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Assay Detail

CHEMBL3271706

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Binding
Inhibition of Mycobacterium tuberculosis acetohydroxy acid synthase after 60 mins by acetoin formation-based colorimetry
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

Design and synthesis of triazolopyrimidine acylsulfonamides as novel anti-mycobacterial leads acting through inhibition of acetohydroxyacid synthase.
Patil V, Kale M, Raichurkar A, Bhaskar B, Prahlad D, Balganesh M, Nandan S, Shahul Hameed P.
Bioorg Med Chem Lett (2014) 24 : 2222 -2225
PubMed 24703230 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 6.43 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3260395 1 7.75
CHEMBL3260383 1 7.60
CHEMBL3260382 1 7.15
CHEMBL3260381 1 7.04
CHEMBL3260379 1 6.98
CHEMBL3260380 1 6.82
CHEMBL3260394 1 6.70
CHEMBL3260388 1 6.59
CHEMBL3260396 1 6.54
CHEMBL3260385 1 6.29
CHEMBL513261 SULFOMETURON METHYL 1 6.12
CHEMBL3260386 1 5.81
CHEMBL3260391 1 5.60
CHEMBL3260390 1 5.36
CHEMBL3260389 1 5.31
CHEMBL3260384 1 5.24
CHEMBL3260387 1 -
CHEMBL3260392 1 -
CHEMBL3260393 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3260395 IC50 = 17.78 nM 7.75
CHEMBL3260383 IC50 = 25.12 nM 7.60
CHEMBL3260382 IC50 = 70.79 nM 7.15
CHEMBL3260381 IC50 = 91.2 nM 7.04
CHEMBL3260379 IC50 = 104.71 nM 6.98
CHEMBL3260380 IC50 = 151.36 nM 6.82
CHEMBL3260394 IC50 = 199.53 nM 6.70
CHEMBL3260388 IC50 = 257.04 nM 6.59
CHEMBL3260396 IC50 = 288.4 nM 6.54
CHEMBL3260385 IC50 = 512.86 nM 6.29
CHEMBL513261 SULFOMETURON METHYL IC50 = 758.58 nM 6.12
CHEMBL3260386 IC50 = 1548.82 nM 5.81
CHEMBL3260391 IC50 = 2511.89 nM 5.60
CHEMBL3260390 IC50 = 4365.16 nM 5.36
CHEMBL3260389 IC50 = 4897.79 nM 5.31
CHEMBL3260384 IC50 = 5754.4 nM 5.24
CHEMBL3260387 IC50 < 63.1 nM -
CHEMBL3260392 IC50 > 30199.52 nM -
CHEMBL3260393 IC50 > 30199.52 nM -