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Assay Detail

CHEMBL808179

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

Binding
Inhibition of [3H]- N-allylnormetazocine ([3H]NANM) binding to sigma receptor
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sigma non-opioid intracellular receptor 1 (CHEMBL3602)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Phencyclidine-like effects of tetrahydroisoquinolines and related compounds.
Gray NM, Cheng BK, Mick SJ, Lair CM, Contreras PC.
J Med Chem (1989) 32 : 1242 -1248
PubMed 2542555 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 5.54 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL21326 1 7.30
CHEMBL279676 TENOCYCLIDINE 2.0 1 6.62
CHEMBL21640 1 6.37
CHEMBL275528 PHENCYCLIDINE 2.0 1 6.28
CHEMBL21805 1 5.89
CHEMBL21464 1 5.89
CHEMBL283744 1 5.80
CHEMBL284237 DIZOCILPINE 2.0 1 5.77
CHEMBL21277 1 5.75
CHEMBL442106 1 5.75
CHEMBL21465 1 5.70
CHEMBL21484 1 5.66
CHEMBL282475 1 5.60
CHEMBL277493 1 5.58
CHEMBL21342 1 5.58
CHEMBL283105 1 5.57
CHEMBL22053 1 5.57
CHEMBL278781 1 5.54
CHEMBL22005 1 5.51
CHEMBL22078 1 5.50
CHEMBL21920 1 5.47
CHEMBL21830 1 5.42
CHEMBL22133 1 5.42
CHEMBL283130 1 5.38
CHEMBL21273 1 5.30
CHEMBL418745 1 5.30
CHEMBL21323 1 5.27
CHEMBL21969 1 5.25
CHEMBL281568 1 5.20
CHEMBL283377 1 5.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL21326 IC50 = 50.0 nM 7.30
CHEMBL279676 TENOCYCLIDINE IC50 = 240.0 nM 6.62
CHEMBL21640 IC50 = 430.0 nM 6.37
CHEMBL275528 PHENCYCLIDINE IC50 = 530.0 nM 6.28
CHEMBL21805 IC50 = 1300.0 nM 5.89
CHEMBL21464 IC50 = 1300.0 nM 5.89
CHEMBL283744 IC50 = 1600.0 nM 5.80
CHEMBL284237 DIZOCILPINE IC50 = 1700.0 nM 5.77
CHEMBL21277 IC50 = 1800.0 nM 5.75
CHEMBL442106 IC50 = 1800.0 nM 5.75
CHEMBL21465 IC50 = 2000.0 nM 5.70
CHEMBL21484 IC50 = 2200.0 nM 5.66
CHEMBL282475 IC50 = 2500.0 nM 5.60
CHEMBL277493 IC50 = 2600.0 nM 5.58
CHEMBL21342 IC50 = 2600.0 nM 5.58
CHEMBL283105 IC50 = 2700.0 nM 5.57
CHEMBL22053 IC50 = 2700.0 nM 5.57
CHEMBL278781 IC50 = 2900.0 nM 5.54
CHEMBL22005 IC50 = 3100.0 nM 5.51
CHEMBL22078 IC50 = 3200.0 nM 5.50
CHEMBL21920 IC50 = 3400.0 nM 5.47
CHEMBL21830 IC50 = 3800.0 nM 5.42
CHEMBL22133 IC50 = 3800.0 nM 5.42
CHEMBL283130 IC50 = 4200.0 nM 5.38
CHEMBL21273 IC50 = 5000.0 nM 5.30
CHEMBL418745 IC50 = 5000.0 nM 5.30
CHEMBL21323 IC50 = 5400.0 nM 5.27
CHEMBL21969 IC50 = 5600.0 nM 5.25
CHEMBL281568 IC50 = 6300.0 nM 5.20
CHEMBL283377 IC50 = 7800.0 nM 5.11
CHEMBL21272 IC50 = 7800.0 nM 5.11
CHEMBL279013 IC50 = 10000.0 nM 5.00
CHEMBL21633 IC50 = 11000.0 nM 4.96
CHEMBL21911 IC50 = 11000.0 nM 4.96
CHEMBL21477 IC50 = 11000.0 nM 4.96
CHEMBL22009 IC50 = 15000.0 nM 4.82
CHEMBL283104 IC50 = 20000.0 nM 4.70
CHEMBL21672 IC50 > 30000.0 nM -