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Assay Detail

CHEMBL859110

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

Functional
Effect on transactivation of ALP gene expression in HEK293 cells transfected with hERalpha
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Expert

Target

Estrogen receptor (CHEMBL206)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Androstenediol analogs as ER-beta-selective SERMs.
Blizzard TA, Gude C, Morgan JD, Chan W, Birzin ET, Mojena M, Tudela C, Chen F, Knecht K, Su Q, Kraker B, Mosley RT, Holmes MA, Sharma N, Fitzgerald PM, Rohrer SP, Hammond ML.
Bioorg Med Chem Lett (2006) 16 : 834 -838
PubMed 16309907 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 24 6.58 9.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL135 ESTRADIOL 4.0 1 9.12
CHEMBL381566 1 8.00
CHEMBL440283 ANDROSTENEDIOL -1.0 1 7.58
CHEMBL202415 1 7.33
CHEMBL437065 1 6.80
CHEMBL202400 1 6.49
CHEMBL383253 1 6.46
CHEMBL204642 1 6.31
CHEMBL204389 1 6.23
CHEMBL370236 1 6.22
CHEMBL202007 1 6.21
CHEMBL369991 1 6.14
CHEMBL380978 1 6.07
CHEMBL373019 1 6.01
CHEMBL203561 1 6.01
CHEMBL369979 1 6.00
CHEMBL201809 1 6.00
CHEMBL380876 1 5.49
CHEMBL201364 1 -
CHEMBL203748 1 -
CHEMBL204317 1 -
CHEMBL379441 1 -
CHEMBL382632 1 -
CHEMBL201569 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL135 ESTRADIOL EC50 = 0.75 nM 9.12
CHEMBL381566 EC50 = 10.0 nM 8.00
CHEMBL440283 ANDROSTENEDIOL EC50 = 26.0 nM 7.58
CHEMBL202415 EC50 = 47.0 nM 7.33
CHEMBL437065 EC50 = 160.0 nM 6.80
CHEMBL202400 EC50 = 324.0 nM 6.49
CHEMBL383253 EC50 = 344.0 nM 6.46
CHEMBL204642 EC50 = 494.0 nM 6.31
CHEMBL204389 EC50 = 583.0 nM 6.23
CHEMBL370236 EC50 = 603.0 nM 6.22
CHEMBL202007 EC50 = 622.0 nM 6.21
CHEMBL369991 EC50 = 719.0 nM 6.14
CHEMBL380978 EC50 = 844.0 nM 6.07
CHEMBL373019 EC50 = 982.0 nM 6.01
CHEMBL203561 EC50 = 984.0 nM 6.01
CHEMBL369979 EC50 = 1000.0 nM 6.00
CHEMBL201809 EC50 = 1000.0 nM 6.00
CHEMBL380876 EC50 = 3237.0 nM 5.49
CHEMBL201364 EC50 > 1000.0 nM -
CHEMBL203748 EC50 > 1000.0 nM -
CHEMBL204317 EC50 > 1000.0 nM -
CHEMBL379441 EC50 > 1000.0 nM -
CHEMBL382632 EC50 > 1000.0 nM -
CHEMBL201569 EC50 > 1000.0 nM -