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Assay Detail

CHEMBL2034166

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

Binding
Inhibition of Staphylococcus aureus PDF assessed as formate release from fMAS peptide substrate after 20 mins by formate dehydrogenase coupled assay
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Staphylococcus aureus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Peptide deformylase (CHEMBL2010635)
Type SINGLE PROTEIN
Organism Staphylococcus aureus

Publication

Acylprolinamides: a new class of peptide deformylase inhibitors with in vivo antibacterial activity.
Axten JM, Medina JR, Blackledge CW, Duquenne C, Grant SW, Bobko MA, Peng T, Miller WH, Pinckney T, Gallagher TF, Kulkarni S, Lewandowski T, Van Aller GS, Zonis R, Ward P, Campobasso N.
Bioorg Med Chem Lett (2012) 22 : 4028 -4032
PubMed 22579486 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 40 8.61 9.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2032134 1 9.28
CHEMBL2032137 1 9.07
CHEMBL2032133 1 9.05
CHEMBL2032135 1 9.03
CHEMBL2032138 1 9.00
CHEMBL2032132 1 8.92
CHEMBL2032148 1 8.89
CHEMBL2032141 1 8.85
CHEMBL2032142 1 8.85
CHEMBL2032143 1 8.85
CHEMBL2032125 1 8.85
CHEMBL2032126 1 8.82
CHEMBL2032131 1 8.80
CHEMBL2032140 1 8.77
CHEMBL2032136 1 8.77
CHEMBL2032122 1 8.70
CHEMBL2032130 1 8.70
CHEMBL2032129 1 8.68
CHEMBL2029376 1 8.66
CHEMBL2032121 1 8.66
CHEMBL2032116 1 8.64
CHEMBL2032146 1 8.64
CHEMBL2032124 1 8.62
CHEMBL2032117 1 8.60
CHEMBL2032145 1 8.49
CHEMBL2032147 1 8.48
CHEMBL2032123 1 8.47
CHEMBL2032118 1 8.43
CHEMBL2032144 1 8.42
CHEMBL2032113 1 8.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2032134 IC50 = 0.52 nM 9.28
CHEMBL2032137 IC50 = 0.86 nM 9.07
CHEMBL2032133 IC50 = 0.9 nM 9.05
CHEMBL2032135 IC50 = 0.93 nM 9.03
CHEMBL2032138 IC50 = 1.0 nM 9.00
CHEMBL2032132 IC50 = 1.2 nM 8.92
CHEMBL2032148 IC50 = 1.3 nM 8.89
CHEMBL2032141 IC50 = 1.4 nM 8.85
CHEMBL2032142 IC50 = 1.4 nM 8.85
CHEMBL2032143 IC50 = 1.4 nM 8.85
CHEMBL2032125 IC50 = 1.4 nM 8.85
CHEMBL2032126 IC50 = 1.5 nM 8.82
CHEMBL2032131 IC50 = 1.6 nM 8.80
CHEMBL2032140 IC50 = 1.7 nM 8.77
CHEMBL2032136 IC50 = 1.7 nM 8.77
CHEMBL2032122 IC50 = 2.0 nM 8.70
CHEMBL2032130 IC50 = 2.0 nM 8.70
CHEMBL2032129 IC50 = 2.1 nM 8.68
CHEMBL2029376 IC50 = 2.2 nM 8.66
CHEMBL2032121 IC50 = 2.2 nM 8.66
CHEMBL2032116 IC50 = 2.3 nM 8.64
CHEMBL2032146 IC50 = 2.3 nM 8.64
CHEMBL2032124 IC50 = 2.4 nM 8.62
CHEMBL2032117 IC50 = 2.5 nM 8.60
CHEMBL2032145 IC50 = 3.2 nM 8.49
CHEMBL2032147 IC50 = 3.3 nM 8.48
CHEMBL2032123 IC50 = 3.4 nM 8.47
CHEMBL2032118 IC50 = 3.7 nM 8.43
CHEMBL2032144 IC50 = 3.8 nM 8.42
CHEMBL2032113 IC50 = 4.0 nM 8.40
CHEMBL2032127 IC50 = 4.4 nM 8.36
CHEMBL2032120 IC50 = 4.5 nM 8.35
CHEMBL2032115 IC50 = 5.0 nM 8.30
CHEMBL2032112 IC50 = 5.0 nM 8.30
CHEMBL2032119 IC50 = 5.2 nM 8.28
CHEMBL2032128 IC50 = 5.9 nM 8.23
CHEMBL2032111 IC50 = 8.0 nM 8.10
CHEMBL2032114 IC50 = 10.0 nM 8.00
CHEMBL2032139 IC50 = 10.0 nM 8.00
CHEMBL2032110 IC50 = 12.0 nM 7.92