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Assay Detail

CHEMBL1114101

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

Functional
Antagonist activity at estrogen receptor in human Ishikawa cells assessed as 17-beta-estradiol-induced alkaline phosphatase activity after 3 days by chemiluminescence assay
61
Total Activities
61
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Ishikawa
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Estrogen receptor (CHEMBL206)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification and structure-activity relationships of chromene-derived selective estrogen receptor modulators for treatment of postmenopausal symptoms.
Jain N, Xu J, Kanojia RM, Du F, Jian-Zhong G, Pacia E, Lai MT, Musto A, Allan G, Reuman M, Li X, Hahn D, Cousineau M, Peng S, Ritchie D, Russell R, Lundeen S, Sui Z.
J Med Chem (2009) 52 : 7544 -7569
PubMed 19366247 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 61 6.97 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1088485 1 9.70
CHEMBL1087419 1 8.10
CHEMBL1086775 1 8.00
CHEMBL81 RALOXIFENE 4.0 1 7.62
CHEMBL1082864 1 7.59
CHEMBL1086652 1 7.59
CHEMBL1088631 1 7.50
CHEMBL1085899 1 7.46
CHEMBL1087545 1 7.39
CHEMBL1087811 1 7.37
CHEMBL1083186 1 7.21
CHEMBL1087297 1 7.17
CHEMBL1087298 1 7.12
CHEMBL1088343 1 7.12
CHEMBL1082224 1 7.09
CHEMBL1083178 1 7.06
CHEMBL1084922 1 7.05
CHEMBL1084128 1 6.95
CHEMBL1088629 1 6.95
CHEMBL1086644 1 6.92
CHEMBL1084120 1 6.91
CHEMBL1086774 1 6.89
CHEMBL1084129 1 6.88
CHEMBL1086389 1 6.87
CHEMBL1087418 1 6.84
CHEMBL1087426 1 6.82
CHEMBL1088344 1 6.82
CHEMBL1087919 1 6.80
CHEMBL1082528 1 6.79
CHEMBL1086776 1 6.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1088485 IC50 = 0.2 nM 9.70
CHEMBL1087419 IC50 = 8.0 nM 8.10
CHEMBL1086775 IC50 = 10.0 nM 8.00
CHEMBL81 RALOXIFENE IC50 = 24.0 nM 7.62
CHEMBL1082864 IC50 = 25.9 nM 7.59
CHEMBL1086652 IC50 = 25.9 nM 7.59
CHEMBL1088631 IC50 = 32.0 nM 7.50
CHEMBL1085899 IC50 = 35.0 nM 7.46
CHEMBL1087545 IC50 = 41.0 nM 7.39
CHEMBL1087811 IC50 = 43.0 nM 7.37
CHEMBL1083186 IC50 = 61.0 nM 7.21
CHEMBL1087297 IC50 = 68.0 nM 7.17
CHEMBL1087298 IC50 = 76.0 nM 7.12
CHEMBL1088343 IC50 = 76.0 nM 7.12
CHEMBL1082224 IC50 = 81.0 nM 7.09
CHEMBL1083178 IC50 = 87.0 nM 7.06
CHEMBL1084922 IC50 = 90.0 nM 7.05
CHEMBL1084128 IC50 = 113.0 nM 6.95
CHEMBL1088629 IC50 = 113.0 nM 6.95
CHEMBL1086644 IC50 = 121.0 nM 6.92
CHEMBL1084120 IC50 = 122.0 nM 6.91
CHEMBL1086774 IC50 = 128.0 nM 6.89
CHEMBL1084129 IC50 = 133.0 nM 6.88
CHEMBL1086389 IC50 = 134.0 nM 6.87
CHEMBL1087418 IC50 = 144.0 nM 6.84
CHEMBL1087426 IC50 = 150.0 nM 6.82
CHEMBL1088344 IC50 = 150.0 nM 6.82
CHEMBL1087919 IC50 = 158.0 nM 6.80
CHEMBL1082528 IC50 = 161.0 nM 6.79
CHEMBL1086776 IC50 = 165.0 nM 6.78
CHEMBL1084127 IC50 = 194.0 nM 6.71
CHEMBL1087289 IC50 = 259.0 nM 6.59
CHEMBL1088483 IC50 = 259.0 nM 6.59
CHEMBL1085669 IC50 = 287.0 nM 6.54
CHEMBL1082539 IC50 = 293.0 nM 6.53
CHEMBL1085668 IC50 = 405.0 nM 6.39
CHEMBL1087546 IC50 = 420.0 nM 6.38
CHEMBL1087547 IC50 = 590.0 nM 6.23
CHEMBL1085429 IC50 = 1736.0 nM 5.76
CHEMBL1087288 IC50 = 2670.0 nM 5.57
CHEMBL1082529 IC50 = 8990.0 nM 5.05
CHEMBL83 TAMOXIFEN IC50 - -
CHEMBL1087290 IC50 > 10000.0 nM -
CHEMBL1086388 IC50 > 10000.0 nM -
CHEMBL1083805 IC50 > 10000.0 nM -
CHEMBL1083497 IC50 > 10000.0 nM -
CHEMBL1087041 IC50 > 10000.0 nM -
CHEMBL1087040 IC50 > 10000.0 nM -
CHEMBL1083188 IC50 > 10000.0 nM -
CHEMBL1083187 IC50 > 10000.0 nM -