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Assay Detail

CHEMBL867528

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Functional
Inhibition of estrogen receptor in MCF7 cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MCF7
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Estrogen receptor (CHEMBL2093866)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Novel chromene-derived selective estrogen receptor modulators useful for alleviating hot flushes and vaginal dryness.
Jain N, Kanojia RM, Xu J, Jian-Zhong G, Pacia E, Lai MT, Du F, Musto A, Allan G, Hahn D, Lundeen S, Sui Z.
J Med Chem (2006) 49 : 3056 -3059
PubMed 16722623 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.42 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL379415 1 6.96
CHEMBL426322 1 6.82
CHEMBL210648 1 6.66
CHEMBL81 RALOXIFENE 4.0 1 6.65
CHEMBL207324 1 6.38
CHEMBL207362 1 6.29
CHEMBL208085 1 6.22
CHEMBL206680 1 6.18
CHEMBL381489 1 6.17
CHEMBL210699 1 5.85
CHEMBL691 ETHINYL ESTRADIOL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL379415 IC50 = 110.0 nM 6.96
CHEMBL426322 IC50 = 150.0 nM 6.82
CHEMBL210648 IC50 = 220.0 nM 6.66
CHEMBL81 RALOXIFENE IC50 = 222.0 nM 6.65
CHEMBL207324 IC50 = 416.0 nM 6.38
CHEMBL207362 IC50 = 510.0 nM 6.29
CHEMBL208085 IC50 = 599.0 nM 6.22
CHEMBL206680 IC50 = 660.0 nM 6.18
CHEMBL381489 IC50 = 670.0 nM 6.17
CHEMBL210699 IC50 = 1400.0 nM 5.85
CHEMBL691 ETHINYL ESTRADIOL IC50 - -