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Assay Detail

CHEMBL3598601

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

Binding
Inhibition of full-length N-terminal His-tagged Escherichia coli FabH expressed in Escherichia coli BL21 (DE3) using acetyl-CoA/[3H]-acetyl-CoA/holo-ACP as substrate by liquid scintillation counting analysis
13
Total Activities
13
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

Design, synthesis and molecular docking of novel bipyrazolyl thiazolone scaffold as a new class of antibacterial agents
Kalaria PN, Makawana JA, Satasia SP, Raval DK, Zhu H
Medchemcomm (2014) 5 : 1555 -1562
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.06 5.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3596761 1 5.60
CHEMBL3596847 1 5.51
CHEMBL3596760 1 5.41
CHEMBL3596759 1 5.33
CHEMBL176 BEKANAMYCIN 3.0 1 5.20
CHEMBL3596853 1 5.07
CHEMBL3596850 1 5.04
CHEMBL3596849 1 4.95
CHEMBL3596204 1 4.89
CHEMBL3596848 1 4.81
CHEMBL3596851 1 4.76
CHEMBL3596854 1 4.66
CHEMBL3596852 1 4.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3596761 IC50 = 2500.0 nM 5.60
CHEMBL3596847 IC50 = 3100.0 nM 5.51
CHEMBL3596760 IC50 = 3900.0 nM 5.41
CHEMBL3596759 IC50 = 4700.0 nM 5.33
CHEMBL176 BEKANAMYCIN IC50 = 6300.0 nM 5.20
CHEMBL3596853 IC50 = 8500.0 nM 5.07
CHEMBL3596850 IC50 = 9100.0 nM 5.04
CHEMBL3596849 IC50 = 11300.0 nM 4.95
CHEMBL3596204 IC50 = 12800.0 nM 4.89
CHEMBL3596848 IC50 = 15600.0 nM 4.81
CHEMBL3596851 IC50 = 17500.0 nM 4.76
CHEMBL3596854 IC50 = 21900.0 nM 4.66
CHEMBL3596852 IC50 = 26100.0 nM 4.58