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Assay Detail

CHEMBL3861815

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Binding
Inhibition of Mycobacterium tuberculosis H37Rv acetyltransferase Eis assessed as reduction in enzyme-mediated acetylation by measuring CoASH release after 5 mins by DTNB based assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mycobacterium tuberculosis
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Sulfonamide-Based Inhibitors of Aminoglycoside Acetyltransferase Eis Abolish Resistance to Kanamycin in Mycobacterium tuberculosis.
Garzan A, Willby MJ, Green KD, Gajadeera CS, Hou C, Tsodikov OV, Posey JE, Garneau-Tsodikova S.
J Med Chem (2016) 59 : 10619 -10628
PubMed 27933949 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 6.28 9.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3931964 1 9.62
CHEMBL3911185 1 7.57
CHEMBL3963272 1 7.25
CHEMBL3900481 1 7.10
CHEMBL3909504 1 7.00
CHEMBL3967657 1 6.64
CHEMBL3918442 1 6.60
CHEMBL3984204 1 6.52
CHEMBL1600985 1 6.43
CHEMBL3938063 1 6.16
CHEMBL3961587 1 5.52
CHEMBL3963651 1 5.24
CHEMBL3891456 1 5.24
CHEMBL3928430 1 5.21
CHEMBL3906981 1 5.13
CHEMBL3946317 1 4.97
CHEMBL3956582 1 4.57
CHEMBL3937447 1 -
CHEMBL3969855 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3931964 IC50 = 0.24 nM 9.62
CHEMBL3911185 IC50 = 27.0 nM 7.57
CHEMBL3963272 IC50 = 56.0 nM 7.25
CHEMBL3900481 IC50 = 80.0 nM 7.10
CHEMBL3909504 IC50 = 100.0 nM 7.00
CHEMBL3967657 IC50 = 230.0 nM 6.64
CHEMBL3918442 IC50 = 250.0 nM 6.60
CHEMBL3984204 IC50 = 300.0 nM 6.52
CHEMBL1600985 IC50 = 370.0 nM 6.43
CHEMBL3938063 IC50 = 700.0 nM 6.16
CHEMBL3961587 IC50 = 3000.0 nM 5.52
CHEMBL3963651 IC50 = 5800.0 nM 5.24
CHEMBL3891456 IC50 = 5800.0 nM 5.24
CHEMBL3928430 IC50 = 6200.0 nM 5.21
CHEMBL3906981 IC50 = 7400.0 nM 5.13
CHEMBL3946317 IC50 = 10600.0 nM 4.97
CHEMBL3956582 IC50 = 27000.0 nM 4.57
CHEMBL3937447 IC50 > 200000.0 nM -
CHEMBL3969855 IC50 > 200000.0 nM -