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Assay Detail

CHEMBL764432

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

Binding
Inhibition of [3H]1-[1-(2-thienyl) piperidine ([3H]TCP) binding to phencyclidine receptor
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Lysosomal Pro-X carboxypeptidase (CHEMBL2335)
Type SINGLE PROTEIN
Organism Homo sapiens

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 26 5.68 8.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL284237 DIZOCILPINE 2.0 1 8.28
CHEMBL279676 TENOCYCLIDINE 2.0 1 7.70
CHEMBL275528 PHENCYCLIDINE 2.0 1 7.04
CHEMBL21326 1 6.12
CHEMBL21640 1 6.00
CHEMBL21465 1 5.72
CHEMBL21464 1 5.64
CHEMBL21805 1 5.42
CHEMBL21342 1 5.41
CHEMBL283105 1 5.36
CHEMBL21277 1 5.31
CHEMBL21920 1 5.28
CHEMBL283744 1 5.27
CHEMBL22005 1 5.21
CHEMBL21969 1 5.02
CHEMBL282475 1 4.96
CHEMBL21911 1 4.92
CHEMBL21273 1 4.70
CHEMBL278781 1 4.62
CHEMBL283130 1 -
CHEMBL279013 1 -
CHEMBL21672 1 -
CHEMBL277493 1 -
CHEMBL22053 1 -
CHEMBL22078 1 -
CHEMBL22009 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL284237 DIZOCILPINE IC50 = 5.3 nM 8.28
CHEMBL279676 TENOCYCLIDINE IC50 = 20.0 nM 7.70
CHEMBL275528 PHENCYCLIDINE IC50 = 91.0 nM 7.04
CHEMBL21326 IC50 = 760.0 nM 6.12
CHEMBL21640 IC50 = 1000.0 nM 6.00
CHEMBL21465 IC50 = 1900.0 nM 5.72
CHEMBL21464 IC50 = 2300.0 nM 5.64
CHEMBL21805 IC50 = 3800.0 nM 5.42
CHEMBL21342 IC50 = 3900.0 nM 5.41
CHEMBL283105 IC50 = 4400.0 nM 5.36
CHEMBL21277 IC50 = 4900.0 nM 5.31
CHEMBL21920 IC50 = 5300.0 nM 5.28
CHEMBL283744 IC50 = 5400.0 nM 5.27
CHEMBL22005 IC50 = 6200.0 nM 5.21
CHEMBL21969 IC50 = 9500.0 nM 5.02
CHEMBL282475 IC50 = 11000.0 nM 4.96
CHEMBL21911 IC50 = 12000.0 nM 4.92
CHEMBL21273 IC50 = 20000.0 nM 4.70
CHEMBL278781 IC50 = 24000.0 nM 4.62
CHEMBL283130 IC50 > 30000.0 nM -
CHEMBL279013 IC50 > 30000.0 nM -
CHEMBL21672 IC50 > 30000.0 nM -
CHEMBL277493 IC50 > 30000.0 nM -
CHEMBL22053 IC50 > 30000.0 nM -
CHEMBL22078 IC50 > 30000.0 nM -
CHEMBL22009 IC50 > 30000.0 nM -