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Assay Detail

CHEMBL1114102

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

Functional
Antagonist activity at estrogen receptor in human MCF7 cells assessed as 17-beta-estradiol-induced cell proliferation after 24 hrs by [14C]thymidine incorporation assay
ChEMBL ↗
61
Total Activities
61
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MCF7
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 6.29 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1087289 — — 1 8.00
CHEMBL1088483 — — 1 8.00
CHEMBL1088485 — — 1 7.96
CHEMBL1087419 — — 1 7.72
CHEMBL1082864 — — 1 6.82
CHEMBL1086775 — — 1 6.82
CHEMBL1086652 — — 1 6.82
CHEMBL1088631 — — 1 6.76
CHEMBL1087545 — — 1 6.66
CHEMBL1085669 — — 1 6.66
CHEMBL81 RALOXIFENE 4.0 1 6.65
CHEMBL1086644 — — 1 6.55
CHEMBL1083186 — — 1 6.53
CHEMBL1086774 — — 1 6.40
CHEMBL1085899 — — 1 6.37
CHEMBL1085668 — — 1 6.16
CHEMBL1086776 — — 1 6.16
CHEMBL1087811 — — 1 6.09
CHEMBL1087546 — — 1 5.92
CHEMBL1084120 — — 1 5.92
CHEMBL1087298 — — 1 5.92
CHEMBL1088343 — — 1 5.92
CHEMBL1087426 — — 1 5.91
CHEMBL1088344 — — 1 5.91
CHEMBL1082224 — — 1 5.89
CHEMBL1087919 — — 1 5.87
CHEMBL1082528 — — 1 5.87
CHEMBL1086389 — — 1 5.87
CHEMBL1084127 — — 1 5.84
CHEMBL1084922 — — 1 5.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1087289 — IC50 = 10.0 nM 8.00
CHEMBL1088483 — IC50 = 10.0 nM 8.00
CHEMBL1088485 — IC50 = 11.0 nM 7.96
CHEMBL1087419 — IC50 = 19.0 nM 7.72
CHEMBL1082864 — IC50 = 150.0 nM 6.82
CHEMBL1086775 — IC50 = 150.0 nM 6.82
CHEMBL1086652 — IC50 = 150.0 nM 6.82
CHEMBL1088631 — IC50 = 174.0 nM 6.76
CHEMBL1087545 — IC50 = 217.0 nM 6.66
CHEMBL1085669 — IC50 = 220.0 nM 6.66
CHEMBL81 RALOXIFENE IC50 = 222.0 nM 6.65
CHEMBL1086644 — IC50 = 280.0 nM 6.55
CHEMBL1083186 — IC50 = 293.0 nM 6.53
CHEMBL1086774 — IC50 = 401.0 nM 6.40
CHEMBL1085899 — IC50 = 424.0 nM 6.37
CHEMBL1085668 — IC50 = 687.0 nM 6.16
CHEMBL1086776 — IC50 = 688.0 nM 6.16
CHEMBL1087811 — IC50 = 816.0 nM 6.09
CHEMBL1087546 — IC50 = 1200.0 nM 5.92
CHEMBL1084120 — IC50 = 1200.0 nM 5.92
CHEMBL1087298 — IC50 = 1210.0 nM 5.92
CHEMBL1088343 — IC50 = 1210.0 nM 5.92
CHEMBL1087426 — IC50 = 1236.0 nM 5.91
CHEMBL1088344 — IC50 = 1236.0 nM 5.91
CHEMBL1082224 — IC50 = 1300.0 nM 5.89
CHEMBL1087919 — IC50 = 1350.0 nM 5.87
CHEMBL1086389 — IC50 = 1350.0 nM 5.87
CHEMBL1082528 — IC50 = 1355.0 nM 5.87
CHEMBL1084127 — IC50 = 1456.0 nM 5.84
CHEMBL1084922 — IC50 = 1550.0 nM 5.81
CHEMBL1084128 — IC50 = 1570.0 nM 5.80
CHEMBL1088629 — IC50 = 1570.0 nM 5.80
CHEMBL1084129 — IC50 = 1660.0 nM 5.78
CHEMBL1087547 — IC50 = 1800.0 nM 5.75
CHEMBL1087418 — IC50 = 1844.0 nM 5.73
CHEMBL1087297 — IC50 = 1920.0 nM 5.72
CHEMBL1083178 — IC50 = 2460.0 nM 5.61
CHEMBL1087288 — IC50 = 10000.0 nM 5.00
CHEMBL1085161 — IC50 > 10000.0 nM -
CHEMBL1083188 — IC50 > 10000.0 nM -
CHEMBL1087040 — IC50 > 10000.0 nM -
CHEMBL1087041 — IC50 > 10000.0 nM -
CHEMBL1083497 — IC50 > 10000.0 nM -
CHEMBL1083805 — IC50 > 10000.0 nM -
CHEMBL1086388 — IC50 > 10000.0 nM -
CHEMBL1082539 — IC50 > 10000.0 nM -
CHEMBL1087290 — IC50 > 10000.0 nM -
CHEMBL1082529 — IC50 > 10000.0 nM -
CHEMBL83 TAMOXIFEN IC50 - — -
CHEMBL1083187 — IC50 > 10000.0 nM -