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Assay Detail

CHEMBL4275017

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

Binding
Inhibition of Escherichia coli GyrB (1 to 220 residues) expressed in Escherichia coli BL21(DE3)
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

DNA gyrase subunit B (CHEMBL1826)
Type SINGLE PROTEIN
Organism Escherichia coli

Publication

Discovery of dual GyrB/ParE inhibitors active against Gram-negative bacteria.
Ho SY, Wang W, Ng FM, Wong YX, Poh ZY, Tan SWE, Ang SH, Liew SS, Joyner Wong YS, Tan Y, Poulsen A, Pendharkar V, Sangthongpitag K, Manchester J, Basarab G, Hill J, Keller TH, Cherian J.
Eur J Med Chem (2018) 157 : 610 -621
PubMed 30125722 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 8.28 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4283208 1 8.70
CHEMBL4286573 1 8.70
CHEMBL4294536 1 8.52
CHEMBL4295081 1 8.52
CHEMBL4291061 1 8.40
CHEMBL4286625 1 8.40
CHEMBL4290062 1 8.30
CHEMBL4293447 1 8.22
CHEMBL4294467 1 8.22
CHEMBL4281775 1 8.22
CHEMBL3235085 1 8.22
CHEMBL4279382 1 8.15
CHEMBL4278317 1 8.10
CHEMBL4279313 1 8.10
CHEMBL4289650 1 8.05
CHEMBL4289998 1 8.05
CHEMBL4286232 1 7.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4283208 IC50 = 2.0 nM 8.70
CHEMBL4286573 IC50 = 2.0 nM 8.70
CHEMBL4294536 IC50 = 3.0 nM 8.52
CHEMBL4295081 IC50 = 3.0 nM 8.52
CHEMBL4291061 IC50 = 4.0 nM 8.40
CHEMBL4286625 IC50 = 4.0 nM 8.40
CHEMBL4290062 IC50 = 5.0 nM 8.30
CHEMBL4293447 IC50 = 6.0 nM 8.22
CHEMBL4294467 IC50 = 6.0 nM 8.22
CHEMBL4281775 IC50 = 6.0 nM 8.22
CHEMBL3235085 IC50 = 6.0 nM 8.22
CHEMBL4279382 IC50 = 7.0 nM 8.15
CHEMBL4278317 IC50 = 8.0 nM 8.10
CHEMBL4279313 IC50 = 8.0 nM 8.10
CHEMBL4289650 IC50 = 9.0 nM 8.05
CHEMBL4289998 IC50 = 9.0 nM 8.05
CHEMBL4286232 IC50 = 14.0 nM 7.85