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Assay Detail

CHEMBL648470

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

Binding
Alpha-2 adrenergic receptor binding affinity by measuring the displacement of [3H]clonidine binding in rat cerebral cortex
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adrenergic receptor alpha-2 (CHEMBL2093864)
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 14 6.09 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL341723 1 7.50
CHEMBL140477 1 7.00
CHEMBL142912 1 7.00
CHEMBL141194 1 6.43
CHEMBL143397 1 6.36
CHEMBL143463 1 6.28
CHEMBL142995 1 5.82
CHEMBL142635 NAFTOPIDIL 4.0 1 5.80
CHEMBL143288 1 5.77
CHEMBL142859 1 5.64
CHEMBL142948 1 5.52
CHEMBL142474 1 5.48
CHEMBL143944 1 5.34
CHEMBL143923 1 5.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL341723 Ki = 32.0 nM 7.50
CHEMBL140477 Ki = 99.0 nM 7.00
CHEMBL142912 Ki = 100.0 nM 7.00
CHEMBL141194 Ki = 370.0 nM 6.43
CHEMBL143397 Ki = 440.0 nM 6.36
CHEMBL143463 Ki = 530.0 nM 6.28
CHEMBL142995 Ki = 1500.0 nM 5.82
CHEMBL142635 NAFTOPIDIL Ki = 1600.0 nM 5.80
CHEMBL143288 Ki = 1706.0 nM 5.77
CHEMBL142859 Ki = 2300.0 nM 5.64
CHEMBL142948 Ki = 3000.0 nM 5.52
CHEMBL142474 Ki = 3300.0 nM 5.48
CHEMBL143944 Ki = 4600.0 nM 5.34
CHEMBL143923 Ki = 4600.0 nM 5.34