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Assay Detail

CHEMBL677407

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

Binding
Inhibition of [125I]-endothelin-3 [ET-3] binding to endothelin B receptor (ETB) of rat cerebellum
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Cerebellum
Confidence 9 — Direct single protein target
Curated By Expert

Target

Endothelin receptor type B (CHEMBL4631)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Structure-activity and biophysical studies of the C-terminal hexapeptide of endothelin
Leonard DM, Reily MD, Dunbar JB, Holub KE, Cody WL, Hill KE, Welch KM, Flynn MA, Reynolds EE, Doherty AM
Bioorg Med Chem Lett (1995) 5 : 967 -972
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.41 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1791271 1 7.22
CHEMBL2369709 1 6.57
CHEMBL2369713 1 6.11
CHEMBL1791279 1 5.70
CHEMBL2369714 1 5.18
CHEMBL1791280 1 5.08
CHEMBL289687 1 5.04
CHEMBL2369710 1 4.89
CHEMBL1791277 1 4.85
CHEMBL2369711 1 4.47
CHEMBL432091 1 4.37
CHEMBL34540 1 -
CHEMBL1791272 1 -
CHEMBL2369712 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1791271 IC50 = 60.0 nM 7.22
CHEMBL2369709 IC50 = 270.0 nM 6.57
CHEMBL2369713 IC50 = 780.0 nM 6.11
CHEMBL1791279 IC50 = 2000.0 nM 5.70
CHEMBL2369714 IC50 = 6600.0 nM 5.18
CHEMBL1791280 IC50 = 8300.0 nM 5.08
CHEMBL289687 IC50 = 9100.0 nM 5.04
CHEMBL2369710 IC50 = 13000.0 nM 4.89
CHEMBL1791277 IC50 = 14000.0 nM 4.85
CHEMBL2369711 IC50 = 34000.0 nM 4.47
CHEMBL432091 IC50 = 43000.0 nM 4.37
CHEMBL34540 IC50 > 50000.0 nM -
CHEMBL1791272 IC50 > 50000.0 nM -
CHEMBL2369712 IC50 > 50000.0 nM -