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Assay Detail

CHEMBL4771034

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of Mycobacterium tuberculosis His6-tagged MabA expressed in Escherichia coli BL21 (DE3) assessed as reduction in HBCoA formation using AcAcCoA as substrate preincubated for 30 mins followed by substrate and 100 uM NADPH addition and measured after 15 mins by LC-MS/MS analysis
37
Total Activities
37
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

Discovery of the first Mycobacterium tuberculosis MabA (FabG1) inhibitors through a fragment-based screening.
Faïon L,Djaout K,Frita R,Pintiala C,Cantrelle FX,Moune M,Vandeputte A,Bourbiaux K,Piveteau C,Herledan A,Biela A,Leroux F,Kremer L,Blaise M,Tanina A,Wintjens R,Hanoulle X,Déprez B,Willand N,Baulard AR,Flipo M
Eur J Med Chem (2020) 200 : 112440 -112440
PubMed 32505086 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 37 4.02 4.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4799633 1 4.60
CHEMBL4800208 1 4.42
CHEMBL1453095 1 4.40
CHEMBL4795245 1 4.40
CHEMBL479006 1 4.28
CHEMBL4786178 1 4.23
CHEMBL4794332 1 4.19
CHEMBL4779906 1 4.16
CHEMBL4780207 1 4.16
CHEMBL115897 1 4.14
CHEMBL4777789 1 4.08
CHEMBL4782547 1 4.04
CHEMBL4783850 1 4.02
CHEMBL507614 1 3.73
CHEMBL4778915 1 3.71
CHEMBL4777094 1 3.61
CHEMBL4799804 1 3.51
CHEMBL4792568 1 3.33
CHEMBL4775986 1 3.33
CHEMBL4780954 1 -
CHEMBL4783526 1 -
CHEMBL4793201 1 -
CHEMBL4799784 1 -
CHEMBL4787533 1 -
CHEMBL4780029 1 -
CHEMBL4797728 1 -
CHEMBL4784825 1 -
CHEMBL4780931 1 -
CHEMBL4793595 1 -
CHEMBL4784612 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4799633 IC50 = 25000.0 nM 4.60
CHEMBL4800208 IC50 = 38000.0 nM 4.42
CHEMBL1453095 IC50 = 40000.0 nM 4.40
CHEMBL4795245 IC50 = 40000.0 nM 4.40
CHEMBL479006 IC50 = 53000.0 nM 4.28
CHEMBL4786178 IC50 = 59000.0 nM 4.23
CHEMBL4794332 IC50 = 65000.0 nM 4.19
CHEMBL4779906 IC50 = 70000.0 nM 4.16
CHEMBL4780207 IC50 = 69000.0 nM 4.16
CHEMBL115897 IC50 = 72000.0 nM 4.14
CHEMBL4777789 IC50 = 84000.0 nM 4.08
CHEMBL4782547 IC50 = 92000.0 nM 4.04
CHEMBL4783850 IC50 = 95000.0 nM 4.02
CHEMBL507614 IC50 = 185000.0 nM 3.73
CHEMBL4778915 IC50 = 194000.0 nM 3.71
CHEMBL4777094 IC50 = 243000.0 nM 3.61
CHEMBL4799804 IC50 = 310000.0 nM 3.51
CHEMBL4775986 IC50 = 470000.0 nM 3.33
CHEMBL4792568 IC50 = 470000.0 nM 3.33
CHEMBL4780931 IC50 = 295000.0 nM -
CHEMBL4794188 IC50 > 1000000.0 nM -
CHEMBL4783340 IC50 > 500000.0 nM -
CHEMBL4783055 IC50 > 1000000.0 nM -
CHEMBL4779882 IC50 = 310000.0 nM -
CHEMBL4777830 IC50 > 500000.0 nM -
CHEMBL4791943 IC50 = 1000000.0 nM -
CHEMBL4794016 IC50 > 1000000.0 nM -
CHEMBL4784612 IC50 = 145000.0 nM -
CHEMBL4793595 IC50 > 500000.0 nM -
CHEMBL4784825 IC50 = 186000.0 nM -
CHEMBL4797728 IC50 = 280000.0 nM -
CHEMBL4780029 IC50 = 109000.0 nM -
CHEMBL4787533 IC50 > 500000.0 nM -
CHEMBL4799784 IC50 = 147000.0 nM -
CHEMBL4793201 IC50 > 400000.0 nM -
CHEMBL4783526 IC50 = 126000.0 nM -
CHEMBL4780954 IC50 = 140000.0 nM -