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Assay Detail

CHEMBL862979

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Binding
Inhibitory activity against human PNMT
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Phenylethanolamine N-methyltransferase (CHEMBL4617)
Type SINGLE PROTEIN
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 5.94 8.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL287837 1 8.51
CHEMBL200375 1 7.77
CHEMBL41647 1 7.28
CHEMBL59719 1 7.14
CHEMBL26828 1 7.03
CHEMBL26717 1 6.55
CHEMBL197019 1 6.34
CHEMBL437699 1 6.32
CHEMBL439864 1 6.31
CHEMBL371898 1 6.30
CHEMBL370794 1 6.03
CHEMBL198896 1 6.01
CHEMBL196970 1 6.00
CHEMBL359205 1 5.92
CHEMBL197380 1 5.72
CHEMBL371084 1 5.72
CHEMBL200910 1 5.72
CHEMBL112351 1 5.64
CHEMBL112964 1 5.50
CHEMBL196770 1 5.38
CHEMBL342322 1 5.36
CHEMBL200563 1 5.36
CHEMBL198733 1 5.34
CHEMBL200560 1 5.10
CHEMBL112038 1 4.68
CHEMBL444793 1 4.64
CHEMBL112357 1 4.39
CHEMBL199008 1 4.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL287837 Ki = 3.1 nM 8.51
CHEMBL200375 Ki = 17.0 nM 7.77
CHEMBL41647 Ki = 52.0 nM 7.28
CHEMBL59719 Ki = 72.0 nM 7.14
CHEMBL26828 Ki = 93.0 nM 7.03
CHEMBL26717 Ki = 280.0 nM 6.55
CHEMBL197019 Ki = 460.0 nM 6.34
CHEMBL437699 Ki = 480.0 nM 6.32
CHEMBL439864 Ki = 490.0 nM 6.31
CHEMBL371898 Ki = 500.0 nM 6.30
CHEMBL370794 Ki = 940.0 nM 6.03
CHEMBL198896 Ki = 980.0 nM 6.01
CHEMBL196970 Ki = 990.0 nM 6.00
CHEMBL359205 Ki = 1200.0 nM 5.92
CHEMBL197380 Ki = 1900.0 nM 5.72
CHEMBL371084 Ki = 1900.0 nM 5.72
CHEMBL200910 Ki = 1900.0 nM 5.72
CHEMBL112351 Ki = 2300.0 nM 5.64
CHEMBL112964 Ki = 3200.0 nM 5.50
CHEMBL196770 Ki = 4200.0 nM 5.38
CHEMBL342322 Ki = 4400.0 nM 5.36
CHEMBL200563 Ki = 4400.0 nM 5.36
CHEMBL198733 Ki = 4600.0 nM 5.34
CHEMBL200560 Ki = 8000.0 nM 5.10
CHEMBL112038 Ki = 21000.0 nM 4.68
CHEMBL444793 Ki = 23000.0 nM 4.64
CHEMBL112357 Ki = 41000.0 nM 4.39
CHEMBL199008 Ki = 60000.0 nM 4.22