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Assay Detail

CHEMBL940954

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Binding
Inhibition of kinesin spindle protein by ATPase assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

Kinesin spindle protein (KSP) inhibitors. Part 8: Design and synthesis of 1,4-diaryl-4,5-dihydropyrazoles as potent inhibitors of the mitotic kinesin KSP.
Roecker AJ, Coleman PJ, Mercer SP, Schreier JD, Buser CA, Walsh ES, Hamilton K, Lobell RB, Tao W, Diehl RE, South VJ, Davide JP, Kohl NE, Yan Y, Kuo LC, Li C, Fernandez-Metzler C, Mahan EA, Prueksaritanont T, Hartman GD.
Bioorg Med Chem Lett (2007) 17 : 5677 -5682
PubMed 17766111 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 8.46 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL247044 1 9.70
CHEMBL246603 1 8.92
CHEMBL250125 1 8.80
CHEMBL443490 1 8.70
CHEMBL246604 1 8.68
CHEMBL248400 1 8.42
CHEMBL246422 1 8.42
CHEMBL247414 1 8.41
CHEMBL246000 1 8.40
CHEMBL246001 1 8.38
CHEMBL392599 1 8.33
CHEMBL248244 1 8.28
CHEMBL247594 1 8.00
CHEMBL401006 1 7.78
CHEMBL393647 1 7.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL247044 IC50 = 0.2 nM 9.70
CHEMBL246603 IC50 = 1.2 nM 8.92
CHEMBL250125 IC50 = 1.6 nM 8.80
CHEMBL443490 IC50 = 2.0 nM 8.70
CHEMBL246604 IC50 = 2.1 nM 8.68
CHEMBL248400 IC50 = 3.8 nM 8.42
CHEMBL246422 IC50 = 3.8 nM 8.42
CHEMBL247414 IC50 = 3.9 nM 8.41
CHEMBL246000 IC50 = 4.0 nM 8.40
CHEMBL246001 IC50 = 4.2 nM 8.38
CHEMBL392599 IC50 = 4.7 nM 8.33
CHEMBL248244 IC50 = 5.2 nM 8.28
CHEMBL247594 IC50 = 10.1 nM 8.00
CHEMBL401006 IC50 = 16.5 nM 7.78
CHEMBL393647 IC50 = 21.8 nM 7.66