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Assay Detail

CHEMBL648161

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

Binding
In vitro binding affinity determined for alpha-2 adrenergic receptor by the percentage displacement of [3H]- clonidine at 10e-6 M
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adrenergic receptor alpha-2 (CHEMBL2093864)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

2,4-Diamino-6,7-dimethoxyquinazolines. 2. 2-(4-Carbamoylpiperidino) derivatives as alpha 1-adrenoceptor antagonists and antihypertensive agents.
Alabaster VA, Campbell SF, Danilewicz JC, Greengrass CW, Plews RM.
J Med Chem (1987) 30 : 999 -1003
PubMed 2884316 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 7.06 7.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6789 1 7.27
CHEMBL269537 1 7.27
CHEMBL6766 1 7.26
CHEMBL266927 1 7.25
CHEMBL266317 1 7.25
CHEMBL6481 1 7.21
CHEMBL6424 1 7.21
CHEMBL6556 1 7.20
CHEMBL267457 1 7.19
CHEMBL415288 1 7.17
CHEMBL6474 1 7.15
CHEMBL2 PRAZOSIN 4.0 1 5.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6789 Ki = 53.9 nM 7.27
CHEMBL269537 Ki = 53.3 nM 7.27
CHEMBL6766 Ki = 54.8 nM 7.26
CHEMBL266927 Ki = 55.6 nM 7.25
CHEMBL266317 Ki = 56.0 nM 7.25
CHEMBL6481 Ki = 61.3 nM 7.21
CHEMBL6424 Ki = 62.1 nM 7.21
CHEMBL6556 Ki = 62.7 nM 7.20
CHEMBL267457 Ki = 64.7 nM 7.19
CHEMBL415288 Ki = 68.1 nM 7.17
CHEMBL6474 Ki = 71.4 nM 7.15
CHEMBL2 PRAZOSIN Ki = 4830.0 nM 5.32