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Assay Detail

CHEMBL1016165

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

Functional
Induction of apoptosis in human HCT116 cells assessed as caspase activation after 24 hrs by HTS assay
33
Total Activities
33
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

Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration.
Sirisoma N, Pervin A, Zhang H, Jiang S, Willardsen JA, Anderson MB, Mather G, Pleiman CM, Kasibhatla S, Tseng B, Drewe J, Cai SX.
J Med Chem (2009) 52 : 2341 -2351
PubMed 19296653 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 33 7.52 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL474387 1 8.70
CHEMBL522491 1 8.70
CHEMBL444724 1 8.70
CHEMBL516047 1 8.52
CHEMBL492399 VERUBULIN 2.0 1 8.52
CHEMBL515260 1 8.40
CHEMBL474388 1 8.40
CHEMBL492725 1 8.40
CHEMBL444972 1 8.40
CHEMBL522156 1 8.05
CHEMBL493725 1 8.05
CHEMBL450582 1 7.96
CHEMBL474386 1 7.92
CHEMBL492723 1 7.89
CHEMBL475565 1 7.85
CHEMBL506330 1 7.82
CHEMBL475846 1 7.72
CHEMBL473998 1 7.58
CHEMBL483576 1 7.48
CHEMBL450198 1 7.44
CHEMBL493724 1 7.37
CHEMBL483615 1 7.36
CHEMBL492724 1 7.32
CHEMBL453919 1 7.12
CHEMBL503751 1 7.08
CHEMBL475221 1 6.89
CHEMBL483616 1 6.82
CHEMBL475381 1 6.60
CHEMBL492325 1 6.34
CHEMBL475658 1 6.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL474387 EC50 = 2.0 nM 8.70
CHEMBL444724 EC50 = 2.0 nM 8.70
CHEMBL522491 EC50 = 2.0 nM 8.70
CHEMBL516047 EC50 = 3.0 nM 8.52
CHEMBL492399 VERUBULIN EC50 = 3.0 nM 8.52
CHEMBL515260 EC50 = 4.0 nM 8.40
CHEMBL474388 EC50 = 4.0 nM 8.40
CHEMBL492725 EC50 = 4.0 nM 8.40
CHEMBL444972 EC50 = 4.0 nM 8.40
CHEMBL522156 EC50 = 9.0 nM 8.05
CHEMBL493725 EC50 = 9.0 nM 8.05
CHEMBL450582 EC50 = 11.0 nM 7.96
CHEMBL474386 EC50 = 12.0 nM 7.92
CHEMBL492723 EC50 = 13.0 nM 7.89
CHEMBL475565 EC50 = 14.0 nM 7.85
CHEMBL506330 EC50 = 15.0 nM 7.82
CHEMBL475846 EC50 = 19.0 nM 7.72
CHEMBL473998 EC50 = 26.0 nM 7.58
CHEMBL483576 EC50 = 33.0 nM 7.48
CHEMBL450198 EC50 = 36.0 nM 7.44
CHEMBL493724 EC50 = 43.0 nM 7.37
CHEMBL483615 EC50 = 44.0 nM 7.36
CHEMBL492724 EC50 = 48.0 nM 7.32
CHEMBL453919 EC50 = 75.0 nM 7.12
CHEMBL503751 EC50 = 83.0 nM 7.08
CHEMBL475221 EC50 = 130.0 nM 6.89
CHEMBL483616 EC50 = 150.0 nM 6.82
CHEMBL475381 EC50 = 250.0 nM 6.60
CHEMBL492325 EC50 = 460.0 nM 6.34
CHEMBL475658 EC50 = 630.0 nM 6.20
CHEMBL442844 EC50 = 1300.0 nM 5.89
CHEMBL494943 EC50 = 2600.0 nM 5.58
CHEMBL495141 EC50 = 6100.0 nM 5.21