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Assay Detail

CHEMBL1226614

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

Functional
Antiproliferative activity against IC95 biaryl selected drug-resistant against human HCT116 cells after 72 hrs by Cell titer Glo assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HCT-116
Confidence 1 — Organism
Curated By Autocuration

Target

HCT-116 (CHEMBL394)
Type CELL-LINE
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
IC50 3 8.51 9.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3545252 DOCETAXEL 4.0 1 9.74
CHEMBL436624 1 9.00
CHEMBL1222153 1 6.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3545252 DOCETAXEL IC50 = 0.18 nM 9.74
CHEMBL436624 IC50 = 1.0 nM 9.00
CHEMBL1222153 IC50 = 162.0 nM 6.79