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Assay Detail

CHEMBL2394890

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Functional
Antiproliferative activity against human HT-29 cells after 72 hrs by Cell Titer-Glo Assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HT-29
Confidence 1 — Organism
Curated By Autocuration

Target

HT-29 (CHEMBL384)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of TAK-960: an orally available small molecule inhibitor of polo-like kinase 1 (PLK1).
Nie Z, Feher V, Natala S, McBride C, Kiryanov A, Jones B, Lam B, Liu Y, Kaldor S, Stafford J, Hikami K, Uchiyama N, Kawamoto T, Hikichi Y, Matsumoto S, Amano N, Zhang L, Hosfield D, Skene R, Zou H, Cao X, Ichikawa T.
Bioorg Med Chem Lett (2013) 23 : 3662 -3666
PubMed 23664874 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 16 7.60 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2392545 TAK-960 1.0 1 8.52
CHEMBL2392554 1 8.30
CHEMBL2392553 1 8.30
CHEMBL2392558 1 8.22
CHEMBL2392549 1 8.15
CHEMBL2392556 1 8.10
CHEMBL2392548 1 7.80
CHEMBL2392544 1 7.80
CHEMBL2392552 1 7.50
CHEMBL2392547 1 7.40
CHEMBL2392557 1 7.37
CHEMBL2392551 1 7.16
CHEMBL2392550 1 7.02
CHEMBL2392555 1 6.75
CHEMBL2392546 1 6.58
CHEMBL2392543 1 6.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2392545 TAK-960 EC50 = 3.0 nM 8.52
CHEMBL2392554 EC50 = 5.0 nM 8.30
CHEMBL2392553 EC50 = 5.0 nM 8.30
CHEMBL2392558 EC50 = 6.0 nM 8.22
CHEMBL2392549 EC50 = 7.0 nM 8.15
CHEMBL2392556 EC50 = 8.0 nM 8.10
CHEMBL2392548 EC50 = 16.0 nM 7.80
CHEMBL2392544 EC50 = 16.0 nM 7.80
CHEMBL2392552 EC50 = 32.0 nM 7.50
CHEMBL2392547 EC50 = 40.0 nM 7.40
CHEMBL2392557 EC50 = 43.0 nM 7.37
CHEMBL2392551 EC50 = 70.0 nM 7.16
CHEMBL2392550 EC50 = 95.0 nM 7.02
CHEMBL2392555 EC50 = 180.0 nM 6.75
CHEMBL2392546 EC50 = 264.0 nM 6.58
CHEMBL2392543 EC50 = 270.0 nM 6.57