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Assay Detail

CHEMBL832667

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

Binding
Inhibition of bindign to recombinant human estrogen receptor alpha
30
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Estrogen receptor (CHEMBL206)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Estrogen receptor ligands. Part 9: Dihydrobenzoxathiin SERAMs with alkyl substituted pyrrolidine side chains and linkers.
Blizzard TA, Dininno F, Morgan JD, Chen HY, Wu JY, Kim S, Chan W, Birzin ET, Yang YT, Pai LY, Fitzgerald PM, Sharma N, Li Y, Zhang Z, Hayes EC, Dasilva CA, Tang W, Rohrer SP, Schaeffer JM, Hammond ML.
Bioorg Med Chem Lett (2005) 15 : 107 -113
PubMed 15582421 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 9.01 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL427324 1 9.52
CHEMBL183467 1 9.40
CHEMBL361601 1 9.40
CHEMBL182794 1 9.30
CHEMBL367350 1 9.30
CHEMBL182980 1 9.30
CHEMBL184202 1 9.15
CHEMBL179852 1 9.15
CHEMBL183489 1 9.15
CHEMBL183263 1 9.15
CHEMBL369545 1 9.15
CHEMBL367574 1 9.15
CHEMBL183344 1 9.10
CHEMBL183092 1 9.10
CHEMBL304552 1 9.10
CHEMBL183371 1 9.05
CHEMBL183388 1 9.05
CHEMBL182887 1 9.00
CHEMBL183049 1 9.00
CHEMBL2113027 1 8.96
CHEMBL183086 1 8.92
CHEMBL180792 2 8.89
CHEMBL135 ESTRADIOL 4.0 1 8.89
CHEMBL361751 1 8.77
CHEMBL81 RALOXIFENE 4.0 1 8.74
CHEMBL181944 1 8.60
CHEMBL362623 1 8.59
CHEMBL183584 1 8.52
CHEMBL183044 1 8.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL427324 IC50 = 0.3 nM 9.52
CHEMBL183467 IC50 = 0.4 nM 9.40
CHEMBL361601 IC50 = 0.4 nM 9.40
CHEMBL182794 IC50 = 0.5 nM 9.30
CHEMBL367350 IC50 = 0.5 nM 9.30
CHEMBL182980 IC50 = 0.5 nM 9.30
CHEMBL184202 IC50 = 0.7 nM 9.15
CHEMBL183263 IC50 = 0.7 nM 9.15
CHEMBL183489 IC50 = 0.7 nM 9.15
CHEMBL369545 IC50 = 0.7 nM 9.15
CHEMBL179852 IC50 = 0.7 nM 9.15
CHEMBL367574 IC50 = 0.7 nM 9.15
CHEMBL183092 IC50 = 0.8 nM 9.10
CHEMBL183344 IC50 = 0.8 nM 9.10
CHEMBL304552 IC50 = 0.8 nM 9.10
CHEMBL183388 IC50 = 0.9 nM 9.05
CHEMBL183371 IC50 = 0.9 nM 9.05
CHEMBL183049 IC50 = 1.0 nM 9.00
CHEMBL182887 IC50 = 1.0 nM 9.00
CHEMBL2113027 IC50 = 1.1 nM 8.96
CHEMBL183086 IC50 = 1.2 nM 8.92
CHEMBL135 ESTRADIOL IC50 = 1.3 nM 8.89
CHEMBL180792 IC50 = 1.3 nM 8.89
CHEMBL361751 IC50 = 1.7 nM 8.77
CHEMBL180792 IC50 = 1.7 nM 8.77
CHEMBL81 RALOXIFENE IC50 = 1.8 nM 8.74
CHEMBL181944 IC50 = 2.5 nM 8.60
CHEMBL362623 IC50 = 2.6 nM 8.59
CHEMBL183584 IC50 = 3.0 nM 8.52
CHEMBL183044 IC50 = 6.3 nM 8.20