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Assay Detail

CHEMBL1226599

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

Binding
Inhibition of human KSP A133D mutant using varying ATP levels in presence of saturating levels of microtubule by Lineweaver-Burke plot
2
Total Activities
2
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

ATP-competitive inhibitors of the mitotic kinesin KSP that function via an allosteric mechanism.
Luo L, Parrish CA, Nevins N, McNulty DE, Chaudhari AM, Carson JD, Sudakin V, Shaw AN, Lehr R, Zhao H, Sweitzer S, Lad L, Wood KW, Sakowicz R, Annan RS, Huang PS, Jackson JR, Dhanak D, Copeland RA, Auger KR.
Nat Chem Biol (2007) 3 : 722 -726
PubMed 17922005 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 8.51 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1222153 1 8.85
CHEMBL243668 1 8.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1222153 Ki = 1.4 nM 8.85
CHEMBL243668 Ki = 6.8 nM 8.17