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Assay Detail

CHEMBL1034865

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Binding
Inhibition of Mycobacterium tuberculosis HisG assessed as phosphoribosyl ATP production by spectrophotometry
15
Total Activities
13
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

ATP phosphoribosyltransferase (CHEMBL6086)
Type SINGLE PROTEIN
Organism Mycobacterium tuberculosis

Publication

Discovery of novel nitrobenzothiazole inhibitors for Mycobacterium tuberculosis ATP phosphoribosyl transferase (HisG) through virtual screening.
Cho Y, Ioerger TR, Sacchettini JC.
J Med Chem (2008) 51 : 5984 -5992
PubMed 18778048 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.09 5.40
Ki 4 4.98 5.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL459933 2 5.70
CHEMBL459306 2 5.70
CHEMBL451611 1 5.26
CHEMBL518011 1 5.00
CHEMBL459510 1 5.00
CHEMBL523351 1 4.92
CHEMBL493484 1 4.86
CHEMBL75967 PENTACHLOROPHENOL 1 4.30
CHEMBL1466 DICUMAROL 4.0 1 4.22
CHEMBL461642 1 -
CHEMBL461201 1 -
CHEMBL493482 1 -
CHEMBL491074 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL459933 Ki = 2000.0 nM 5.70
CHEMBL459306 Ki = 2000.0 nM 5.70
CHEMBL459933 IC50 = 4000.0 nM 5.40
CHEMBL451611 IC50 = 5500.0 nM 5.26
CHEMBL459306 IC50 = 6000.0 nM 5.22
CHEMBL518011 IC50 = 10000.0 nM 5.00
CHEMBL459510 IC50 = 10000.0 nM 5.00
CHEMBL523351 IC50 = 11900.0 nM 4.92
CHEMBL493484 IC50 = 13900.0 nM 4.86
CHEMBL75967 PENTACHLOROPHENOL Ki = 50000.0 nM 4.30
CHEMBL1466 DICUMAROL Ki = 60000.0 nM 4.22
CHEMBL461642 IC50 - -
CHEMBL461201 IC50 - -
CHEMBL493482 IC50 - -
CHEMBL491074 IC50 - -