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Assay Detail

CHEMBL759756

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Binding
In vitro inhibitory potency was measured against phenylethanolamine N-methyl-transferase
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Inhibitors of phenylethanolamine N-methyltransferase and epinephrine biosynthesis. 1. Chloro-substituted 1,2,3,4-tetrahydroisoquinolines.
Bondinell WE, Chapin FW, Girard GR, Kaiser C, Krog AJ, Pavloff AM, Schwartz MS, Silvestri JS, Vaidya PD, Lam BL, Wellman GR, Pendleton RG.
J Med Chem (1980) 23 : 506 -511
PubMed 7381849 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.29 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL287837 1 8.00
CHEMBL356439 1 7.00
CHEMBL149816 1 6.70
CHEMBL149023 1 6.70
CHEMBL146188 1 6.70
CHEMBL147230 1 4.70
CHEMBL149022 1 4.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL287837 IC50 = 10.0 nM 8.00
CHEMBL356439 IC50 = 100.0 nM 7.00
CHEMBL149816 IC50 = 200.0 nM 6.70
CHEMBL149023 IC50 = 200.0 nM 6.70
CHEMBL146188 IC50 = 200.0 nM 6.70
CHEMBL147230 IC50 = 20000.0 nM 4.70
CHEMBL149022 IC50 = 60000.0 nM 4.22