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Assay Detail

CHEMBL5326435

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Toxicity
Cytotoxicity against human MCF-10A cells incubated for 72 hrs by CCK8 assay
51
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Toxicity
Organism Homo sapiens
Cell Type MCF-10A
Confidence 1 — Organism
Curated By Autocuration

Target

MCF-10A (CHEMBL614321)
Type CELL-LINE
Organism Homo sapiens

Publication

Structure-guided identification of novel dual-targeting estrogen receptor α degraders with aromatase inhibitory activity for the treatment of endocrine-resistant breast cancer.
Xin L, Min J, Hu H, Li Y, Du C, Xie B, Cheng Y, Deng X, Deng X, Shen K, Huang J, Chen CC, Guo RT, Dong C, Zhou HB.
Eur J Med Chem (2023) 253 : 115328 -115328
PubMed 37037140 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 51 4.57 4.86

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5426251 1 4.86
CHEMBL5405944 1 4.77
CHEMBL5423258 1 4.76
CHEMBL5437007 1 4.75
CHEMBL489 AFIMOXIFENE 3.0 1 4.67
CHEMBL5396802 1 4.66
CHEMBL5426947 1 4.63
CHEMBL5394546 1 4.60
CHEMBL5404063 1 4.58
CHEMBL5414659 1 4.54
CHEMBL5433442 1 4.36
CHEMBL5410004 1 4.29
CHEMBL5398724 1 4.29
CHEMBL4800654 1 4.24
CHEMBL5398866 1 -
CHEMBL5432102 1 -
CHEMBL5394879 1 -
CHEMBL5423408 1 -
CHEMBL5428681 1 -
CHEMBL5423781 1 -
CHEMBL5418690 1 -
CHEMBL5414261 1 -
CHEMBL5394007 1 -
CHEMBL5419649 1 -
CHEMBL5436713 1 -
CHEMBL5424929 1 -
CHEMBL5403080 1 -
CHEMBL5433532 1 -
CHEMBL5402392 1 -
CHEMBL5413340 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5426251 IC50 = 13670.0 nM 4.86
CHEMBL5405944 IC50 = 16890.0 nM 4.77
CHEMBL5423258 IC50 = 17300.0 nM 4.76
CHEMBL5437007 IC50 = 17980.0 nM 4.75
CHEMBL489 AFIMOXIFENE IC50 = 21500.0 nM 4.67
CHEMBL5396802 IC50 = 21720.0 nM 4.66
CHEMBL5426947 IC50 = 23350.0 nM 4.63
CHEMBL5394546 IC50 = 25240.0 nM 4.60
CHEMBL5404063 IC50 = 26330.0 nM 4.58
CHEMBL5414659 IC50 = 28570.0 nM 4.54
CHEMBL5433442 IC50 = 43400.0 nM 4.36
CHEMBL5410004 IC50 = 51250.0 nM 4.29
CHEMBL5398724 IC50 = 50880.0 nM 4.29
CHEMBL4800654 IC50 = 57000.0 nM 4.24
CHEMBL5403786 IC50 > 100000.0 nM -
CHEMBL5436925 IC50 > 100000.0 nM -
CHEMBL5412790 IC50 > 100000.0 nM -
CHEMBL5411799 IC50 > 100000.0 nM -
CHEMBL5400803 IC50 > 100000.0 nM -
CHEMBL5420394 IC50 > 100000.0 nM -
CHEMBL5417452 IC50 > 100000.0 nM -
CHEMBL5422315 IC50 > 100000.0 nM -
CHEMBL5401146 IC50 > 100000.0 nM -
CHEMBL5421409 IC50 > 100000.0 nM -
CHEMBL5414572 IC50 > 100000.0 nM -
CHEMBL5427513 IC50 > 100000.0 nM -
CHEMBL5400203 IC50 > 100000.0 nM -
CHEMBL5399056 IC50 > 100000.0 nM -
CHEMBL5404699 IC50 > 100000.0 nM -
CHEMBL1444 LETROZOLE IC50 > 100000.0 nM -
CHEMBL5426175 IC50 > 100000.0 nM -
CHEMBL5407335 IC50 > 100000.0 nM -
CHEMBL5414261 IC50 > 100000.0 nM -
CHEMBL5413340 IC50 > 100000.0 nM -
CHEMBL5402392 IC50 > 100000.0 nM -
CHEMBL5433532 IC50 > 100000.0 nM -
CHEMBL5403080 IC50 > 100000.0 nM -
CHEMBL5424929 IC50 > 100000.0 nM -
CHEMBL5436713 IC50 > 100000.0 nM -
CHEMBL5419649 IC50 > 100000.0 nM -
CHEMBL5394007 IC50 > 100000.0 nM -
CHEMBL5408038 IC50 > 100000.0 nM -
CHEMBL5418690 IC50 > 100000.0 nM -
CHEMBL5423781 IC50 > 100000.0 nM -
CHEMBL5428681 IC50 > 100000.0 nM -
CHEMBL5423408 IC50 > 100000.0 nM -
CHEMBL5394879 IC50 > 100000.0 nM -
CHEMBL5432102 IC50 > 100000.0 nM -
CHEMBL5398866 IC50 > 100000.0 nM -
CHEMBL1358 FULVESTRANT IC50 > 100000.0 nM -