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Assay Detail

CHEMBL1008349

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

Functional
Induction of apoptosis in human H1299 cells assessed as caspase activation after 48 hrs by HTS assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type NCI-H1299
Confidence 1 — Organism
Curated By Autocuration

Target

NCI-H1299 (CHEMBL612255)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of 4-anilino-N-methylthieno[3,2-d]pyrimidines and 4-anilino-N-methylthieno[2,3-d]pyrimidines as potent apoptosis inducers.
Kemnitzer W, Sirisoma N, May C, Tseng B, Drewe J, Cai SX.
Bioorg Med Chem Lett (2009) 19 : 3536 -3540
PubMed 19464890 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 28 6.88 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL492399 VERUBULIN 2.0 1 8.22
CHEMBL526313 1 7.82
CHEMBL522221 1 7.80
CHEMBL502898 1 7.60
CHEMBL498221 1 7.50
CHEMBL505903 1 7.36
CHEMBL107 COLCHICINE 4.0 1 7.30
CHEMBL495998 1 7.28
CHEMBL498241 1 7.04
CHEMBL496792 1 6.62
CHEMBL497629 1 6.51
CHEMBL496998 1 6.47
CHEMBL498218 1 6.25
CHEMBL527023 1 6.20
CHEMBL205344 1 6.16
CHEMBL521555 1 5.55
CHEMBL521554 1 5.30
CHEMBL526272 1 -
CHEMBL502065 1 -
CHEMBL453786 1 -
CHEMBL452204 1 -
CHEMBL496425 1 -
CHEMBL496793 1 -
CHEMBL496794 1 -
CHEMBL498217 1 -
CHEMBL452657 1 -
CHEMBL498216 1 -
CHEMBL496186 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL492399 VERUBULIN EC50 = 6.0 nM 8.22
CHEMBL526313 EC50 = 15.0 nM 7.82
CHEMBL522221 EC50 = 16.0 nM 7.80
CHEMBL502898 EC50 = 25.0 nM 7.60
CHEMBL498221 EC50 = 32.0 nM 7.50
CHEMBL505903 EC50 = 44.0 nM 7.36
CHEMBL107 COLCHICINE EC50 = 50.0 nM 7.30
CHEMBL495998 EC50 = 53.0 nM 7.28
CHEMBL498241 EC50 = 91.0 nM 7.04
CHEMBL496792 EC50 = 240.0 nM 6.62
CHEMBL497629 EC50 = 310.0 nM 6.51
CHEMBL496998 EC50 = 340.0 nM 6.47
CHEMBL498218 EC50 = 560.0 nM 6.25
CHEMBL527023 EC50 = 630.0 nM 6.20
CHEMBL205344 EC50 = 700.0 nM 6.16
CHEMBL521555 EC50 = 2800.0 nM 5.55
CHEMBL521554 EC50 = 5000.0 nM 5.30
CHEMBL526272 EC50 > 10000.0 nM -
CHEMBL502065 EC50 > 10000.0 nM -
CHEMBL453786 EC50 > 10000.0 nM -
CHEMBL452204 EC50 > 10000.0 nM -
CHEMBL496425 EC50 > 10000.0 nM -
CHEMBL496793 EC50 > 10000.0 nM -
CHEMBL496794 EC50 > 10000.0 nM -
CHEMBL498217 EC50 > 10000.0 nM -
CHEMBL452657 EC50 > 10000.0 nM -
CHEMBL498216 EC50 > 10000.0 nM -
CHEMBL496186 EC50 > 10000.0 nM -