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Assay Detail

CHEMBL675446

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

Binding
Inhibition constant for the displacement of specific binding of [125I]-ET (Kd=2 nM) bound to rat pituitary membrane
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Pituitary gland
Confidence 5 — Multiple protein complex / RNA
Curated By Expert

Target

Endothelin receptor (CHEMBL2111453)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Structure-activity studies of reduced-size gonadotropin-releasing hormone agonists derived from the sequence of an endothelin antagonist.
Yahalom D, Rahimipour S, Koch Y, Ben-Aroya N, Fridkin M.
J Med Chem (2000) 43 : 2824 -2830
PubMed 10956190 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 5.47 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL317064 1 6.92
CHEMBL327528 1 5.22
CHEMBL329946 1 4.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL317064 Ki = 120.0 nM 6.92
CHEMBL327528 Ki = 6000.0 nM 5.22
CHEMBL329946 Ki = 55000.0 nM 4.26