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Assay Detail

CHEMBL868958

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Functional
Mitotic arrest in A2780 cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type A2780
Confidence 1 — Organism
Curated By Intermediate

Target

A2780 (CHEMBL614004)
Type CELL-LINE
Organism Homo sapiens

Publication

Kinesin spindle protein (KSP) inhibitors. Part 3: synthesis and evaluation of phenolic 2,4-diaryl-2,5-dihydropyrroles with reduced hERG binding and employment of a phosphate prodrug strategy for aqueous solubility.
Garbaccio RM, Fraley ME, Tasber ES, Olson CM, Hoffman WF, Arrington KL, Torrent M, Buser CA, Walsh ES, Hamilton K, Schaber MD, Fernandes C, Lobell RB, Tao W, South VJ, Yan Y, Kuo LC, Prueksaritanont T, Slaughter DE, Shu C, Heimbrook DC, Kohl NE, Huber HE, Hartman GD.
Bioorg Med Chem Lett (2006) 16 : 1780 -1783
PubMed 16439122 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 8.16 8.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL262736 1 8.59
CHEMBL206115 1 8.52
CHEMBL377596 1 8.51
CHEMBL381526 1 8.48
CHEMBL206249 1 8.07
CHEMBL206798 1 8.04
CHEMBL381533 1 7.66
CHEMBL378547 1 7.43
CHEMBL439342 1 -
CHEMBL382994 1 -
CHEMBL202734 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL262736 EC50 = 2.6 nM 8.59
CHEMBL206115 EC50 = 3.0 nM 8.52
CHEMBL377596 EC50 = 3.1 nM 8.51
CHEMBL381526 EC50 = 3.3 nM 8.48
CHEMBL206249 EC50 = 8.5 nM 8.07
CHEMBL206798 EC50 = 9.1 nM 8.04
CHEMBL381533 EC50 = 22.0 nM 7.66
CHEMBL378547 EC50 = 37.0 nM 7.43
CHEMBL439342 EC50 - -
CHEMBL382994 EC50 - -
CHEMBL202734 EC50 - -