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Assay Detail

CHEMBL3591298

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

Binding
Binding affinity to human ER-beta ligand binding domain after 2 hrs by competitive fluorometric binding assay
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Estrogen receptor beta (CHEMBL242)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel Bioactive Hybrid Compound Dual Targeting Estrogen Receptor and Histone Deacetylase for the Treatment of Breast Cancer.
Tang C, Li C, Zhang S, Hu Z, Wu J, Dong C, Huang J, Zhou HB.
J Med Chem (2015) 58 : 4550 -4572
PubMed 25993269 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 33 6.54 7.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3589358 1 7.41
CHEMBL3589346 1 7.31
CHEMBL3589360 1 7.30
CHEMBL3589368 1 7.25
CHEMBL3589363 1 7.22
CHEMBL3589353 1 7.17
CHEMBL3589355 1 7.09
CHEMBL3589352 1 7.06
CHEMBL3589356 1 7.04
CHEMBL3589359 1 7.02
CHEMBL3589701 1 6.99
CHEMBL3589367 1 6.99
CHEMBL3589357 1 6.99
CHEMBL3589361 1 6.92
CHEMBL3589351 1 6.90
CHEMBL3589362 1 6.70
CHEMBL3589364 1 6.59
CHEMBL3589365 1 6.32
CHEMBL3589354 1 6.21
CHEMBL3589350 1 6.20
CHEMBL3588865 1 6.18
CHEMBL3589347 1 6.12
CHEMBL3589349 1 6.11
CHEMBL3589700 1 6.09
CHEMBL3589366 1 6.01
CHEMBL3589348 1 5.85
CHEMBL3589696 1 5.67
CHEMBL3589699 1 5.62
CHEMBL3589697 1 5.55
CHEMBL3589369 1 5.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3589358 Ki = 39.04 nM 7.41
CHEMBL3589346 Ki = 49.06 nM 7.31
CHEMBL3589360 Ki = 49.78 nM 7.30
CHEMBL3589368 Ki = 55.65 nM 7.25
CHEMBL3589363 Ki = 60.5 nM 7.22
CHEMBL3589353 Ki = 67.73 nM 7.17
CHEMBL3589355 Ki = 81.53 nM 7.09
CHEMBL3589352 Ki = 87.32 nM 7.06
CHEMBL3589356 Ki = 91.89 nM 7.04
CHEMBL3589359 Ki = 95.24 nM 7.02
CHEMBL3589701 Ki = 102.41 nM 6.99
CHEMBL3589367 Ki = 101.49 nM 6.99
CHEMBL3589357 Ki = 101.49 nM 6.99
CHEMBL3589361 Ki = 121.43 nM 6.92
CHEMBL3589351 Ki = 126.87 nM 6.90
CHEMBL3589362 Ki = 200.01 nM 6.70
CHEMBL3589364 Ki = 255.64 nM 6.59
CHEMBL3589365 Ki = 478.87 nM 6.32
CHEMBL3589354 Ki = 618.18 nM 6.21
CHEMBL3589350 Ki = 629.63 nM 6.20
CHEMBL3588865 Ki = 653.85 nM 6.18
CHEMBL3589347 Ki = 755.56 nM 6.12
CHEMBL3589349 Ki = 772.73 nM 6.11
CHEMBL3589700 Ki = 809.52 nM 6.09
CHEMBL3589366 Ki = 971.43 nM 6.01
CHEMBL3589348 Ki = 1416.67 nM 5.85
CHEMBL3589696 Ki = 2125.0 nM 5.67
CHEMBL3589699 Ki = 2428.57 nM 5.62
CHEMBL3589697 Ki = 2833.33 nM 5.55
CHEMBL3589369 Ki = 3090.9 nM 5.51
CHEMBL3589698 Ki = 3400.0 nM 5.47
CHEMBL3589694 Ki > 5000.0 nM -
CHEMBL3589695 Ki > 5000.0 nM -