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Assay Detail

CHEMBL676547

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

Binding
Affinity against ET B receptor
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design and synthesis of nonpeptidal endothelin receptor antagonists based on the structure of a cyclic pentapeptide
Murugesan N, Zhengxiang Gu, Lee V, Webb ML, Liu EC, Hermsmeier M, Hunt JT
Bioorg Med Chem Lett (1995) 5 : 253 -258
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 4.97 5.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL314364 1 5.22
CHEMBL314691 BQ-123 2.0 1 5.16
CHEMBL86489 1 5.16
CHEMBL421349 1 5.10
CHEMBL314915 1 5.05
CHEMBL315096 1 4.96
CHEMBL313184 1 4.92
CHEMBL86581 1 4.22
CHEMBL87859 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL314364 Ki = 6000.0 nM 5.22
CHEMBL314691 BQ-123 Ki = 7000.0 nM 5.16
CHEMBL86489 Ki = 7000.0 nM 5.16
CHEMBL421349 Ki = 8000.0 nM 5.10
CHEMBL314915 Ki = 9000.0 nM 5.05
CHEMBL315096 Ki = 11000.0 nM 4.96
CHEMBL313184 Ki = 12000.0 nM 4.92
CHEMBL86581 Ki = 60000.0 nM 4.22
CHEMBL87859 Ki > 100000.0 nM -