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Assay Detail

CHEMBL3582780

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

Functional
Cytotoxicity against human MCF7 cells assessed as cell viability after 5 days by CellTiter-Glo assay
38
Total Activities
38
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

Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts.
Lai A, Kahraman M, Govek S, Nagasawa J, Bonnefous C, Julien J, Douglas K, Sensintaffar J, Lu N, Lee KJ, Aparicio A, Kaufman J, Qian J, Shao G, Prudente R, Moon MJ, Joseph JD, Darimont B, Brigham D, Grillot K, Heyman R, Rix PJ, Hager JH, Smith ND.
J Med Chem (2015) 58 : 4888 -4904
PubMed 25879485 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 7.38 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3581682 1 8.70
CHEMBL3581681 1 8.70
CHEMBL3581693 BRILANESTRANT 2.0 1 8.70
CHEMBL3581692 1 8.40
CHEMBL3581688 1 8.40
CHEMBL3581680 1 8.40
CHEMBL195515 1 8.30
CHEMBL3581691 1 8.30
CHEMBL3581641 1 8.22
CHEMBL3581638 1 8.05
CHEMBL3581683 1 7.92
CHEMBL3581685 1 7.92
CHEMBL3581645 1 7.92
CHEMBL3581644 1 7.85
CHEMBL3581684 1 7.82
CHEMBL3581678 1 7.80
CHEMBL3580674 1 7.68
CHEMBL3581690 1 7.60
CHEMBL3581646 1 7.51
CHEMBL3581643 1 7.44
CHEMBL3581687 1 7.33
CHEMBL3581640 1 7.28
CHEMBL3581637 1 7.25
CHEMBL3581689 1 7.16
CHEMBL3581686 1 7.00
CHEMBL3581679 1 6.82
CHEMBL3581636 1 6.80
CHEMBL3581677 1 6.70
CHEMBL3581675 1 6.68
CHEMBL226267 ARZOXIFENE 3.0 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3581682 IC50 = 2.0 nM 8.70
CHEMBL3581693 BRILANESTRANT IC50 = 2.0 nM 8.70
CHEMBL3581681 IC50 = 2.0 nM 8.70
CHEMBL3581692 IC50 = 4.0 nM 8.40
CHEMBL3581688 IC50 = 4.0 nM 8.40
CHEMBL3581680 IC50 = 4.0 nM 8.40
CHEMBL195515 IC50 = 5.0 nM 8.30
CHEMBL3581691 IC50 = 5.0 nM 8.30
CHEMBL3581641 IC50 = 6.0 nM 8.22
CHEMBL3581638 IC50 = 9.0 nM 8.05
CHEMBL3581685 IC50 = 12.0 nM 7.92
CHEMBL3581645 IC50 = 12.0 nM 7.92
CHEMBL3581683 IC50 = 12.0 nM 7.92
CHEMBL3581644 IC50 = 14.0 nM 7.85
CHEMBL3581684 IC50 = 15.0 nM 7.82
CHEMBL3581678 IC50 = 16.0 nM 7.80
CHEMBL3580674 IC50 = 21.0 nM 7.68
CHEMBL3581690 IC50 = 25.0 nM 7.60
CHEMBL3581646 IC50 = 31.0 nM 7.51
CHEMBL3581643 IC50 = 36.0 nM 7.44
CHEMBL3581687 IC50 = 47.0 nM 7.33
CHEMBL3581640 IC50 = 53.0 nM 7.28
CHEMBL3581637 IC50 = 56.0 nM 7.25
CHEMBL3581689 IC50 = 70.0 nM 7.16
CHEMBL3581686 IC50 = 100.0 nM 7.00
CHEMBL3581679 IC50 = 150.0 nM 6.82
CHEMBL3581636 IC50 = 158.0 nM 6.80
CHEMBL3581677 IC50 = 200.0 nM 6.70
CHEMBL3581675 IC50 = 210.0 nM 6.68
CHEMBL226267 ARZOXIFENE IC50 = 400.0 nM 6.40
CHEMBL44426 PIPENDOXIFENE IC50 = 400.0 nM 6.40
CHEMBL3581642 IC50 = 570.0 nM 6.24
CHEMBL1358 FULVESTRANT IC50 = 600.0 nM 6.22
CHEMBL33899 IC50 = 985.0 nM 6.01
CHEMBL3581639 IC50 = 1180.0 nM 5.93
CHEMBL3581635 IC50 = 2310.0 nM 5.64
CHEMBL3581676 IC50 = 2900.0 nM 5.54
CHEMBL3581634 IC50 - -