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Assay Detail

CHEMBL3117199

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Binding
Inhibition of Clostridium botulinum BoNT/A LC expressed in Escherichia coli assessed as cleavage of SNAPtide preincubated for 5 mins followed by SNAPtide addition measured for 105 mins by fluorescence assay
62
Total Activities
62
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Clostridium botulinum
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Botulinum neurotoxin type A (CHEMBL5192)
Type SINGLE PROTEIN
Organism Clostridium botulinum

Publication

Identification of clinically viable quinolinol inhibitors of botulinum neurotoxin A light chain.
Caglič D, Krutein MC, Bompiani KM, Barlow DJ, Benoni G, Pelletier JC, Reitz AB, Lairson LL, Houseknecht KL, Smith GR, Dickerson TJ.
J Med Chem (2014) 57 : 669 -676
PubMed 24387280 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 62 5.42 6.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3112883 1 6.10
CHEMBL3112887 1 6.05
CHEMBL3112908 1 6.00
CHEMBL3112891 1 5.96
CHEMBL3112896 1 5.92
CHEMBL3112892 1 5.85
CHEMBL3112895 1 5.82
CHEMBL3112885 1 5.80
CHEMBL3112913 1 5.72
CHEMBL3112910 1 5.72
CHEMBL3112894 1 5.70
CHEMBL3112911 1 5.70
CHEMBL3112889 1 5.68
CHEMBL3112901 1 5.68
CHEMBL1688558 1 5.66
CHEMBL3112923 1 5.64
CHEMBL1497004 1 5.60
CHEMBL3112906 1 5.60
CHEMBL3112900 1 5.55
CHEMBL3112915 1 5.54
CHEMBL3112919 1 5.52
CHEMBL3112898 1 5.52
CHEMBL598057 1 5.48
CHEMBL3112893 1 5.46
CHEMBL3112905 1 5.46
CHEMBL3112884 1 5.44
CHEMBL3112917 1 5.38
CHEMBL589706 1 5.37
CHEMBL3112921 1 5.36
CHEMBL3112907 1 5.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3112883 IC50 = 800.0 nM 6.10
CHEMBL3112887 IC50 = 900.0 nM 6.05
CHEMBL3112908 IC50 = 1000.0 nM 6.00
CHEMBL3112891 IC50 = 1100.0 nM 5.96
CHEMBL3112896 IC50 = 1200.0 nM 5.92
CHEMBL3112892 IC50 = 1400.0 nM 5.85
CHEMBL3112895 IC50 = 1500.0 nM 5.82
CHEMBL3112885 IC50 = 1600.0 nM 5.80
CHEMBL3112913 IC50 = 1900.0 nM 5.72
CHEMBL3112910 IC50 = 1900.0 nM 5.72
CHEMBL3112894 IC50 = 2000.0 nM 5.70
CHEMBL3112911 IC50 = 2000.0 nM 5.70
CHEMBL3112889 IC50 = 2100.0 nM 5.68
CHEMBL3112901 IC50 = 2100.0 nM 5.68
CHEMBL1688558 IC50 = 2200.0 nM 5.66
CHEMBL3112923 IC50 = 2300.0 nM 5.64
CHEMBL1497004 IC50 = 2500.0 nM 5.60
CHEMBL3112906 IC50 = 2500.0 nM 5.60
CHEMBL3112900 IC50 = 2800.0 nM 5.55
CHEMBL3112915 IC50 = 2900.0 nM 5.54
CHEMBL3112919 IC50 = 3000.0 nM 5.52
CHEMBL3112898 IC50 = 3000.0 nM 5.52
CHEMBL598057 IC50 = 3300.0 nM 5.48
CHEMBL3112893 IC50 = 3500.0 nM 5.46
CHEMBL3112905 IC50 = 3500.0 nM 5.46
CHEMBL3112884 IC50 = 3600.0 nM 5.44
CHEMBL3112917 IC50 = 4200.0 nM 5.38
CHEMBL589706 IC50 = 4300.0 nM 5.37
CHEMBL3112921 IC50 = 4400.0 nM 5.36
CHEMBL3112907 IC50 = 4500.0 nM 5.35
CHEMBL3112890 IC50 = 4600.0 nM 5.34
CHEMBL3112920 IC50 = 5100.0 nM 5.29
CHEMBL3112914 IC50 = 5100.0 nM 5.29
CHEMBL3112922 IC50 = 5200.0 nM 5.28
CHEMBL3112909 IC50 = 5600.0 nM 5.25
CHEMBL3112912 IC50 = 5600.0 nM 5.25
CHEMBL3112918 IC50 = 5600.0 nM 5.25
CHEMBL3112897 IC50 = 6200.0 nM 5.21
CHEMBL3112925 IC50 = 6700.0 nM 5.17
CHEMBL3112904 IC50 = 7100.0 nM 5.15
CHEMBL3112899 IC50 = 7100.0 nM 5.15
CHEMBL3112916 IC50 = 7800.0 nM 5.11
CHEMBL224325 CHLORQUINALDOL IC50 = 10100.0 nM 5.00
CHEMBL3112886 IC50 = 10700.0 nM 4.97
CHEMBL1200596 CHLOROXINE IC50 = 11500.0 nM 4.94
CHEMBL3112888 IC50 = 13400.0 nM 4.87
CHEMBL3112927 IC50 = 14100.0 nM 4.85
CHEMBL3112924 IC50 = 16700.0 nM 4.78
CHEMBL497 CLIOQUINOL IC50 = 20300.0 nM 4.69
CHEMBL3112926 IC50 = 26700.0 nM 4.57