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Assay Detail

CHEMBL1685513

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Functional
Cytotoxicity against human MES-SA cells
ChEMBL ↗
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MES-SA
Confidence 1 — Organism
Curated By Autocuration

Target

NON-PROTEIN TARGET (CHEMBL3879801) ↗
Type NON-MOLECULAR

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 9.45 10.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1683596 — — 1 10.15
CHEMBL1683595 — — 1 10.10
CHEMBL1683550 — — 1 9.96
CHEMBL1683546 — — 1 9.92
CHEMBL1683601 — — 1 9.89
CHEMBL1683605 — — 1 9.89
CHEMBL1683597 — — 1 9.89
CHEMBL1683598 — — 1 9.89
CHEMBL1683602 — — 1 9.85
CHEMBL1683594 — — 1 9.82
CHEMBL1683599 — — 1 9.80
CHEMBL1683554 — — 1 9.80
CHEMBL1683592 — — 1 9.77
CHEMBL1683591 — — 1 9.77
CHEMBL1683556 — — 1 9.74
CHEMBL1683553 — — 1 9.64
CHEMBL1683549 — — 1 9.64
CHEMBL1683551 — — 1 9.60
CHEMBL1683603 — — 1 9.55
CHEMBL1683593 — — 1 9.16
CHEMBL1683590 ERIBULIN 4.0 1 8.78
CHEMBL1683547 — — 1 8.72
CHEMBL1683604 — — 1 8.66
CHEMBL159 VINBLASTINE 4.0 1 8.64
CHEMBL428647 PACLITAXEL 4.0 1 8.53
CHEMBL1683600 — — 1 8.50
CHEMBL53463 DOXORUBICIN 4.0 1 7.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1683596 — IC50 = 0.07 nM 10.15
CHEMBL1683595 — IC50 = 0.08 nM 10.10
CHEMBL1683550 — IC50 = 0.11 nM 9.96
CHEMBL1683546 — IC50 = 0.12 nM 9.92
CHEMBL1683601 — IC50 = 0.13 nM 9.89
CHEMBL1683605 — IC50 = 0.13 nM 9.89
CHEMBL1683597 — IC50 = 0.13 nM 9.89
CHEMBL1683598 — IC50 = 0.13 nM 9.89
CHEMBL1683602 — IC50 = 0.14 nM 9.85
CHEMBL1683594 — IC50 = 0.15 nM 9.82
CHEMBL1683599 — IC50 = 0.16 nM 9.80
CHEMBL1683554 — IC50 = 0.16 nM 9.80
CHEMBL1683592 — IC50 = 0.17 nM 9.77
CHEMBL1683591 — IC50 = 0.17 nM 9.77
CHEMBL1683556 — IC50 = 0.18 nM 9.74
CHEMBL1683553 — IC50 = 0.23 nM 9.64
CHEMBL1683549 — IC50 = 0.23 nM 9.64
CHEMBL1683551 — IC50 = 0.25 nM 9.60
CHEMBL1683603 — IC50 = 0.28 nM 9.55
CHEMBL1683593 — IC50 = 0.69 nM 9.16
CHEMBL1683590 ERIBULIN IC50 = 1.66 nM 8.78
CHEMBL1683547 — IC50 = 1.91 nM 8.72
CHEMBL1683604 — IC50 = 2.17 nM 8.66
CHEMBL159 VINBLASTINE IC50 = 2.28 nM 8.64
CHEMBL428647 PACLITAXEL IC50 = 2.96 nM 8.53
CHEMBL1683600 — IC50 = 3.16 nM 8.50
CHEMBL53463 DOXORUBICIN IC50 = 26.4 nM 7.58