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Assay Detail

CHEMBL5163406

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

Functional
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 6 days by cell titre glo luminescence assay
60
Total Activities
60
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 Thieno[2,3-<i>e</i>]indazole Derivatives as Novel Oral Selective Estrogen Receptor Degraders with Highly Improved Antitumor Effect and Favorable Druggability.
Lu Z, Cao Y, Zhang D, Meng X, Guo B, Kong D, Yang Y.
J Med Chem (2022) 65 : 5724 -5750
PubMed 35357160 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 60 8.34 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5171948 1 9.30
CHEMBL5177756 1 9.22
CHEMBL5173113 1 9.22
CHEMBL5205357 1 9.22
CHEMBL5205039 1 9.15
CHEMBL5180046 1 9.10
CHEMBL5169445 1 9.10
CHEMBL5184413 1 9.10
CHEMBL5181850 1 9.05
CHEMBL5185539 1 9.00
CHEMBL5190953 1 9.00
CHEMBL5207484 1 8.96
CHEMBL5197035 1 8.96
CHEMBL5203346 1 8.92
CHEMBL5207893 1 8.92
CHEMBL5191700 1 8.85
CHEMBL5171955 1 8.85
CHEMBL5189071 1 8.82
CHEMBL5181826 1 8.80
CHEMBL5191391 1 8.77
CHEMBL5198894 1 8.77
CHEMBL5208566 1 8.77
CHEMBL5202286 1 8.72
CHEMBL5198039 1 8.66
CHEMBL5193428 1 8.62
CHEMBL5174315 1 8.59
CHEMBL5187985 1 8.57
CHEMBL5205546 1 8.55
CHEMBL5184683 1 8.48
CHEMBL5191161 1 8.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5171948 IC50 = 0.5 nM 9.30
CHEMBL5177756 IC50 = 0.6 nM 9.22
CHEMBL5205357 IC50 = 0.6 nM 9.22
CHEMBL5173113 IC50 = 0.6 nM 9.22
CHEMBL5205039 IC50 = 0.7 nM 9.15
CHEMBL5180046 IC50 = 0.8 nM 9.10
CHEMBL5169445 IC50 = 0.8 nM 9.10
CHEMBL5184413 IC50 = 0.8 nM 9.10
CHEMBL5181850 IC50 = 0.9 nM 9.05
CHEMBL5185539 IC50 = 1.0 nM 9.00
CHEMBL5190953 IC50 = 1.0 nM 9.00
CHEMBL5207484 IC50 = 1.1 nM 8.96
CHEMBL5197035 IC50 = 1.1 nM 8.96
CHEMBL5207893 IC50 = 1.2 nM 8.92
CHEMBL5203346 IC50 = 1.2 nM 8.92
CHEMBL5191700 IC50 = 1.4 nM 8.85
CHEMBL5171955 IC50 = 1.4 nM 8.85
CHEMBL5189071 IC50 = 1.5 nM 8.82
CHEMBL5181826 IC50 = 1.6 nM 8.80
CHEMBL5191391 IC50 = 1.7 nM 8.77
CHEMBL5198894 IC50 = 1.7 nM 8.77
CHEMBL5208566 IC50 = 1.7 nM 8.77
CHEMBL5202286 IC50 = 1.9 nM 8.72
CHEMBL5198039 IC50 = 2.2 nM 8.66
CHEMBL5193428 IC50 = 2.4 nM 8.62
CHEMBL5174315 IC50 = 2.6 nM 8.59
CHEMBL5187985 IC50 = 2.7 nM 8.57
CHEMBL5205546 IC50 = 2.8 nM 8.55
CHEMBL5184683 IC50 = 3.3 nM 8.48
CHEMBL5191161 IC50 = 4.2 nM 8.38
CHEMBL5173602 IC50 = 4.2 nM 8.38
CHEMBL5206306 IC50 = 4.4 nM 8.36
CHEMBL5188343 IC50 = 4.7 nM 8.33
CHEMBL5170271 IC50 = 5.1 nM 8.29
CHEMBL5208192 IC50 = 5.3 nM 8.28
CHEMBL5198988 IC50 = 5.9 nM 8.23
CHEMBL5207013 IC50 = 5.9 nM 8.23
CHEMBL5202599 IC50 = 6.2 nM 8.21
CHEMBL5172442 IC50 = 7.6 nM 8.12
CHEMBL5198626 IC50 = 7.8 nM 8.11
CHEMBL5200219 IC50 = 7.9 nM 8.10
CHEMBL5179839 IC50 = 8.3 nM 8.08
CHEMBL5192103 IC50 = 8.8 nM 8.06
CHEMBL4475463 AMCENESTRANT IC50 = 9.1 nM 8.04
CHEMBL5208191 IC50 = 14.7 nM 7.83
CHEMBL5178254 IC50 = 15.1 nM 7.82
CHEMBL5181707 IC50 = 19.4 nM 7.71
CHEMBL5187550 IC50 = 23.9 nM 7.62
CHEMBL5178968 IC50 = 26.6 nM 7.58
CHEMBL5176820 IC50 = 27.3 nM 7.56