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Assay Detail

CHEMBL1694080

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Binding
Inhibition of C-terminal His6-tagged human Eg5 basal ATPase activity
25
Total Activities
25
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Kinesin-like protein KIF11 (CHEMBL4581)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationship and multidrug resistance study of new S-trityl-L-cysteine derivatives as inhibitors of Eg5.
Kaan HY, Weiss J, Menger D, Ulaganathan V, Tkocz K, Laggner C, Popowycz F, Joseph B, Kozielski F.
J Med Chem (2011) 54 : 1576 -1586
PubMed 21344920 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 24 6.33 7.14
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL392695 S-TRITYL-L-CYSTEINE 1 7.14
CHEMBL1688930 1 7.12
CHEMBL1688927 1 7.08
CHEMBL399251 1 7.01
CHEMBL408072 1 6.81
CHEMBL259257 1 6.76
CHEMBL1688931 1 6.52
CHEMBL1688926 1 6.37
CHEMBL1688925 1 5.87
CHEMBL1688929 1 5.60
CHEMBL1688924 1 5.49
CHEMBL1688932 1 4.23
CHEMBL1688923 1 -
CHEMBL1688922 1 -
CHEMBL232133 1 -
CHEMBL1688921 1 -
CHEMBL1688920 1 -
CHEMBL1688928 1 -
CHEMBL412132 1 -
CHEMBL409102 1 -
CHEMBL429597 1 -
CHEMBL259256 1 -
CHEMBL261613 1 -
CHEMBL1688933 1 -
CHEMBL392369 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL392695 S-TRITYL-L-CYSTEINE Ki = 71.9 nM 7.14
CHEMBL1688930 Ki = 76.2 nM 7.12
CHEMBL1688927 Ki = 84.2 nM 7.08
CHEMBL399251 Ki = 98.6 nM 7.01
CHEMBL408072 Ki = 156.1 nM 6.81
CHEMBL259257 Ki = 174.5 nM 6.76
CHEMBL1688931 Ki = 302.1 nM 6.52
CHEMBL1688926 Ki = 428.6 nM 6.37
CHEMBL1688925 Ki = 1349.7 nM 5.87
CHEMBL1688929 Ki = 2536.3 nM 5.60
CHEMBL1688924 Ki = 3263.7 nM 5.49
CHEMBL1688932 Ki = 58333.0 nM 4.23
CHEMBL1688923 Ki < 50.0 nM -
CHEMBL1688922 Ki < 50.0 nM -
CHEMBL232133 Ki < 50.0 nM -
CHEMBL1688921 Ki < 50.0 nM -
CHEMBL1688920 Ki < 50.0 nM -
CHEMBL1688928 Ki < 50.0 nM -
CHEMBL412132 Ki < 50.0 nM -
CHEMBL409102 Ki < 50.0 nM -
CHEMBL429597 Ki < 50.0 nM -
CHEMBL259256 Ki < 50.0 nM -
CHEMBL261613 Ki < 50.0 nM -
CHEMBL1688933 Inhibition - % -
CHEMBL392369 Ki < 50.0 nM -