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Assay Detail

CHEMBL671687

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Functional
Tested for antagonistic activity against Endothelin B receptor in the rat cerebellum.
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Cerebellum
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Discovery of a novel series of orally active non-peptide endothelin-A (ETA) receptor-selective antagonists.
Doherty AM, Patt WC, Edmunds JJ, Berryman KA, Reisdorph BR, Plummer MS, Shahripour A, Lee C, Cheng XM, Walker DM.
J Med Chem (1995) 38 : 1259 -1263
PubMed 7731010 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.68 6.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL11115 1 6.66
CHEMBL274383 PD-155080 1 6.30
CHEMBL10733 1 6.14
CHEMBL273613 1 5.35
CHEMBL10374 1 5.35
CHEMBL267094 1 5.28
CHEMBL11131 1 4.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL11115 IC50 = 220.0 nM 6.66
CHEMBL274383 PD-155080 IC50 = 500.0 nM 6.30
CHEMBL10733 IC50 = 720.0 nM 6.14
CHEMBL273613 IC50 = 4500.0 nM 5.35
CHEMBL10374 IC50 = 4500.0 nM 5.35
CHEMBL267094 IC50 = 5200.0 nM 5.28
CHEMBL11131 IC50 = 22000.0 nM 4.66