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Assay Detail

CHEMBL4830324

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Functional
Antiproliferative activity against human MDA-MB-453 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MDA-MB-453
Confidence 1 — Organism
Curated By Autocuration

Target

MDA-MB-453 (CHEMBL614334)
Type CELL-LINE
Organism Homo sapiens

Publication

X-ray Crystallography-Guided Design, Antitumor Efficacy, and QSAR Analysis of Metabolically Stable Cyclopenta-Pyrimidinyl Dihydroquinoxalinone as a Potent Tubulin Polymerization Inhibitor.
Banerjee S, Mahmud F, Deng S, Ma L, Yun MK, Fakayode SO, Arnst KE, Yang L, Chen H, Wu Z, Lukka PB, Parmar K, Meibohm B, White SW, Wang Y, Li W, Miller DD.
J Med Chem (2021) 64 : 13072 -13095
PubMed 34406768 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 7.73 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4855608 1 9.30
CHEMBL428647 PACLITAXEL 4.0 1 9.15
CHEMBL4871913 1 9.00
CHEMBL4520878 1 8.92
CHEMBL4876166 1 8.85
CHEMBL4879163 1 8.43
CHEMBL4850900 1 8.35
CHEMBL4876313 1 8.34
CHEMBL4878879 1 8.31
CHEMBL107 COLCHICINE 4.0 1 8.24
CHEMBL4858577 1 8.14
CHEMBL4845756 1 7.51
CHEMBL4855607 1 7.38
CHEMBL4857102 1 7.37
CHEMBL4088019 1 6.98
CHEMBL4849437 1 6.89
CHEMBL4863678 1 6.71
CHEMBL4075372 1 6.42
CHEMBL4864654 1 6.25
CHEMBL4861176 1 6.16
CHEMBL4877188 1 5.59
CHEMBL4859195 1 -
CHEMBL4878065 1 -
CHEMBL4059730 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4855608 IC50 = 0.5 nM 9.30
CHEMBL428647 PACLITAXEL IC50 = 0.7 nM 9.15
CHEMBL4871913 IC50 = 1.0 nM 9.00
CHEMBL4520878 IC50 = 1.2 nM 8.92
CHEMBL4876166 IC50 = 1.4 nM 8.85
CHEMBL4879163 IC50 = 3.7 nM 8.43
CHEMBL4850900 IC50 = 4.5 nM 8.35
CHEMBL4876313 IC50 = 4.6 nM 8.34
CHEMBL4878879 IC50 = 4.9 nM 8.31
CHEMBL107 COLCHICINE IC50 = 5.8 nM 8.24
CHEMBL4858577 IC50 = 7.3 nM 8.14
CHEMBL4845756 IC50 = 30.6 nM 7.51
CHEMBL4855607 IC50 = 42.0 nM 7.38
CHEMBL4857102 IC50 = 43.0 nM 7.37
CHEMBL4088019 IC50 = 105.4 nM 6.98
CHEMBL4849437 IC50 = 129.0 nM 6.89
CHEMBL4863678 IC50 = 193.0 nM 6.71
CHEMBL4075372 IC50 = 378.7 nM 6.42
CHEMBL4864654 IC50 = 556.3 nM 6.25
CHEMBL4861176 IC50 = 692.6 nM 6.16
CHEMBL4877188 IC50 = 2562.0 nM 5.59
CHEMBL4859195 IC50 > 1000.0 nM -
CHEMBL4878065 IC50 > 1000.0 nM -
CHEMBL4059730 IC50 > 1000.0 nM -