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Assay Detail

CHEMBL890213

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

Binding
Displacement of [3H]clonidine from adrenergic alpha2 receptor in Sprague-Dawley rat cortex membrane
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Exploring the active site of phenylethanolamine N-methyltransferase with 1,2,3,4-tetrahydrobenz[h]isoquinoline inhibitors.
Grunewald GL, Seim MR, Regier RC, Criscione KR.
Bioorg Med Chem (2007) 15 : 1298 -1310
PubMed 17126018 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 6.41 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL243176 1 7.96
CHEMBL41749 1 7.80
CHEMBL287837 1 7.68
CHEMBL130744 1 7.11
CHEMBL243836 1 7.00
CHEMBL243835 1 6.80
CHEMBL281864 1 6.64
CHEMBL14346 1,2,3,4-TETRAHYDROISOQUINOLINE 1 6.46
CHEMBL243834 1 6.39
CHEMBL390453 1 6.23
CHEMBL338311 1 6.08
CHEMBL413311 1 5.54
CHEMBL281289 1 5.37
CHEMBL27162 1 5.14
CHEMBL26717 1 4.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL243176 Ki = 11.0 nM 7.96
CHEMBL41749 Ki = 16.0 nM 7.80
CHEMBL287837 Ki = 21.0 nM 7.68
CHEMBL130744 Ki = 78.0 nM 7.11
CHEMBL243836 Ki = 100.0 nM 7.00
CHEMBL243835 Ki = 160.0 nM 6.80
CHEMBL281864 Ki = 230.0 nM 6.64
CHEMBL14346 1,2,3,4-TETRAHYDROISOQUINOLINE Ki = 350.0 nM 6.46
CHEMBL243834 Ki = 410.0 nM 6.39
CHEMBL390453 Ki = 590.0 nM 6.23
CHEMBL338311 Ki = 840.0 nM 6.08
CHEMBL413311 Ki = 2900.0 nM 5.54
CHEMBL281289 Ki = 4300.0 nM 5.37
CHEMBL27162 Ki = 7300.0 nM 5.14
CHEMBL26717 Ki = 100000.0 nM 4.00