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Assay Detail

CHEMBL1685517

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Functional
Cytotoxicity against human HCT15 cells
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HCT-15
Confidence 1 — Organism
Curated By Autocuration

Target

HCT-15 (CHEMBL612263)
Type CELL-LINE
Organism Homo sapiens

Publication

Novel second generation analogs of eribulin. Part II: Orally available and active against resistant tumors in vivo.
Narayan S, Carlson EM, Cheng H, Condon K, Du H, Eckley S, Hu Y, Jiang Y, Kumar V, Lewis BM, Saxton P, Schuck E, Seletsky BM, Tendyke K, Zhang H, Zheng W, Littlefield BA, Towle MJ, Yu MJ.
Bioorg Med Chem Lett (2011) 21 : 1634 -1638
PubMed 21324692 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 9.06 9.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1683550 1 9.85
CHEMBL1683602 1 9.82
CHEMBL1683546 1 9.80
CHEMBL1683605 1 9.77
CHEMBL1683556 1 9.72
CHEMBL1683554 1 9.70
CHEMBL1683592 1 9.68
CHEMBL1683601 1 9.68
CHEMBL1683596 1 9.66
CHEMBL1683553 1 9.47
CHEMBL1683594 1 9.44
CHEMBL1683603 1 9.43
CHEMBL1683597 1 9.40
CHEMBL1683549 1 9.34
CHEMBL1683551 1 9.34
CHEMBL1683600 1 9.21
CHEMBL1683598 1 9.17
CHEMBL1683599 1 9.11
CHEMBL1683593 1 9.05
CHEMBL1683547 1 8.51
CHEMBL1683604 1 8.27
CHEMBL1683591 1 8.07
CHEMBL159 VINBLASTINE 4.0 1 7.54
CHEMBL53463 DOXORUBICIN 4.0 1 6.81
CHEMBL1683590 ERIBULIN 4.0 1 6.69
CHEMBL1683595 1 -
CHEMBL428647 PACLITAXEL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1683550 IC50 = 0.14 nM 9.85
CHEMBL1683602 IC50 = 0.15 nM 9.82
CHEMBL1683546 IC50 = 0.16 nM 9.80
CHEMBL1683605 IC50 = 0.17 nM 9.77
CHEMBL1683556 IC50 = 0.19 nM 9.72
CHEMBL1683554 IC50 = 0.2 nM 9.70
CHEMBL1683592 IC50 = 0.21 nM 9.68
CHEMBL1683601 IC50 = 0.21 nM 9.68
CHEMBL1683596 IC50 = 0.22 nM 9.66
CHEMBL1683553 IC50 = 0.34 nM 9.47
CHEMBL1683594 IC50 = 0.36 nM 9.44
CHEMBL1683603 IC50 = 0.37 nM 9.43
CHEMBL1683597 IC50 = 0.4 nM 9.40
CHEMBL1683549 IC50 = 0.46 nM 9.34
CHEMBL1683551 IC50 = 0.46 nM 9.34
CHEMBL1683600 IC50 = 0.62 nM 9.21
CHEMBL1683598 IC50 = 0.67 nM 9.17
CHEMBL1683599 IC50 = 0.78 nM 9.11
CHEMBL1683593 IC50 = 0.89 nM 9.05
CHEMBL1683547 IC50 = 3.11 nM 8.51
CHEMBL1683604 IC50 = 5.4 nM 8.27
CHEMBL1683591 IC50 = 8.57 nM 8.07
CHEMBL159 VINBLASTINE IC50 = 28.5 nM 7.54
CHEMBL53463 DOXORUBICIN IC50 = 153.95 nM 6.81
CHEMBL1683590 ERIBULIN IC50 = 204.0 nM 6.69
CHEMBL1683595 IC50 - -
CHEMBL428647 PACLITAXEL IC50 - -