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Assay Detail

CHEMBL971730

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Functional
Induction of apoptosis in human HCT116 cells assessed as caspase 3 activation after 24 hrs
26
Total Activities
26
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 2-chloro-N-(4-methoxyphenyl)-N-methylquinazolin-4-amine (EP128265, MPI-0441138) as a potent inducer of apoptosis with high in vivo activity.
Sirisoma N, Kasibhatla S, Pervin A, Zhang H, Jiang S, Willardsen JA, Anderson MB, Baichwal V, Mather GG, Jessing K, Hussain R, Hoang K, Pleiman CM, Tseng B, Drewe J, Cai SX.
J Med Chem (2008) 51 : 4771 -4779
PubMed 18651728 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 26 7.20 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL444724 1 8.70
CHEMBL457612 1 8.30
CHEMBL512022 1 8.10
CHEMBL456790 1 7.89
CHEMBL458063 1 7.82
CHEMBL107 COLCHICINE 4.0 1 7.82
CHEMBL442575 1 7.68
CHEMBL500814 1 7.54
CHEMBL458062 1 7.51
CHEMBL456789 1 7.31
CHEMBL457838 1 7.23
CHEMBL457628 1 7.19
CHEMBL457846 1 7.14
CHEMBL505530 1 6.92
CHEMBL512029 1 6.92
CHEMBL457396 1 6.52
CHEMBL511514 1 6.46
CHEMBL492325 1 6.34
CHEMBL513771 1 6.01
CHEMBL456788 1 5.96
CHEMBL458061 1 5.85
CHEMBL456157 1 -
CHEMBL458032 1 -
CHEMBL457613 1 -
CHEMBL456373 1 -
CHEMBL456374 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL444724 EC50 = 2.0 nM 8.70
CHEMBL457612 EC50 = 5.0 nM 8.30
CHEMBL512022 EC50 = 8.0 nM 8.10
CHEMBL456790 EC50 = 13.0 nM 7.89
CHEMBL458063 EC50 = 15.0 nM 7.82
CHEMBL107 COLCHICINE EC50 = 15.0 nM 7.82
CHEMBL442575 EC50 = 21.0 nM 7.68
CHEMBL500814 EC50 = 29.0 nM 7.54
CHEMBL458062 EC50 = 31.0 nM 7.51
CHEMBL456789 EC50 = 49.0 nM 7.31
CHEMBL457838 EC50 = 59.0 nM 7.23
CHEMBL457628 EC50 = 65.0 nM 7.19
CHEMBL457846 EC50 = 72.0 nM 7.14
CHEMBL505530 EC50 = 120.0 nM 6.92
CHEMBL512029 EC50 = 120.0 nM 6.92
CHEMBL457396 EC50 = 300.0 nM 6.52
CHEMBL511514 EC50 = 350.0 nM 6.46
CHEMBL492325 EC50 = 460.0 nM 6.34
CHEMBL513771 EC50 = 970.0 nM 6.01
CHEMBL456788 EC50 = 1110.0 nM 5.96
CHEMBL458061 EC50 = 1400.0 nM 5.85
CHEMBL456157 EC50 > 10000.0 nM -
CHEMBL458032 EC50 > 10000.0 nM -
CHEMBL457613 EC50 > 10000.0 nM -
CHEMBL456373 EC50 > 10000.0 nM -
CHEMBL456374 EC50 > 10000.0 nM -