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Assay Detail

CHEMBL4356679

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Functional
Antiproliferative activity against human MCF7:5C cells assessed as reduction in cell viability incubated for 7 days by Hoechst 33258 dye based assay
23
Total Activities
23
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Design and Synthesis of Basic Selective Estrogen Receptor Degraders for Endocrine Therapy Resistant Breast Cancer.
Lu Y, Gutgesell LM, Xiong R, Zhao J, Li Y, Rosales CI, Hollas M, Shen Z, Gordon-Blake J, Dye K, Wang Y, Lee S, Chen H, He D, Dubrovyskyii O, Zhao H, Huang F, Lasek AW, Tonetti DA, Thatcher GRJ.
J Med Chem (2019) 62 : 11301 -11323
PubMed 31746603 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 9.38 10.06
pIC50 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4447374 1 10.06
CHEMBL4538085 1 9.93
CHEMBL4564385 1 9.92
CHEMBL4436415 1 9.85
CHEMBL4586663 1 9.79
CHEMBL4547439 1 9.74
CHEMBL4515212 1 9.58
CHEMBL4527655 1 9.58
CHEMBL4441662 1 9.53
CHEMBL4533964 1 9.46
CHEMBL4578883 1 9.44
CHEMBL4483006 1 9.42
CHEMBL4524872 1 9.35
CHEMBL4532671 1 9.02
CHEMBL4436707 1 9.00
CHEMBL4440649 1 8.97
CHEMBL4516021 1 8.89
CHEMBL1358 FULVESTRANT 4.0 1 8.76
CHEMBL4543096 1 8.67
CHEMBL4448178 1 8.55
CHEMBL4562548 1 -
CHEMBL4464171 1 -
CHEMBL81 RALOXIFENE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4447374 IC50 = 0.0871 nM 10.06
CHEMBL4538085 IC50 = 0.1175 nM 9.93
CHEMBL4564385 IC50 = 0.1202 nM 9.92
CHEMBL4436415 IC50 = 0.1413 nM 9.85
CHEMBL4586663 IC50 = 0.1622 nM 9.79
CHEMBL4547439 IC50 = 0.182 nM 9.74
CHEMBL4515212 IC50 = 0.263 nM 9.58
CHEMBL4527655 IC50 = 0.263 nM 9.58
CHEMBL4441662 IC50 = 0.2951 nM 9.53
CHEMBL4533964 IC50 = 0.3467 nM 9.46
CHEMBL4578883 IC50 = 0.3631 nM 9.44
CHEMBL4483006 IC50 = 0.3802 nM 9.42
CHEMBL4524872 IC50 = 0.4467 nM 9.35
CHEMBL4532671 IC50 = 0.955 nM 9.02
CHEMBL4436707 IC50 = 1.0 nM 9.00
CHEMBL4440649 IC50 = 1.072 nM 8.97
CHEMBL4516021 IC50 = 1.288 nM 8.89
CHEMBL1358 FULVESTRANT IC50 = 1.738 nM 8.76
CHEMBL4543096 IC50 = 2.138 nM 8.67
CHEMBL4448178 IC50 = 2.818 nM 8.55
CHEMBL4562548 pIC50 - -
CHEMBL4464171 IC50 > 100.0 nM -
CHEMBL81 RALOXIFENE pIC50 - -