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Assay Detail

CHEMBL759752

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Binding
Inhibitory constant against human phenylethanolamine N-methyl-transferase over-expressed in Escherichia coli
31
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Phenylethanolamine N-methyltransferase (CHEMBL4617)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Phenylethanolamine N-methyltransferase kinetics: bovine versus recombinant human enzyme.
Grunewald GL, McLeish MJ, Criscione KR.
Bioorg Med Chem Lett (2001) 11 : 1579 -1582
PubMed 11412985 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 31 5.53 6.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38681 1 6.55
CHEMBL337144 1 6.52
CHEMBL287837 1 6.52
CHEMBL26717 1 6.24
CHEMBL275595 1 6.18
CHEMBL39493 1 6.09
CHEMBL290890 1 6.02
CHEMBL43183 1 6.00
CHEMBL342625 1 5.96
CHEMBL39928 1 5.92
CHEMBL336026 1 5.82
CHEMBL43021 1 5.70
CHEMBL41647 1 5.68
CHEMBL40081 1 5.58
CHEMBL287360 1 5.46
CHEMBL135908 1 5.35
CHEMBL35982 3 5.00
CHEMBL290010 1 5.00
CHEMBL41689 1 4.89
CHEMBL14346 1,2,3,4-TETRAHYDROISOQUINOLINE 1 4.82
CHEMBL39125 1 4.70
CHEMBL288524 1 4.29
CHEMBL36909 1 4.21
CHEMBL41079 1 -
CHEMBL19969 1 -
CHEMBL288525 1 -
CHEMBL278059 1 -
CHEMBL39492 1 -
CHEMBL282700 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38681 Ki = 280.0 nM 6.55
CHEMBL337144 Ki = 300.0 nM 6.52
CHEMBL287837 Ki = 300.0 nM 6.52
CHEMBL26717 Ki = 580.0 nM 6.24
CHEMBL275595 Ki = 660.0 nM 6.18
CHEMBL39493 Ki = 810.0 nM 6.09
CHEMBL290890 Ki = 950.0 nM 6.02
CHEMBL43183 Ki = 1000.0 nM 6.00
CHEMBL342625 Ki = 1100.0 nM 5.96
CHEMBL39928 Ki = 1200.0 nM 5.92
CHEMBL336026 Ki = 1500.0 nM 5.82
CHEMBL43021 Ki = 2000.0 nM 5.70
CHEMBL41647 Ki = 2100.0 nM 5.68
CHEMBL40081 Ki = 2600.0 nM 5.58
CHEMBL287360 Ki = 3500.0 nM 5.46
CHEMBL135908 Ki = 4500.0 nM 5.35
CHEMBL35982 Ki = 10000.0 nM 5.00
CHEMBL290010 Ki = 10000.0 nM 5.00
CHEMBL35982 Ki = 13000.0 nM 4.89
CHEMBL41689 Ki = 13000.0 nM 4.89
CHEMBL14346 1,2,3,4-TETRAHYDROISOQUINOLINE Ki = 15000.0 nM 4.82
CHEMBL35982 Ki = 16000.0 nM 4.80
CHEMBL39125 Ki = 20000.0 nM 4.70
CHEMBL288524 Ki = 51000.0 nM 4.29
CHEMBL36909 Ki = 62000.0 nM 4.21
CHEMBL19969 Ki = 4800000.0 nM -
CHEMBL41079 Ki = 530000.0 nM -
CHEMBL288525 Ki = 180000.0 nM -
CHEMBL278059 Ki = 830000.0 nM -
CHEMBL39492 Ki = 730000.0 nM -
CHEMBL282700 Ki = 430000.0 nM -