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Assay Detail

CHEMBL4332085

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 measured after 5 days by Cell-titer-Glo assay
63
Total Activities
63
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

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
IC50 63 7.88 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1358 FULVESTRANT 4.0 1 9.22
CHEMBL4474820 1 9.15
CHEMBL4527199 1 9.05
CHEMBL4464136 1 9.05
CHEMBL4563585 1 8.85
CHEMBL4442838 1 8.74
CHEMBL4448909 1 8.68
CHEMBL4559957 1 8.66
CHEMBL3581693 BRILANESTRANT 2.0 1 8.60
CHEMBL4577104 1 8.59
CHEMBL4531707 1 8.54
CHEMBL4456861 1 8.54
CHEMBL4455921 1 8.54
CHEMBL4472714 1 8.52
CHEMBL4562048 1 8.38
CHEMBL4582772 1 8.37
CHEMBL4560511 1 8.36
CHEMBL4455108 1 8.36
CHEMBL195515 1 8.34
CHEMBL4552977 1 8.30
CHEMBL4519174 1 8.29
CHEMBL4444687 1 8.29
CHEMBL4531957 1 8.23
CHEMBL4440665 1 8.16
CHEMBL3581641 1 8.14
CHEMBL4437503 1 8.14
CHEMBL4561552 1 8.12
CHEMBL4513432 1 8.04
CHEMBL4451352 1 7.96
CHEMBL4457003 1 7.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1358 FULVESTRANT IC50 = 0.6 nM 9.22
CHEMBL4474820 IC50 = 0.7 nM 9.15
CHEMBL4464136 IC50 = 0.9 nM 9.05
CHEMBL4527199 IC50 = 0.9 nM 9.05
CHEMBL4563585 IC50 = 1.4 nM 8.85
CHEMBL4442838 IC50 = 1.8 nM 8.74
CHEMBL4448909 IC50 = 2.1 nM 8.68
CHEMBL4559957 IC50 = 2.2 nM 8.66
CHEMBL3581693 BRILANESTRANT IC50 = 2.5 nM 8.60
CHEMBL4577104 IC50 = 2.6 nM 8.59
CHEMBL4531707 IC50 = 2.9 nM 8.54
CHEMBL4456861 IC50 = 2.9 nM 8.54
CHEMBL4455921 IC50 = 2.9 nM 8.54
CHEMBL4472714 IC50 = 3.0 nM 8.52
CHEMBL4562048 IC50 = 4.2 nM 8.38
CHEMBL4582772 IC50 = 4.3 nM 8.37
CHEMBL4560511 IC50 = 4.4 nM 8.36
CHEMBL4455108 IC50 = 4.4 nM 8.36
CHEMBL195515 IC50 = 4.6 nM 8.34
CHEMBL4552977 IC50 = 5.0 nM 8.30
CHEMBL4519174 IC50 = 5.1 nM 8.29
CHEMBL4444687 IC50 = 5.1 nM 8.29
CHEMBL4531957 IC50 = 5.9 nM 8.23
CHEMBL4440665 IC50 = 6.9 nM 8.16
CHEMBL4437503 IC50 = 7.3 nM 8.14
CHEMBL3581641 IC50 = 7.2 nM 8.14
CHEMBL4561552 IC50 = 7.5 nM 8.12
CHEMBL4513432 IC50 = 9.2 nM 8.04
CHEMBL4451352 IC50 = 11.0 nM 7.96
CHEMBL4457003 IC50 = 12.0 nM 7.92
CHEMBL4474494 IC50 = 15.0 nM 7.82
CHEMBL4467689 IC50 = 16.0 nM 7.80
CHEMBL4460153 IC50 = 16.0 nM 7.80
CHEMBL4572383 IC50 = 16.0 nM 7.80
CHEMBL4554587 IC50 = 20.0 nM 7.70
CHEMBL4436368 IC50 = 31.0 nM 7.51
CHEMBL4521219 IC50 = 40.0 nM 7.40
CHEMBL4568824 IC50 = 51.0 nM 7.29
CHEMBL4462781 IC50 = 80.0 nM 7.10
CHEMBL4475951 IC50 = 81.0 nM 7.09
CHEMBL4435583 IC50 = 90.0 nM 7.05
CHEMBL4563996 IC50 = 94.0 nM 7.03
CHEMBL4542877 IC50 = 120.0 nM 6.92
CHEMBL4556145 IC50 = 120.0 nM 6.92
CHEMBL4520785 IC50 = 170.0 nM 6.77
CHEMBL4473222 IC50 = 180.0 nM 6.75
CHEMBL4553383 IC50 = 220.0 nM 6.66
CHEMBL4437988 IC50 = 290.0 nM 6.54
CHEMBL4475225 IC50 = 300.0 nM 6.52
CHEMBL4454739 IC50 = 380.0 nM 6.42