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Assay Detail

CHEMBL682290

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

Binding
Inhibitory concentration against estrogen receptor alpha using radioligand binding assay.
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Estrogen receptor (CHEMBL206)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Estrogen receptor modulators: identification and structure-activity relationships of potent ERalpha-selective tetrahydroisoquinoline ligands.
Renaud J, Bischoff SF, Buhl T, Floersheim P, Fournier B, Halleux C, Kallen J, Keller H, Schlaeppi JM, Stark W.
J Med Chem (2003) 46 : 2945 -2957
PubMed 12825935 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 7.44 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2113354 1 8.40
CHEMBL2137046 1 7.77
CHEMBL101382 1 7.72
CHEMBL316080 1 7.68
CHEMBL1116 RALOXIFENE HYDROCHLORIDE 4.0 1 7.66
CHEMBL100763 1 7.57
CHEMBL174502 1 7.55
CHEMBL135 ESTRADIOL 4.0 1 7.55
CHEMBL101807 1 7.54
CHEMBL327515 1 7.51
CHEMBL328388 1 7.51
CHEMBL101997 1 7.51
CHEMBL100617 1 7.47
CHEMBL103294 1 7.46
CHEMBL98558 1 7.42
CHEMBL101083 1 7.42
CHEMBL319211 1 7.41
CHEMBL98470 1 7.36
CHEMBL100595 1 7.34
CHEMBL103305 1 7.31
CHEMBL328810 1 7.25
CHEMBL319678 1 7.18
CHEMBL100231 1 7.15
CHEMBL101719 1 7.15
CHEMBL323119 1 7.03
CHEMBL103650 1 6.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2113354 IC50 = 4.0 nM 8.40
CHEMBL2137046 IC50 = 17.0 nM 7.77
CHEMBL101382 IC50 = 19.0 nM 7.72
CHEMBL316080 IC50 = 21.0 nM 7.68
CHEMBL1116 RALOXIFENE HYDROCHLORIDE IC50 = 22.0 nM 7.66
CHEMBL100763 IC50 = 27.0 nM 7.57
CHEMBL174502 IC50 = 28.0 nM 7.55
CHEMBL135 ESTRADIOL IC50 = 28.0 nM 7.55
CHEMBL101807 IC50 = 29.0 nM 7.54
CHEMBL327515 IC50 = 31.0 nM 7.51
CHEMBL328388 IC50 = 31.0 nM 7.51
CHEMBL101997 IC50 = 31.0 nM 7.51
CHEMBL100617 IC50 = 34.0 nM 7.47
CHEMBL103294 IC50 = 35.0 nM 7.46
CHEMBL98558 IC50 = 38.0 nM 7.42
CHEMBL101083 IC50 = 38.0 nM 7.42
CHEMBL319211 IC50 = 39.0 nM 7.41
CHEMBL98470 IC50 = 44.0 nM 7.36
CHEMBL100595 IC50 = 46.0 nM 7.34
CHEMBL103305 IC50 = 49.0 nM 7.31
CHEMBL328810 IC50 = 56.0 nM 7.25
CHEMBL319678 IC50 = 66.0 nM 7.18
CHEMBL100231 IC50 = 71.0 nM 7.15
CHEMBL101719 IC50 = 71.0 nM 7.15
CHEMBL323119 IC50 = 94.0 nM 7.03
CHEMBL103650 IC50 = 285.0 nM 6.54