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Assay Detail

CHEMBL941922

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

Functional
Antiproliferative activity against HeLa cells assessed as G2/M arrest by MTS assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HeLa
Confidence 1 — Organism
Curated By Autocuration

Target

HeLa (CHEMBL399)
Type CELL-LINE
Organism Homo sapiens

Publication

Cyanopyridyl containing 1,4-dihydroindeno[1,2-c]pyrazoles as potent checkpoint kinase 1 inhibitors: improving oral biovailability.
Tong Y, Przytulinska M, Tao ZF, Bouska J, Stewart KD, Park C, Li G, Claiborne A, Kovar P, Chen Z, Merta PJ, Bui MH, Olson A, Osterling D, Zhang H, Sham HL, Rosenberg SH, Sowin TJ, Lin NH.
Bioorg Med Chem Lett (2007) 17 : 5665 -5670
PubMed 17768051 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 21 4.99 5.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL248910 1 5.57
CHEMBL248720 1 5.40
CHEMBL248719 1 5.27
CHEMBL398754 1 5.21
CHEMBL249077 1 5.12
CHEMBL249114 1 5.09
CHEMBL249323 1 5.01
CHEMBL398951 1 4.68
CHEMBL400797 1 4.54
CHEMBL249116 1 4.48
CHEMBL249283 1 4.48
CHEMBL248911 1 -
CHEMBL245796 1 -
CHEMBL249115 1 -
CHEMBL400570 1 -
CHEMBL249324 1 -
CHEMBL251755 1 -
CHEMBL249076 1 -
CHEMBL249282 1 -
CHEMBL401177 1 -
CHEMBL398750 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL248910 EC50 = 2700.0 nM 5.57
CHEMBL248720 EC50 = 4000.0 nM 5.40
CHEMBL248719 EC50 = 5400.0 nM 5.27
CHEMBL398754 EC50 = 6200.0 nM 5.21
CHEMBL249077 EC50 = 7600.0 nM 5.12
CHEMBL249114 EC50 = 8100.0 nM 5.09
CHEMBL249323 EC50 = 9700.0 nM 5.01
CHEMBL398951 EC50 = 21000.0 nM 4.68
CHEMBL400797 EC50 = 29000.0 nM 4.54
CHEMBL249116 EC50 = 33000.0 nM 4.48
CHEMBL249283 EC50 = 33000.0 nM 4.48
CHEMBL248911 EC50 > 59000.0 nM -
CHEMBL245796 EC50 > 59000.0 nM -
CHEMBL249115 EC50 > 59000.0 nM -
CHEMBL400570 EC50 > 59000.0 nM -
CHEMBL249324 EC50 > 59000.0 nM -
CHEMBL251755 EC50 > 59000.0 nM -
CHEMBL249076 EC50 > 59000.0 nM -
CHEMBL249282 EC50 > 59000.0 nM -
CHEMBL401177 EC50 > 52000.0 nM -
CHEMBL398750 EC50 > 59000.0 nM -