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Assay Detail

CHEMBL4333841

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

Functional
Antiproliferative activity against human MCF7 cells after 5 days by CellTiter-Glo assay
13
Total Activities
13
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

Maximizing ER-α Degradation Maximizes Activity in a Tamoxifen-Resistant Breast Cancer Model: Identification of GDC-0927.
Kahraman M, Govek SP, Nagasawa JY, Lai A, Bonnefous C, Douglas K, Sensintaffar J, Liu N, Lee K, Aparicio A, Kaufman J, Qian J, Shao G, Prudente R, Joseph JD, Darimont B, Brigham D, Heyman R, Rix PJ, Hager JH, Smith ND.
ACS Med Chem Lett (2019) 10 : 50 -55
PubMed 30655946 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 9.49 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4563316 1 10.00
CHEMBL4447340 1 10.00
CHEMBL4438992 1 9.70
CHEMBL4524752 1 9.70
CHEMBL4435067 1 9.70
CHEMBL4438260 1 9.70
CHEMBL4464718 1 9.52
CHEMBL4576272 1 9.52
CHEMBL4454014 1 9.40
CHEMBL4438826 1 9.40
CHEMBL4574167 1 9.40
CHEMBL4461269 1 8.85
CHEMBL4450664 1 8.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4563316 IC50 = 0.1 nM 10.00
CHEMBL4447340 IC50 = 0.1 nM 10.00
CHEMBL4438992 IC50 = 0.2 nM 9.70
CHEMBL4524752 IC50 = 0.2 nM 9.70
CHEMBL4435067 IC50 = 0.2 nM 9.70
CHEMBL4438260 IC50 = 0.2 nM 9.70
CHEMBL4464718 IC50 = 0.3 nM 9.52
CHEMBL4576272 IC50 = 0.3 nM 9.52
CHEMBL4454014 IC50 = 0.4 nM 9.40
CHEMBL4438826 IC50 = 0.4 nM 9.40
CHEMBL4574167 IC50 = 0.4 nM 9.40
CHEMBL4461269 IC50 = 1.4 nM 8.85
CHEMBL4450664 IC50 = 3.6 nM 8.44