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Assay Detail

CHEMBL1695276

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

Functional
Cell cycle arrest in human A431 cells assessed as accumulation at G2/M phase after 24 hrs using propidium iodide staining by cell sorting method
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type A-431
Confidence 1 — Organism
Curated By Autocuration

Target

A-431 (CHEMBL614069)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of Dual VEGFR-2 and Tubulin Inhibitors with in Vivo Efficacy.
Chekler EL, Kiselyov AS, Ouyang X, Chen X, Pattaropong V, Wang Y, Tuma MC, Doody JF.
ACS Med Chem Lett (2010) 1 : 488 -492
PubMed 24900236 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 28 7.50 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1087218 1 8.05
CHEMBL1688350 1 8.00
CHEMBL203062 1 7.89
CHEMBL205166 1 7.80
CHEMBL203642 1 7.75
CHEMBL204754 1 7.75
CHEMBL1688352 1 7.75
CHEMBL204710 1 7.70
CHEMBL382359 1 7.51
CHEMBL1688351 1 7.47
CHEMBL381122 1 7.31
CHEMBL1688345 1 6.28
CHEMBL1087349 1 6.21
CHEMBL1688247 1 -
CHEMBL1688248 1 -
CHEMBL1688249 1 -
CHEMBL1688250 1 -
CHEMBL1688344 1 -
CHEMBL1688346 1 -
CHEMBL1688347 1 -
CHEMBL1688348 1 -
CHEMBL1688349 1 -
CHEMBL1688246 1 -
CHEMBL1688356 1 -
CHEMBL1688355 1 -
CHEMBL1688354 1 -
CHEMBL1688353 1 -
CHEMBL1688357 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1087218 EC50 = 9.0 nM 8.05
CHEMBL1688350 EC50 = 10.0 nM 8.00
CHEMBL203062 EC50 = 13.0 nM 7.89
CHEMBL205166 EC50 = 16.0 nM 7.80
CHEMBL203642 EC50 = 18.0 nM 7.75
CHEMBL204754 EC50 = 18.0 nM 7.75
CHEMBL1688352 EC50 = 18.0 nM 7.75
CHEMBL204710 EC50 = 20.0 nM 7.70
CHEMBL382359 EC50 = 31.0 nM 7.51
CHEMBL1688351 EC50 = 34.0 nM 7.47
CHEMBL381122 EC50 = 49.0 nM 7.31
CHEMBL1688345 EC50 = 520.0 nM 6.28
CHEMBL1087349 EC50 = 620.0 nM 6.21
CHEMBL1688247 EC50 > 10000.0 nM -
CHEMBL1688248 EC50 > 10000.0 nM -
CHEMBL1688249 EC50 > 10000.0 nM -
CHEMBL1688250 EC50 > 10000.0 nM -
CHEMBL1688344 EC50 > 10000.0 nM -
CHEMBL1688346 EC50 > 10000.0 nM -
CHEMBL1688347 EC50 > 10000.0 nM -
CHEMBL1688348 EC50 > 10000.0 nM -
CHEMBL1688349 EC50 > 10000.0 nM -
CHEMBL1688246 EC50 > 10000.0 nM -
CHEMBL1688356 EC50 > 10000.0 nM -
CHEMBL1688355 EC50 > 10000.0 nM -
CHEMBL1688354 EC50 > 10000.0 nM -
CHEMBL1688353 EC50 > 10000.0 nM -
CHEMBL1688357 EC50 > 10000.0 nM -