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Assay Detail

CHEMBL4151746

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

Functional
Antiproliferative activity against human MCF7 cells assessed as reduction in cell proliferation in RPMI containing 10% FBS incubated for 5 days by Cell-titer-Glo assay
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MCF7
Confidence 1 — Organism
Curated By Intermediate

Target

MCF7 (CHEMBL387)
Type CELL-LINE
Organism Homo sapiens

Publication

Identification of an Orally Bioavailable Chromene-Based Selective Estrogen Receptor Degrader (SERD) That Demonstrates Robust Activity in a Model of Tamoxifen-Resistant Breast Cancer.
Nagasawa J, Govek S, Kahraman M, Lai A, Bonnefous C, Douglas K, Sensintaffar J, Lu N, Lee K, Aparicio A, Kaufman J, Qian J, Shao G, Prudente R, Joseph JD, Darimont B, Brigham D, Maheu K, Heyman R, Rix PJ, Hager JH, Smith ND.
J Med Chem (2018) 61 : 7917 -7928
PubMed 30086626 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 9.37 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4164869 1 10.00
CHEMBL4168008 1 10.00
CHEMBL4159755 1 10.00
CHEMBL4164133 1 10.00
CHEMBL4171078 1 9.70
CHEMBL4161695 1 9.70
CHEMBL4163162 1 9.70
CHEMBL4175179 1 9.70
CHEMBL4161455 1 9.70
CHEMBL4176563 1 9.70
CHEMBL4164447 1 9.70
CHEMBL4175085 1 9.70
CHEMBL4171332 1 9.70
CHEMBL4160734 1 9.70
CHEMBL4174789 1 9.70
CHEMBL4169918 1 9.70
CHEMBL4162508 1 9.70
CHEMBL4163562 1 9.52
CHEMBL4167575 1 9.52
CHEMBL4169627 1 9.52
CHEMBL4169959 1 9.40
CHEMBL4167152 1 9.40
CHEMBL4165638 1 9.00
CHEMBL4175025 1 8.59
CHEMBL4159900 1 8.37
CHEMBL4170549 1 8.00
CHEMBL4173984 1 7.57
CHEMBL4159656 1 7.23
CHEMBL4165523 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4164869 IC50 = 0.1 nM 10.00
CHEMBL4168008 IC50 = 0.1 nM 10.00
CHEMBL4159755 IC50 = 0.1 nM 10.00
CHEMBL4164133 IC50 = 0.1 nM 10.00
CHEMBL4171078 IC50 = 0.2 nM 9.70
CHEMBL4161695 IC50 = 0.2 nM 9.70
CHEMBL4163162 IC50 = 0.2 nM 9.70
CHEMBL4175179 IC50 = 0.2 nM 9.70
CHEMBL4161455 IC50 = 0.2 nM 9.70
CHEMBL4176563 IC50 = 0.2 nM 9.70
CHEMBL4164447 IC50 = 0.2 nM 9.70
CHEMBL4175085 IC50 = 0.2 nM 9.70
CHEMBL4171332 IC50 = 0.2 nM 9.70
CHEMBL4160734 IC50 = 0.2 nM 9.70
CHEMBL4174789 IC50 = 0.2 nM 9.70
CHEMBL4169918 IC50 = 0.2 nM 9.70
CHEMBL4162508 IC50 = 0.2 nM 9.70
CHEMBL4163562 IC50 = 0.3 nM 9.52
CHEMBL4167575 IC50 = 0.3 nM 9.52
CHEMBL4169627 IC50 = 0.3 nM 9.52
CHEMBL4169959 IC50 = 0.4 nM 9.40
CHEMBL4167152 IC50 = 0.4 nM 9.40
CHEMBL4165638 IC50 = 1.0 nM 9.00
CHEMBL4175025 IC50 = 2.6 nM 8.59
CHEMBL4159900 IC50 = 4.3 nM 8.37
CHEMBL4170549 IC50 = 10.0 nM 8.00
CHEMBL4173984 IC50 = 27.0 nM 7.57
CHEMBL4159656 IC50 = 59.0 nM 7.23
CHEMBL4165523 IC50 - -