Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4332083

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

Binding
Induction of ERalpha degradation in human MCF7 cells in phenol red free RPMI medium containing 5% charcoal-stripped FBS incubated for 4 hrs by IRDye 800CW/DRAQ5 dye based in-cell Western assay
ChEMBL ↗
63
Total Activities
63
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MCF7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Estrogen receptor (CHEMBL206) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective estrogen receptor degraders with novel structural motifs induce regression in a tamoxifen-resistant breast cancer xenograft.
Govek SP, Bonnefous C, Julien JD, Nagasawa JY, Kahraman M, Lai AG, Douglas KL, Aparicio AM, Darimont BD, Grillot KL, Joseph JD, Kaufman JA, Lee KJ, Lu N, Moon MJ, Prudente RY, Sensintaffar J, Rix PJ, Hager JH, Smith ND.
Bioorg Med Chem Lett (2019) 29 : 367 -372
PubMed 30587451 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 63 8.10 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4474820 — — 1 9.52
CHEMBL1358 FULVESTRANT 4.0 1 9.40
CHEMBL4527199 — — 1 9.40
CHEMBL4464136 — — 1 9.40
CHEMBL4448909 — — 1 9.22
CHEMBL4472714 — — 1 9.15
CHEMBL3581693 BRILANESTRANT 2.0 1 9.15
CHEMBL4559957 — — 1 9.15
CHEMBL4563585 — — 1 9.10
CHEMBL4442838 — — 1 9.10
CHEMBL4562048 — — 1 9.10
CHEMBL4577104 — — 1 9.00
CHEMBL4531707 — — 1 8.96
CHEMBL4455921 — — 1 8.96
CHEMBL4455108 — — 1 8.96
CHEMBL4437503 — — 1 8.85
CHEMBL4444687 — — 1 8.82
CHEMBL4519174 — — 1 8.82
CHEMBL4560511 — — 1 8.82
CHEMBL4552977 — — 1 8.80
CHEMBL4513432 — — 1 8.77
CHEMBL195515 — — 1 8.77
CHEMBL4456861 — — 1 8.74
CHEMBL4582772 — — 1 8.72
CHEMBL4440665 — — 1 8.72
CHEMBL4451352 — — 1 8.68
CHEMBL3581641 — — 1 8.59
CHEMBL4572383 — — 1 8.55
CHEMBL4554587 — — 1 8.39
CHEMBL4561552 — — 1 8.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4474820 — EC50 = 0.3 nM 9.52
CHEMBL1358 FULVESTRANT EC50 = 0.4 nM 9.40
CHEMBL4464136 — EC50 = 0.4 nM 9.40
CHEMBL4527199 — EC50 = 0.4 nM 9.40
CHEMBL4448909 — EC50 = 0.6 nM 9.22
CHEMBL4472714 — EC50 = 0.7 nM 9.15
CHEMBL3581693 BRILANESTRANT EC50 = 0.7 nM 9.15
CHEMBL4559957 — EC50 = 0.7 nM 9.15
CHEMBL4563585 — EC50 = 0.8 nM 9.10
CHEMBL4442838 — EC50 = 0.8 nM 9.10
CHEMBL4562048 — EC50 = 0.8 nM 9.10
CHEMBL4577104 — EC50 = 1.0 nM 9.00
CHEMBL4455108 — EC50 = 1.1 nM 8.96
CHEMBL4455921 — EC50 = 1.1 nM 8.96
CHEMBL4531707 — EC50 = 1.1 nM 8.96
CHEMBL4437503 — EC50 = 1.4 nM 8.85
CHEMBL4444687 — EC50 = 1.5 nM 8.82
CHEMBL4519174 — EC50 = 1.5 nM 8.82
CHEMBL4560511 — EC50 = 1.5 nM 8.82
CHEMBL4552977 — EC50 = 1.6 nM 8.80
CHEMBL4513432 — EC50 = 1.7 nM 8.77
CHEMBL195515 — EC50 = 1.7 nM 8.77
CHEMBL4456861 — EC50 = 1.8 nM 8.74
CHEMBL4582772 — EC50 = 1.9 nM 8.72
CHEMBL4440665 — EC50 = 1.9 nM 8.72
CHEMBL4451352 — EC50 = 2.1 nM 8.68
CHEMBL3581641 — EC50 = 2.6 nM 8.59
CHEMBL4572383 — EC50 = 2.8 nM 8.55
CHEMBL4554587 — EC50 = 4.1 nM 8.39
CHEMBL4561552 — EC50 = 4.2 nM 8.38
CHEMBL4531957 — EC50 = 4.3 nM 8.37
CHEMBL4467689 — EC50 = 4.8 nM 8.32
CHEMBL4457003 — EC50 = 5.0 nM 8.30
CHEMBL4460153 — EC50 = 5.9 nM 8.23
CHEMBL4436368 — EC50 = 7.4 nM 8.13
CHEMBL4521219 — EC50 = 12.0 nM 7.92
CHEMBL4462781 — EC50 = 15.0 nM 7.82
CHEMBL4568824 — EC50 = 17.0 nM 7.77
CHEMBL4474494 — EC50 = 19.0 nM 7.72
CHEMBL4435583 — EC50 = 22.0 nM 7.66
CHEMBL4475951 — EC50 = 27.0 nM 7.57
CHEMBL4542877 — EC50 = 28.0 nM 7.55
CHEMBL4556145 — EC50 = 37.0 nM 7.43
CHEMBL4563996 — EC50 = 50.0 nM 7.30
CHEMBL4473222 — EC50 = 57.0 nM 7.24
CHEMBL4520785 — EC50 = 75.0 nM 7.12
CHEMBL4437988 — EC50 = 83.0 nM 7.08
CHEMBL4553383 — EC50 = 90.0 nM 7.05
CHEMBL4538724 — EC50 = 99.0 nM 7.00
CHEMBL4475225 — EC50 = 140.0 nM 6.85