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Assay Detail

CHEMBL934296

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Binding
Inhibition of human Eg5 basal ATPase activity
ChEMBL ↗
65
Total Activities
65
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 of S-trityl-L-cysteine analogues as inhibitors of the human mitotic kinesin Eg5.
Debonis S, Skoufias DA, Indorato RL, Liger F, Marquet B, Laggner C, Joseph B, Kozielski F.
J Med Chem (2008) 51 : 1115 -1125
PubMed 18266314 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 35 5.99 7.30
Activity 30 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL392695 S-TRITYL-L-CYSTEINE — 1 7.30
CHEMBL429597 — — 1 7.00
CHEMBL232728 — — 1 6.92
CHEMBL408072 — — 1 6.82
CHEMBL412251 — — 1 6.82
CHEMBL259257 — — 1 6.82
CHEMBL270138 — — 1 6.76
CHEMBL259256 — — 1 6.76
CHEMBL261613 — — 1 6.70
CHEMBL261611 — — 1 6.70
CHEMBL392369 — — 1 6.70
CHEMBL409102 — — 1 6.70
CHEMBL412132 — — 1 6.60
CHEMBL405609 — — 1 6.35
CHEMBL272404 — — 1 6.22
CHEMBL409317 — — 1 6.22
CHEMBL412292 — — 1 6.12
CHEMBL412312 — — 1 6.05
CHEMBL410695 — — 1 6.00
CHEMBL264923 — — 1 5.82
CHEMBL270748 — — 1 5.82
CHEMBL410315 — — 1 5.82
CHEMBL558431 — — 1 5.76
CHEMBL409295 — — 1 5.70
CHEMBL405611 — — 1 5.60
CHEMBL272618 — — 1 5.40
CHEMBL408179 — — 1 5.28
CHEMBL269918 — — 1 5.22
CHEMBL408325 — — 1 5.17
CHEMBL436920 — — 1 5.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL392695 S-TRITYL-L-CYSTEINE Ki = 50.0 nM 7.30
CHEMBL429597 — Ki = 100.0 nM 7.00
CHEMBL232728 — Ki = 120.0 nM 6.92
CHEMBL408072 — Ki = 150.0 nM 6.82
CHEMBL412251 — Ki = 150.0 nM 6.82
CHEMBL259257 — Ki = 150.0 nM 6.82
CHEMBL270138 — Ki = 175.0 nM 6.76
CHEMBL259256 — Ki = 175.0 nM 6.76
CHEMBL261613 — Ki = 200.0 nM 6.70
CHEMBL261611 — Ki = 200.0 nM 6.70
CHEMBL392369 — Ki = 200.0 nM 6.70
CHEMBL409102 — Ki = 200.0 nM 6.70
CHEMBL412132 — Ki = 250.0 nM 6.60
CHEMBL405609 — Ki = 450.0 nM 6.35
CHEMBL409317 — Ki = 600.0 nM 6.22
CHEMBL272404 — Ki = 600.0 nM 6.22
CHEMBL412292 — Ki = 750.0 nM 6.12
CHEMBL412312 — Ki = 900.0 nM 6.05
CHEMBL410695 — Ki = 1000.0 nM 6.00
CHEMBL264923 — Ki = 1500.0 nM 5.82
CHEMBL270748 — Ki = 1500.0 nM 5.82
CHEMBL410315 — Ki = 1500.0 nM 5.82
CHEMBL558431 — Ki = 1750.0 nM 5.76
CHEMBL409295 — Ki = 2000.0 nM 5.70
CHEMBL405611 — Ki = 2500.0 nM 5.60
CHEMBL272618 — Ki = 4000.0 nM 5.40
CHEMBL408179 — Ki = 5230.0 nM 5.28
CHEMBL269918 — Ki = 6000.0 nM 5.22
CHEMBL408325 — Ki = 6750.0 nM 5.17
CHEMBL436920 — Ki = 7000.0 nM 5.16
CHEMBL411111 — Ki = 13000.0 nM 4.89
CHEMBL411702 — Ki = 14000.0 nM 4.85
CHEMBL260522 — Ki = 23000.0 nM 4.64
CHEMBL270344 — Ki = 23000.0 nM 4.64
CHEMBL272406 — Ki = 35000.0 nM 4.46
CHEMBL409818 — Activity - — -
CHEMBL260301 — Activity - — -
CHEMBL270537 — Activity - — -
CHEMBL261392 — Activity - — -
CHEMBL410131 — Activity - — -
CHEMBL409296 — Activity - — -
CHEMBL270470 — Activity - — -
CHEMBL269853 — Activity - — -
CHEMBL407416 — Activity - — -
CHEMBL407353 — Activity - — -
CHEMBL259043 o-tolyl(trityl)sulfane Activity - — -
CHEMBL272034 — Activity - — -
CHEMBL411304 — Activity - — -
CHEMBL270524 ETHYL(TRITYL)SULFANE Activity - — -
CHEMBL261170 — Activity - — -