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Assay Detail

CHEMBL1273398

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

Binding
Inhibition of Bacillus anthracis lethal factor assessed as proteolysis using MCA-KKVYPYPME-Dap(Dnp)-NH2 peptide substrate by FRET assay
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bacillus anthracis
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Lethal factor (CHEMBL4372)
Type SINGLE PROTEIN
Organism Bacillus anthracis

Publication

Antidotes to anthrax lethal factor intoxication. Part 1: Discovery of potent lethal factor inhibitors with in vivo efficacy.
Jiao GS, Kim S, Moayeri M, Cregar-Hernandez L, McKasson L, Margosiak SA, Leppla SH, Johnson AT.
Bioorg Med Chem Lett (2010) 20 : 6850 -6853
PubMed 20864339 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 29 8.12 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1271420 1 10.30
CHEMBL1269994 1 9.62
CHEMBL1270304 1 9.52
CHEMBL1270103 1 9.39
CHEMBL1270210 1 9.36
CHEMBL1270211 1 9.33
CHEMBL1269887 1 9.16
CHEMBL1269993 1 9.07
CHEMBL1270102 1 8.96
CHEMBL1270404 1 8.89
CHEMBL1270305 1 8.85
CHEMBL1270403 1 8.68
CHEMBL1271419 1 8.51
CHEMBL1271312 1 8.14
CHEMBL1269054 1 8.09
CHEMBL1269886 1 8.03
CHEMBL1271003 1 7.96
CHEMBL1270697 1 7.48
CHEMBL1270905 1 7.38
CHEMBL1270698 1 7.05
CHEMBL1270496 1 7.02
CHEMBL1270599 1 7.00
CHEMBL1270802 1 6.94
CHEMBL1270904 1 6.93
CHEMBL1270497 1 6.91
CHEMBL1271004 1 6.87
CHEMBL1270801 1 6.82
CHEMBL1270498 1 6.64
CHEMBL1270598 1 6.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1271420 Ki = 0.05 nM 10.30
CHEMBL1269994 Ki = 0.24 nM 9.62
CHEMBL1270304 Ki = 0.3 nM 9.52
CHEMBL1270103 Ki = 0.41 nM 9.39
CHEMBL1270210 Ki = 0.44 nM 9.36
CHEMBL1270211 Ki = 0.47 nM 9.33
CHEMBL1269887 Ki = 0.69 nM 9.16
CHEMBL1269993 Ki = 0.85 nM 9.07
CHEMBL1270102 Ki = 1.1 nM 8.96
CHEMBL1270404 Ki = 1.3 nM 8.89
CHEMBL1270305 Ki = 1.4 nM 8.85
CHEMBL1270403 Ki = 2.1 nM 8.68
CHEMBL1271419 Ki = 3.1 nM 8.51
CHEMBL1271312 Ki = 7.3 nM 8.14
CHEMBL1269054 Ki = 8.2 nM 8.09
CHEMBL1269886 Ki = 9.3 nM 8.03
CHEMBL1271003 Ki = 11.0 nM 7.96
CHEMBL1270697 Ki = 33.0 nM 7.48
CHEMBL1270905 Ki = 42.0 nM 7.38
CHEMBL1270698 Ki = 90.0 nM 7.05
CHEMBL1270496 Ki = 96.0 nM 7.02
CHEMBL1270599 Ki = 99.0 nM 7.00
CHEMBL1270802 Ki = 115.0 nM 6.94
CHEMBL1270904 Ki = 118.0 nM 6.93
CHEMBL1270497 Ki = 122.0 nM 6.91
CHEMBL1271004 Ki = 135.0 nM 6.87
CHEMBL1270801 Ki = 151.0 nM 6.82
CHEMBL1270498 Ki = 230.0 nM 6.64
CHEMBL1270598 Ki = 350.0 nM 6.46