wei Y, Zhang H, Stamos D.
J Med Chem (2008) 51 : 5243 -5263
PubMed 18690678 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 7.26 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL519583 1 8.30
CHEMBL487664 1 8.22
CHEMBL36506 NOVOBIOCIN 4.0 1 7.85
CHEMBL222348 1 7.82
CHEMBL487832 1 7.75
CHEMBL512701 1 7.70
CHEMBL472009 1 7.48
CHEMBL472010 1 7.21
CHEMBL472524 1 7.09
CHEMBL486646 1 6.92
CHEMBL486645 1 6.89
CHEMBL472525 1 6.40
CHEMBL471145 1 4.70
CHEMBL487851 1 -
CHEMBL487852 1 -
CHEMBL487663 1 -
CHEMBL222333 1 -
CHEMBL471319 1 -
CHEMBL486831 1 -
CHEMBL486832 1 -
CHEMBL519397 1 -
CHEMBL488699 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL519583 Ki = 5.0 nM 8.30
CHEMBL487664 Ki = 6.0 nM 8.22
CHEMBL36506 NOVOBIOCIN Ki = 14.0 nM 7.85
CHEMBL222348 Ki = 15.0 nM 7.82
CHEMBL487832 Ki = 18.0 nM 7.75
CHEMBL512701 Ki = 20.0 nM 7.70
CHEMBL472009 Ki = 33.0 nM 7.48
CHEMBL472010 Ki = 61.0 nM 7.21
CHEMBL472524 Ki = 81.0 nM 7.09
CHEMBL486646 Ki = 120.0 nM 6.92
CHEMBL486645 Ki = 130.0 nM 6.89
CHEMBL472525 Ki = 400.0 nM 6.40
CHEMBL471145 Ki = 20000.0 nM 4.70
CHEMBL487851 Ki < 4.0 nM -
CHEMBL487852 Ki < 4.0 nM -
CHEMBL487663 Ki < 4.0 nM -
CHEMBL222333 Ki < 4.0 nM -
CHEMBL471319 Ki < 4.0 nM -
CHEMBL486831 Ki < 4.0 nM -
CHEMBL486832 Ki < 4.0 nM -
CHEMBL519397 Ki < 4.0 nM -
CHEMBL488699 Ki < 4.0 nM -