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Assay Detail

CHEMBL1687607

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Functional
Antiproliferative activity against human HCT15 cells assessed as growth inhibition
26
Total Activities
26
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 I: Compounds containing a lipophilic C32 side chain overcome P-glycoprotein susceptibility.
Narayan S, Carlson EM, Cheng H, Du H, Hu Y, Jiang Y, Lewis BM, Seletsky BM, Tendyke K, Zhang H, Zheng W, Littlefield BA, Towle MJ, Yu MJ.
Bioorg Med Chem Lett (2011) 21 : 1630 -1633
PubMed 21324686 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 8.95 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1683529 1 9.70
CHEMBL1683523 1 9.68
CHEMBL1683522 1 9.66
CHEMBL1683528 1 9.66
CHEMBL1683530 1 9.64
CHEMBL1683543 1 9.62
CHEMBL1683525 1 9.49
CHEMBL1683539 1 9.40
CHEMBL1683538 1 9.40
CHEMBL1683537 1 9.36
CHEMBL1683534 1 9.32
CHEMBL1683524 1 9.26
CHEMBL1683535 1 9.21
CHEMBL1683532 1 9.21
CHEMBL1683527 1 9.17
CHEMBL1683542 1 9.17
CHEMBL1683540 1 9.08
CHEMBL1683526 1 8.91
CHEMBL1683533 1 8.15
CHEMBL1683536 1 7.74
CHEMBL159 VINBLASTINE 4.0 1 7.54
CHEMBL53463 DOXORUBICIN 4.0 1 6.81
CHEMBL1683590 ERIBULIN 4.0 1 6.69
CHEMBL1683531 1 -
CHEMBL1683541 1 -
CHEMBL428647 PACLITAXEL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1683529 IC50 = 0.2 nM 9.70
CHEMBL1683523 IC50 = 0.21 nM 9.68
CHEMBL1683522 IC50 = 0.22 nM 9.66
CHEMBL1683528 IC50 = 0.22 nM 9.66
CHEMBL1683530 IC50 = 0.23 nM 9.64
CHEMBL1683543 IC50 = 0.24 nM 9.62
CHEMBL1683525 IC50 = 0.32 nM 9.49
CHEMBL1683539 IC50 = 0.4 nM 9.40
CHEMBL1683538 IC50 = 0.4 nM 9.40
CHEMBL1683537 IC50 = 0.44 nM 9.36
CHEMBL1683534 IC50 = 0.48 nM 9.32
CHEMBL1683524 IC50 = 0.55 nM 9.26
CHEMBL1683535 IC50 = 0.61 nM 9.21
CHEMBL1683532 IC50 = 0.62 nM 9.21
CHEMBL1683527 IC50 = 0.67 nM 9.17
CHEMBL1683542 IC50 = 0.68 nM 9.17
CHEMBL1683540 IC50 = 0.83 nM 9.08
CHEMBL1683526 IC50 = 1.24 nM 8.91
CHEMBL1683533 IC50 = 7.08 nM 8.15
CHEMBL1683536 IC50 = 18.3 nM 7.74
CHEMBL159 VINBLASTINE IC50 = 28.5 nM 7.54
CHEMBL53463 DOXORUBICIN IC50 = 153.95 nM 6.81
CHEMBL1683590 ERIBULIN IC50 = 204.0 nM 6.69
CHEMBL1683531 IC50 - -
CHEMBL1683541 IC50 - -
CHEMBL428647 PACLITAXEL IC50 - -