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Assay Detail

CHEMBL4424726

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

Functional
Antiproliferative activity against human MCF7 cells after 3 days by CellTiter-Glo luminescent cell viability assay
13
Total Activities
10
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

Unexpected equivalent potency of a constrained chromene enantiomeric pair rationalized by co-crystal structures in complex with estrogen receptor alpha.
Zhang B, Kiefer JR, Blake RA, Chang JH, Hartman S, Ingalla ER, Kleinheinz T, Mody V, Nannini M, Ortwine DF, Ran Y, Sambrone A, Sampath D, Vinogradova M, Zhong Y, Nwachukwu JC, Nettles KW, Lai T, Liao J, Zheng X, Chen H, Wang X, Liang J.
Bioorg Med Chem Lett (2019) 29 : 905 -911
PubMed 30732944 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 9.02 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4449709 1 9.70
CHEMBL4447340 1 9.70
CHEMBL4439408 2 9.52
CHEMBL4539802 1 9.52
CHEMBL4437985 1 9.40
CHEMBL4464224 1 9.15
CHEMBL4443826 2 9.10
CHEMBL4464058 1 9.05
CHEMBL1087419 1 8.92
CHEMBL4464146 2 8.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4449709 IC50 = 0.2 nM 9.70
CHEMBL4447340 IC50 = 0.2 nM 9.70
CHEMBL4439408 IC50 = 0.3 nM 9.52
CHEMBL4539802 IC50 = 0.3 nM 9.52
CHEMBL4437985 IC50 = 0.4 nM 9.40
CHEMBL4439408 IC50 = 0.6 nM 9.22
CHEMBL4464224 IC50 = 0.7 nM 9.15
CHEMBL4443826 IC50 = 0.8 nM 9.10
CHEMBL4464058 IC50 = 0.9 nM 9.05
CHEMBL1087419 IC50 = 1.2 nM 8.92
CHEMBL4464146 IC50 = 5.0 nM 8.30
CHEMBL4443826 IC50 = 10.0 nM 8.00
CHEMBL4464146 IC50 = 20.0 nM 7.70