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Assay Detail

CHEMBL3294267

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

Binding
Inhibition of C-terminal His-tagged KSP ATPase motor domain (unknown origin) expressed in bacteria incubated for 30 mins prior to ATP addition measured after 15 mins by luminescence assay
54
Total Activities
54
Compounds Tested
1
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

Optimization of diaryl amine derivatives as kinesin spindle protein inhibitors.
Takeuchi T, Oishi S, Kaneda M, Misu R, Ohno H, Sawada J, Asai A, Nakamura S, Nakanishi I, Fujii N.
Bioorg Med Chem (2014) 22 : 3171 -3179
PubMed 24794744 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 54 6.53 7.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3289009 1 7.46
CHEMBL3288965 1 7.37
CHEMBL3288973 1 7.35
CHEMBL3289010 1 7.30
CHEMBL3289006 1 7.30
CHEMBL3289003 1 7.29
CHEMBL1802986 1 7.28
CHEMBL3288994 1 7.17
CHEMBL3288964 1 7.07
CHEMBL1802987 1 7.02
CHEMBL1803018 1 6.92
CHEMBL3288983 1 6.80
CHEMBL3289005 1 6.72
CHEMBL1173704 1 6.68
CHEMBL3288963 1 6.57
CHEMBL3289002 1 6.54
CHEMBL3288976 1 6.48
CHEMBL3288972 1 6.41
CHEMBL3289007 1 6.37
CHEMBL3288982 1 6.37
CHEMBL3288990 1 6.36
CHEMBL3288966 1 6.26
CHEMBL3288981 1 6.09
CHEMBL3289001 1 6.09
CHEMBL3289008 1 6.04
CHEMBL3288988 1 5.92
CHEMBL3288974 1 5.70
CHEMBL3288970 1 5.50
CHEMBL3288999 1 5.44
CHEMBL3288997 1 5.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3289009 IC50 = 35.0 nM 7.46
CHEMBL3288965 IC50 = 43.0 nM 7.37
CHEMBL3288973 IC50 = 45.0 nM 7.35
CHEMBL3289010 IC50 = 50.0 nM 7.30
CHEMBL3289006 IC50 = 50.0 nM 7.30
CHEMBL3289003 IC50 = 51.0 nM 7.29
CHEMBL1802986 IC50 = 52.0 nM 7.28
CHEMBL3288994 IC50 = 68.0 nM 7.17
CHEMBL3288964 IC50 = 85.0 nM 7.07
CHEMBL1802987 IC50 = 95.0 nM 7.02
CHEMBL1803018 IC50 = 120.0 nM 6.92
CHEMBL3288983 IC50 = 160.0 nM 6.80
CHEMBL3289005 IC50 = 190.0 nM 6.72
CHEMBL1173704 IC50 = 210.0 nM 6.68
CHEMBL3288963 IC50 = 270.0 nM 6.57
CHEMBL3289002 IC50 = 290.0 nM 6.54
CHEMBL3288976 IC50 = 330.0 nM 6.48
CHEMBL3288972 IC50 = 390.0 nM 6.41
CHEMBL3289007 IC50 = 430.0 nM 6.37
CHEMBL3288982 IC50 = 430.0 nM 6.37
CHEMBL3288990 IC50 = 440.0 nM 6.36
CHEMBL3288966 IC50 = 550.0 nM 6.26
CHEMBL3288981 IC50 = 810.0 nM 6.09
CHEMBL3289001 IC50 = 810.0 nM 6.09
CHEMBL3289008 IC50 = 920.0 nM 6.04
CHEMBL3288988 IC50 = 1200.0 nM 5.92
CHEMBL3288974 IC50 = 2000.0 nM 5.70
CHEMBL3288970 IC50 = 3200.0 nM 5.50
CHEMBL3288999 IC50 = 3600.0 nM 5.44
CHEMBL3288997 IC50 = 4600.0 nM 5.34
CHEMBL3288961 IC50 = 7000.0 nM 5.16
CHEMBL3288985 IC50 > 6300.0 nM -
CHEMBL3288986 IC50 > 6300.0 nM -
CHEMBL3288987 IC50 > 6300.0 nM -
CHEMBL3288989 IC50 > 6300.0 nM -
CHEMBL3288975 IC50 > 6300.0 nM -
CHEMBL3288991 IC50 > 6300.0 nM -
CHEMBL3288992 IC50 > 6300.0 nM -
CHEMBL3288993 IC50 > 6300.0 nM -
CHEMBL3288979 IC50 > 6300.0 nM -
CHEMBL3288996 IC50 > 6300.0 nM -
CHEMBL3288995 IC50 > 6300.0 nM -
CHEMBL3288998 IC50 > 6300.0 nM -
CHEMBL3288967 IC50 > 6300.0 nM -
CHEMBL3288968 IC50 > 6300.0 nM -
CHEMBL3289000 IC50 > 6300.0 nM -
CHEMBL3288969 IC50 > 6300.0 nM -
CHEMBL3288971 IC50 > 6300.0 nM -
CHEMBL3288962 IC50 > 6300.0 nM -
CHEMBL3289004 IC50 > 6300.0 nM -