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Assay Detail

CHEMBL652294

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

Binding
Beta-2 adrenergic receptor binding affinity by measuring the displacement of [3H]DHA binding in rat lung
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Beta-2 adrenergic receptor (CHEMBL2289)
Type SINGLE PROTEIN
Organism Canis lupus familiaris

Publication

(1,4-Benzothiazinyloxy)alkylpiperazine derivatives as potential antihypertensive agents.
Cecchetti V, Schiaffella F, Tabarrini O, Fravolini A.
Bioorg Med Chem Lett (2000) 10 : 465 -468
PubMed 10743949 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.47 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL143463 1 8.57
CHEMBL140908 1 7.64
CHEMBL341614 1 7.06
CHEMBL142635 NAFTOPIDIL 4.0 1 6.00
CHEMBL142474 1 5.40
CHEMBL143944 1 5.32
CHEMBL143608 1 5.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL143463 Ki = 2.7 nM 8.57
CHEMBL140908 Ki = 23.0 nM 7.64
CHEMBL341614 Ki = 88.0 nM 7.06
CHEMBL142635 NAFTOPIDIL Ki = 1000.0 nM 6.00
CHEMBL142474 Ki = 4000.0 nM 5.40
CHEMBL143944 Ki = 4800.0 nM 5.32
CHEMBL143608 Ki = 5300.0 nM 5.28