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Assay Detail

CHEMBL677101

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Binding
Binding affinity for estrogen receptor of rabbit uterine skeletal muscle tissue
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Estrogen receptor (CHEMBL2093866)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Synthesis and pharmacology of a novel pyrrolo[2,1,5-cd] indolizine (NNC 45-0095), a high affinity non-steroidal agonist for the estrogen receptor.
Jørgensen AS, Jacobsen P, Christiansen LB, Bury PS, Kanstrup A, Thorpe SM, Bain S, Naerum L, Wassermann K.
Bioorg Med Chem Lett (2000) 10 : 399 -402
PubMed 10714509 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.59 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL135 ESTRADIOL 4.0 1 9.15
CHEMBL1628161 MOXESTROL 2.0 1 8.60
CHEMBL420017 1 8.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL135 ESTRADIOL IC50 = 0.7 nM 9.15
CHEMBL1628161 MOXESTROL IC50 = 2.5 nM 8.60
CHEMBL420017 IC50 = 9.5 nM 8.02