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Assay Detail

CHEMBL645558

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

Binding
Alpha-1 adrenergic receptor binding affinity by measuring the displacement of [3H]prazosin binding in rat brain
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adrenergic receptor alpha-1 (CHEMBL1907610)
Type PROTEIN FAMILY
Organism Rattus norvegicus

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 16 7.45 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL143463 1 8.89
CHEMBL142948 1 8.08
CHEMBL140477 1 7.85
CHEMBL141194 1 7.82
CHEMBL142474 1 7.80
CHEMBL143944 1 7.70
CHEMBL143288 1 7.64
CHEMBL341723 1 7.64
CHEMBL341614 1 7.57
CHEMBL143397 1 7.42
CHEMBL142635 NAFTOPIDIL 4.0 1 7.41
CHEMBL142995 1 7.22
CHEMBL142859 1 7.14
CHEMBL143608 1 7.05
CHEMBL143923 1 6.27
CHEMBL143679 1 5.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL143463 Ki = 1.3 nM 8.89
CHEMBL142948 Ki = 8.3 nM 8.08
CHEMBL140477 Ki = 14.0 nM 7.85
CHEMBL141194 Ki = 15.0 nM 7.82
CHEMBL142474 Ki = 16.0 nM 7.80
CHEMBL143944 Ki = 20.0 nM 7.70
CHEMBL143288 Ki = 23.0 nM 7.64
CHEMBL341723 Ki = 23.0 nM 7.64
CHEMBL341614 Ki = 27.0 nM 7.57
CHEMBL143397 Ki = 38.0 nM 7.42
CHEMBL142635 NAFTOPIDIL Ki = 39.0 nM 7.41
CHEMBL142995 Ki = 60.0 nM 7.22
CHEMBL142859 Ki = 73.0 nM 7.14
CHEMBL143608 Ki = 90.0 nM 7.05
CHEMBL143923 Ki = 540.0 nM 6.27
CHEMBL143679 Ki = 2400.0 nM 5.62