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Assay Detail

CHEMBL886439

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

Binding
Inhibition of human ERbeta
21
Total Activities
21
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

Steroid hormone receptor ERR2 (CHEMBL3751)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

ERbeta ligands. Part 6: 6H-Chromeno[4,3-b]quinolines as a new series of estrogen receptor beta-selective ligands.
Vu AT, Campbell AN, Harris HA, Unwalla RJ, Manas ES, Mewshaw RE.
Bioorg Med Chem Lett (2007) 17 : 4053 -4056
PubMed 17482813 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 6.40 8.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL135 ESTRADIOL 4.0 1 8.49
CHEMBL250097 1 7.25
CHEMBL402491 1 7.06
CHEMBL402492 1 7.01
CHEMBL198411 1 6.67
CHEMBL372783 1 6.67
CHEMBL44 GENISTEIN 2.0 1 6.40
CHEMBL197667 1 6.34
CHEMBL198089 1 6.30
CHEMBL250302 1 6.30
CHEMBL250300 1 6.28
CHEMBL250507 1 6.26
CHEMBL250301 1 6.21
CHEMBL198679 1 6.20
CHEMBL402493 1 6.19
CHEMBL398815 1 6.09
CHEMBL437390 1 5.99
CHEMBL398814 1 5.95
CHEMBL440757 1 5.82
CHEMBL250505 1 5.63
CHEMBL250506 1 5.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL135 ESTRADIOL IC50 = 3.2 nM 8.49
CHEMBL250097 IC50 = 56.0 nM 7.25
CHEMBL402491 IC50 = 88.0 nM 7.06
CHEMBL402492 IC50 = 98.0 nM 7.01
CHEMBL198411 IC50 = 212.0 nM 6.67
CHEMBL372783 IC50 = 213.0 nM 6.67
CHEMBL44 GENISTEIN IC50 = 395.0 nM 6.40
CHEMBL197667 IC50 = 455.0 nM 6.34
CHEMBL198089 IC50 = 504.0 nM 6.30
CHEMBL250302 IC50 = 504.0 nM 6.30
CHEMBL250300 IC50 = 526.0 nM 6.28
CHEMBL250507 IC50 = 549.0 nM 6.26
CHEMBL250301 IC50 = 624.0 nM 6.21
CHEMBL198679 IC50 = 634.0 nM 6.20
CHEMBL402493 IC50 = 641.0 nM 6.19
CHEMBL398815 IC50 = 820.0 nM 6.09
CHEMBL437390 IC50 = 1017.0 nM 5.99
CHEMBL398814 IC50 = 1130.0 nM 5.95
CHEMBL440757 IC50 = 1500.0 nM 5.82
CHEMBL250505 IC50 = 2345.0 nM 5.63
CHEMBL250506 IC50 = 5235.0 nM 5.28