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Assay Detail

CHEMBL5042339

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Binding
Inhibition of Mycobacterium abscessus DNA gyrase using pBR322 DNA as substrate measured after 2 days by fluorescence based microplate reader assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mycobacteroides abscessus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Structure-Activity Relationship of Anti-<i>Mycobacterium abscessus</i> Piperidine-4-carboxamides, a New Class of NBTI DNA Gyrase Inhibitors.
Beuchel A, Robaa D, Negatu DA, Madani A, Alvarez N, Zimmerman MD, Richter A, Mann L, Hoenke S, Csuk R, Dick T, Imming P.
ACS Med Chem Lett (2022) 13 : 417 -427
PubMed 35300094 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.57 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5085925 1 6.96
CHEMBL5072749 1 5.82
CHEMBL5084804 1 5.82
CHEMBL3317856 GEPOTIDACIN 3.0 1 5.70
CHEMBL5071218 1 5.52
CHEMBL3637783 1 5.52
CHEMBL5091986 1 5.52
CHEMBL5091038 1 5.22
CHEMBL5079578 1 5.22
CHEMBL5069966 1 4.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5085925 IC50 = 110.0 nM 6.96
CHEMBL5072749 IC50 = 1500.0 nM 5.82
CHEMBL5084804 IC50 = 1500.0 nM 5.82
CHEMBL3317856 GEPOTIDACIN IC50 = 2000.0 nM 5.70
CHEMBL5071218 IC50 = 3000.0 nM 5.52
CHEMBL3637783 IC50 = 3000.0 nM 5.52
CHEMBL5091986 IC50 = 3000.0 nM 5.52
CHEMBL5091038 IC50 = 6000.0 nM 5.22
CHEMBL5079578 IC50 = 6000.0 nM 5.22
CHEMBL5069966 IC50 = 40000.0 nM 4.40