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Assay Detail

CHEMBL643680

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

Binding
The compound was tested in vitro for binding affinity against Alpha-2 adrenergic receptor using [3H]clonidine
8
Total Activities
8
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

Synthesis and evaluation of 3-trifluoromethyl-7-substituted-1,2,3, 4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.
Grunewald GL, Caldwell TM, Li Q, Criscione KR.
J Med Chem (1999) 42 : 3315 -3323
PubMed 10464018 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 6.12 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL287837 1 7.68
CHEMBL14346 1,2,3,4-TETRAHYDROISOQUINOLINE 1 6.46
CHEMBL59994 1 6.17
CHEMBL60434 1 6.12
CHEMBL38681 1 5.35
CHEMBL6409 CGS-19281A 1 4.92
CHEMBL444793 1 -
CHEMBL41647 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL287837 Ki = 21.0 nM 7.68
CHEMBL14346 1,2,3,4-TETRAHYDROISOQUINOLINE Ki = 350.0 nM 6.46
CHEMBL59994 Ki = 670.0 nM 6.17
CHEMBL60434 Ki = 760.0 nM 6.12
CHEMBL38681 Ki = 4500.0 nM 5.35
CHEMBL6409 CGS-19281A Ki = 12000.0 nM 4.92
CHEMBL444793 Ki = 400000.0 nM -
CHEMBL41647 Ki = 1400000.0 nM -