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Assay Detail

CHEMBL867526

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Functional
Inhibition of estrogen receptor in Ishikawa cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Ishikawa
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 12 7.09 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL379415 1 7.92
CHEMBL206680 1 7.89
CHEMBL207324 1 7.77
CHEMBL81 RALOXIFENE 4.0 1 7.64
CHEMBL208085 1 7.36
CHEMBL426322 1 7.10
CHEMBL381489 1 7.00
CHEMBL207362 1 6.76
CHEMBL210648 1 6.75
CHEMBL210699 1 6.39
CHEMBL209090 1 5.42
CHEMBL691 ETHINYL ESTRADIOL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL379415 IC50 = 12.0 nM 7.92
CHEMBL206680 IC50 = 13.0 nM 7.89
CHEMBL207324 IC50 = 17.1 nM 7.77
CHEMBL81 RALOXIFENE IC50 = 23.0 nM 7.64
CHEMBL208085 IC50 = 43.3 nM 7.36
CHEMBL426322 IC50 = 80.0 nM 7.10
CHEMBL381489 IC50 = 99.0 nM 7.00
CHEMBL207362 IC50 = 175.0 nM 6.76
CHEMBL210648 IC50 = 180.0 nM 6.75
CHEMBL210699 IC50 = 410.0 nM 6.39
CHEMBL209090 IC50 = 3800.0 nM 5.42
CHEMBL691 ETHINYL ESTRADIOL IC50 - -