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Assay Detail

CHEMBL862985

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

Binding
Displacement of [3H]clonidine from Adrenergic alpha-2 receptor
28
Total Activities
28
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 (CHEMBL2095158)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Inhibitors of phenylethanolamine N-methyltransferase devoid of alpha2-adrenoceptor affinity.
Grunewald GL, Lu J, Criscione KR, Okoro CO.
Bioorg Med Chem Lett (2005) 15 : 5319 -5323
PubMed 16169723 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 28 5.46 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL287837 1 7.68
CHEMBL26828 1 6.66
CHEMBL200375 1 5.96
CHEMBL437699 1 5.92
CHEMBL200563 1 5.41
CHEMBL439864 1 4.55
CHEMBL59719 1 4.51
CHEMBL198733 1 4.44
CHEMBL26717 1 4.00
CHEMBL199008 1 -
CHEMBL112038 1 -
CHEMBL342322 1 -
CHEMBL359205 1 -
CHEMBL112351 1 -
CHEMBL371084 1 -
CHEMBL197019 1 -
CHEMBL196970 1 -
CHEMBL112964 1 -
CHEMBL112357 1 -
CHEMBL371898 1 -
CHEMBL198896 1 -
CHEMBL196770 1 -
CHEMBL370794 1 -
CHEMBL200910 1 -
CHEMBL444793 1 -
CHEMBL41647 1 -
CHEMBL200560 1 -
CHEMBL197380 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL287837 Ki = 21.0 nM 7.68
CHEMBL26828 Ki = 220.0 nM 6.66
CHEMBL200375 Ki = 1100.0 nM 5.96
CHEMBL437699 Ki = 1200.0 nM 5.92
CHEMBL200563 Ki = 3900.0 nM 5.41
CHEMBL439864 Ki = 28000.0 nM 4.55
CHEMBL59719 Ki = 31000.0 nM 4.51
CHEMBL198733 Ki = 36000.0 nM 4.44
CHEMBL26717 Ki = 100000.0 nM 4.00
CHEMBL199008 Ki > 1000000.0 nM -
CHEMBL112038 Ki = 2900000.0 nM -
CHEMBL342322 Ki - -
CHEMBL359205 Ki - -
CHEMBL112351 Ki = 1400000.0 nM -
CHEMBL371084 Ki - -
CHEMBL197019 Ki - -
CHEMBL196970 Ki > 1000000.0 nM -
CHEMBL112964 Ki > 1000000.0 nM -
CHEMBL112357 Ki = 3900000.0 nM -
CHEMBL371898 Ki - -
CHEMBL198896 Ki > 1000000.0 nM -
CHEMBL196770 Ki - -
CHEMBL370794 Ki - -
CHEMBL200910 Ki > 1000000.0 nM -
CHEMBL444793 Ki = 400000.0 nM -
CHEMBL41647 Ki = 1400000.0 nM -
CHEMBL200560 Ki > 1000000.0 nM -
CHEMBL197380 Ki - -