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Assay Detail

CHEMBL5731406

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

Binding
Biological Assay: The compounds of the present invention have an inhibition effect on the binding of E (estrogen) to ER (estrogen receptor), thereby blocking the binding of a complex of E and ER to ERE (estrogen responsive element), and subsequently blocking the expression of downstream luciferase protein.
ChEMBL ↗
261
Total Activities
87
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

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

Target

G-protein coupled estrogen receptor 1 (CHEMBL5872) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Piperidine derivative and preparation method and pharmaceutical use thereof
(2018)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 87 8.53 10.40
kon 87 - -
k_off 87 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4448852 — — 3 10.40
CHEMBL5964875 — — 3 9.68
CHEMBL5979005 — — 3 9.68
CHEMBL5835059 — — 3 9.62
CHEMBL5841693 — — 3 9.54
CHEMBL5904942 — — 3 9.51
CHEMBL5827662 — — 3 9.49
CHEMBL5740053 — — 3 9.49
CHEMBL5920005 — — 3 9.48
CHEMBL6004991 — — 3 9.44
CHEMBL5967118 — — 3 9.37
CHEMBL5761732 — — 3 9.35
CHEMBL5951465 — — 3 9.29
CHEMBL5833057 — — 3 9.19
CHEMBL6032703 — — 3 9.19
CHEMBL5924129 — — 3 9.14
CHEMBL5927812 — — 3 9.14
CHEMBL5938490 — — 3 9.13
CHEMBL5915577 — — 3 9.11
CHEMBL5766406 — — 3 9.11
CHEMBL6005597 — — 3 9.09
CHEMBL5983785 — — 3 9.08
CHEMBL5825226 — — 3 9.07
CHEMBL6065669 — — 3 9.07
CHEMBL6061420 — — 3 9.06
CHEMBL5974785 — — 3 8.97
CHEMBL5819525 — — 3 8.93
CHEMBL5886900 — — 3 8.91
CHEMBL5945249 — — 3 8.90
CHEMBL5955907 — — 3 8.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4448852 — IC50 = 0.04 nM 10.40
CHEMBL5964875 — IC50 = 0.21 nM 9.68
CHEMBL5979005 — IC50 = 0.21 nM 9.68
CHEMBL5835059 — IC50 = 0.24 nM 9.62
CHEMBL5841693 — IC50 = 0.29 nM 9.54
CHEMBL5904942 — IC50 = 0.31 nM 9.51
CHEMBL5740053 — IC50 = 0.32 nM 9.49
CHEMBL5827662 — IC50 = 0.32 nM 9.49
CHEMBL5920005 — IC50 = 0.33 nM 9.48
CHEMBL6004991 — IC50 = 0.36 nM 9.44
CHEMBL5967118 — IC50 = 0.43 nM 9.37
CHEMBL5761732 — IC50 = 0.45 nM 9.35
CHEMBL5951465 — IC50 = 0.51 nM 9.29
CHEMBL5833057 — IC50 = 0.64 nM 9.19
CHEMBL6032703 — IC50 = 0.64 nM 9.19
CHEMBL5927812 — IC50 = 0.72 nM 9.14
CHEMBL5924129 — IC50 = 0.73 nM 9.14
CHEMBL5938490 — IC50 = 0.74 nM 9.13
CHEMBL5915577 — IC50 = 0.77 nM 9.11
CHEMBL5766406 — IC50 = 0.77 nM 9.11
CHEMBL6005597 — IC50 = 0.82 nM 9.09
CHEMBL5983785 — IC50 = 0.84 nM 9.08
CHEMBL6065669 — IC50 = 0.85 nM 9.07
CHEMBL5825226 — IC50 = 0.86 nM 9.07
CHEMBL6061420 — IC50 = 0.87 nM 9.06
CHEMBL5974785 — IC50 = 1.07 nM 8.97
CHEMBL5819525 — IC50 = 1.17 nM 8.93
CHEMBL5886900 — IC50 = 1.22 nM 8.91
CHEMBL5955907 — IC50 = 1.25 nM 8.90
CHEMBL5945249 — IC50 = 1.26 nM 8.90
CHEMBL5839289 — IC50 = 1.32 nM 8.88
CHEMBL5843070 — IC50 = 1.36 nM 8.87
CHEMBL6034275 — IC50 = 1.39 nM 8.86
CHEMBL5791507 — IC50 = 1.45 nM 8.84
CHEMBL5957467 — IC50 = 1.52 nM 8.82
CHEMBL6034914 — IC50 = 1.5 nM 8.82
CHEMBL5926577 — IC50 = 1.59 nM 8.80
CHEMBL5792993 — IC50 = 1.7 nM 8.77
CHEMBL5754044 — IC50 = 1.82 nM 8.74
CHEMBL5894718 — IC50 = 1.85 nM 8.73
CHEMBL5999411 — IC50 = 1.88 nM 8.73
CHEMBL6045088 — IC50 = 1.94 nM 8.71
CHEMBL5897592 — IC50 = 2.11 nM 8.68
CHEMBL6008545 — IC50 = 2.28 nM 8.64
CHEMBL5778911 — IC50 = 2.47 nM 8.61
CHEMBL5900040 — IC50 = 2.97 nM 8.53
CHEMBL5843499 — IC50 = 3.14 nM 8.50
CHEMBL6010442 — IC50 = 3.25 nM 8.49
CHEMBL5978277 — IC50 = 3.2 nM 8.49
CHEMBL6005752 — IC50 = 3.4 nM 8.47