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Assay Detail

CHEMBL4619353

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 viability after 72 hrs by Celltiter-Glo assay
19
Total Activities
19
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-149 as a Full Antagonist and Efficient Degrader of Estrogen Receptor alpha for ER+ Breast Cancer.
Liang J, Blake R, Chang J, Friedman LS, Goodacre S, Hartman S, Ingalla ER, Kiefer JR, Kleinheinz T, Labadie S, Li J, Lai KW, Liao J, Mody V, McLean N, Metcalfe C, Nannini M, Otwine D, Ran Y, Ray N, Roussel F, Sambrone A, Sampath D, Vinogradova M, Wai J, Wang T, Yeap K, Young A, Zbieg J, Zhang B, Zheng X, Zhong Y, Wang X.
ACS Med Chem Lett (2020) 11 : 1342 -1347
PubMed 32551022 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 8.68 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4447340 1 9.52
CHEMBL4649161 1 9.18
CHEMBL4646522 1 9.09
CHEMBL4644074 1 9.08
CHEMBL4633886 1 9.05
CHEMBL4640902 1 8.89
CHEMBL4644486 1 8.82
CHEMBL4635493 1 8.82
CHEMBL4528514 1 8.80
CHEMBL4645364 1 8.77
CHEMBL4640074 1 8.74
CHEMBL4648503 1 8.64
CHEMBL1358 FULVESTRANT 4.0 1 8.59
CHEMBL4644611 1 8.57
CHEMBL4641732 1 8.52
CHEMBL4638997 1 8.25
CHEMBL4634404 1 8.19
CHEMBL4641773 1 8.07
CHEMBL3581693 BRILANESTRANT 2.0 1 7.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4447340 IC50 = 0.3 nM 9.52
CHEMBL4649161 IC50 = 0.66 nM 9.18
CHEMBL4646522 IC50 = 0.82 nM 9.09
CHEMBL4644074 IC50 = 0.84 nM 9.08
CHEMBL4633886 IC50 = 0.9 nM 9.05
CHEMBL4640902 IC50 = 1.3 nM 8.89
CHEMBL4644486 IC50 = 1.5 nM 8.82
CHEMBL4635493 IC50 = 1.5 nM 8.82
CHEMBL4528514 IC50 = 1.6 nM 8.80
CHEMBL4645364 IC50 = 1.7 nM 8.77
CHEMBL4640074 IC50 = 1.8 nM 8.74
CHEMBL4648503 IC50 = 2.3 nM 8.64
CHEMBL1358 FULVESTRANT IC50 = 2.6 nM 8.59
CHEMBL4644611 IC50 = 2.7 nM 8.57
CHEMBL4641732 IC50 = 3.0 nM 8.52
CHEMBL4638997 IC50 = 5.6 nM 8.25
CHEMBL4634404 IC50 = 6.4 nM 8.19
CHEMBL4641773 IC50 = 8.5 nM 8.07
CHEMBL3581693 BRILANESTRANT IC50 = 44.0 nM 7.36