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

CHEMBL885975

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

Binding
Inhibition of Escherichia coli H560 DNA gyrase assessed as DNA cleavage
24
Total Activities
24
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

Structure-activity relationships of 3-aminoquinazolinediones, a new class of bacterial type-2 topoisomerase (DNA gyrase and topo IV) inhibitors.
Tran TP, Ellsworth EL, Sanchez JP, Watson BM, Stier MA, Showalter HD, Domagala JM, Shapiro MA, Joannides ET, Gracheck SJ, Nguyen DQ, Bird P, Yip J, Sharadendu A, Ha C, Ramezani S, Wu X, Singh R.
Bioorg Med Chem Lett (2007) 17 : 1312 -1320
PubMed 17196390 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 5.50 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL247694 1 7.00
CHEMBL383917 1 6.70
CHEMBL393504 1 6.62
CHEMBL245443 1 6.52
CHEMBL397315 1 6.40
CHEMBL8 CIPROFLOXACIN 4.0 1 6.40
CHEMBL393303 1 5.92
CHEMBL247497 1 5.89
CHEMBL247085 1 5.80
CHEMBL248505 1 5.52
CHEMBL247695 1 5.37
CHEMBL247898 1 5.28
CHEMBL393505 1 5.21
CHEMBL248497 1 5.09
CHEMBL245634 1 5.00
CHEMBL394491 1 4.96
CHEMBL248305 1 4.77
CHEMBL437768 1 4.70
CHEMBL248506 1 4.68
CHEMBL247087 1 4.64
CHEMBL395622 1 4.46
CHEMBL247086 1 4.01
CHEMBL245432 1 -
CHEMBL247292 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL247694 IC50 = 100.0 nM 7.00
CHEMBL383917 IC50 = 200.0 nM 6.70
CHEMBL393504 IC50 = 240.0 nM 6.62
CHEMBL245443 IC50 = 300.0 nM 6.52
CHEMBL397315 IC50 = 400.0 nM 6.40
CHEMBL8 CIPROFLOXACIN IC50 = 400.0 nM 6.40
CHEMBL393303 IC50 = 1200.0 nM 5.92
CHEMBL247497 IC50 = 1300.0 nM 5.89
CHEMBL247085 IC50 = 1600.0 nM 5.80
CHEMBL248505 IC50 = 3000.0 nM 5.52
CHEMBL247695 IC50 = 4300.0 nM 5.37
CHEMBL247898 IC50 = 5200.0 nM 5.28
CHEMBL393505 IC50 = 6100.0 nM 5.21
CHEMBL248497 IC50 = 8200.0 nM 5.09
CHEMBL245634 IC50 = 10000.0 nM 5.00
CHEMBL394491 IC50 = 11000.0 nM 4.96
CHEMBL248305 IC50 = 17000.0 nM 4.77
CHEMBL437768 IC50 = 20000.0 nM 4.70
CHEMBL248506 IC50 = 21000.0 nM 4.68
CHEMBL247087 IC50 = 23000.0 nM 4.64
CHEMBL395622 IC50 = 35000.0 nM 4.46
CHEMBL247086 IC50 = 98000.0 nM 4.01
CHEMBL245432 IC50 - -
CHEMBL247292 IC50 > 100000.0 nM -