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Assay Detail

CHEMBL4810888

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

Functional
Antiproliferation activity against human MCF7 cells assessed as reduction in cell viability measured by CellTiter-Glo luminescent assay assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

MCF7 (CHEMBL387)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of GNE-502 as an orally bioavailable and potent degrader for estrogen receptor positive breast cancer.
Zbieg JR, Liang J, Li J, Blake RA, Chang J, Friedman L, Goodacre S, Hartman SJ, Rei Ingalla E, Kiefer JR, Kleinheinz T, Labadie S, Lai T, Liao J, McLean N, Metcalfe C, Mody V, Nannini M, Ortwine DF, Ran Y, Ray N, Roussel F, Sambrone A, Sampath D, Vinogradova M, Wai J, Wang T, Yeap K, Zhang B, Zheng X, Zhong Y, Wang X.
Bioorg Med Chem Lett (2021) 50 : 128335 -128335
PubMed 34425201 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 9.30 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4877968 1 9.40
CHEMBL4851830 1 9.30
CHEMBL4849978 1 9.30
CHEMBL4649161 1 9.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4877968 IC50 = 0.4 nM 9.40
CHEMBL4851830 IC50 = 0.5 nM 9.30
CHEMBL4849978 IC50 = 0.5 nM 9.30
CHEMBL4649161 IC50 = 0.66 nM 9.18