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Assay Detail

CHEMBL1819932

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Binding
Inhibition of Mycobacterium tuberculosis recombinant EphB expressed in Escherichia coli BL21 using CMNPC as substrate after 30 mins by fluorescent assay relative to control
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mycobacterium tuberculosis
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Epoxide hydrolase B (CHEMBL1795155)
Type SINGLE PROTEIN
Organism Mycobacterium tuberculosis

Publication

The structure-activity relationship of urea derivatives as anti-tuberculosis agents.
Brown JR, North EJ, Hurdle JG, Morisseau C, Scarborough JS, Sun D, Korduláková J, Scherman MS, Jones V, Grzegorzewicz A, Crew RM, Jackson M, McNeil MR, Lee RE.
Bioorg Med Chem (2011) 19 : 5585 -5595
PubMed 21840723 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.44 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL354676 DIPHENYLUREA 1 7.72
CHEMBL242255 1 6.89
CHEMBL1076347 TRICLOCARBAN 2.0 1 6.66
CHEMBL1818421 1 4.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL354676 DIPHENYLUREA IC50 = 19.0 nM 7.72
CHEMBL242255 IC50 = 130.0 nM 6.89
CHEMBL1076347 TRICLOCARBAN IC50 = 220.0 nM 6.66
CHEMBL1818421 IC50 = 31600.0 nM 4.50