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Assay Detail

CHEMBL748048

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

Binding
Tested for displacement of radioligand [3H]-Naloxone from opiate receptor
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Opioid receptor (CHEMBL2095192)
Type PROTEIN FAMILY
Organism Mus musculus

Publication

Structure-affinity relationship studies on 5-HT1A receptor ligands. 1. Heterobicyclic phenylpiperazines with N4-alkyl substituents.
van Steen BJ, van Wijngaarden I, Tulp MT, Soudijn W.
J Med Chem (1993) 36 : 2751 -2760
PubMed 8410989 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.89 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL441636 1 7.52
CHEMBL328583 1 7.26
CHEMBL328019 1 6.82
CHEMBL92960 1 6.70
CHEMBL92779 1 6.40
CHEMBL607 MEPERIDINE 4.0 1 6.30
CHEMBL92124 1 6.05
CHEMBL89961 1 5.40
CHEMBL285244 1 5.30
CHEMBL96626 1 5.10
CHEMBL92787 1 4.70
CHEMBL440699 1 4.70
CHEMBL329911 1 4.30
CHEMBL93306 1 -
CHEMBL90632 1 -
CHEMBL92403 1 -
CHEMBL92303 1 -
CHEMBL93296 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL441636 IC50 = 30.0 nM 7.52
CHEMBL328583 IC50 = 55.0 nM 7.26
CHEMBL328019 IC50 = 150.0 nM 6.82
CHEMBL92960 IC50 = 200.0 nM 6.70
CHEMBL92779 IC50 = 400.0 nM 6.40
CHEMBL607 MEPERIDINE IC50 = 500.0 nM 6.30
CHEMBL92124 IC50 = 900.0 nM 6.05
CHEMBL89961 IC50 = 4000.0 nM 5.40
CHEMBL285244 IC50 = 5000.0 nM 5.30
CHEMBL96626 IC50 = 8000.0 nM 5.10
CHEMBL92787 IC50 = 20000.0 nM 4.70
CHEMBL440699 IC50 = 20000.0 nM 4.70
CHEMBL329911 IC50 = 50000.0 nM 4.30
CHEMBL93306 IC50 = 400000.0 nM -
CHEMBL90632 IC50 = 500000.0 nM -
CHEMBL92403 IC50 = 700000.0 nM -
CHEMBL92303 IC50 = 200000.0 nM -
CHEMBL93296 IC50 = 200000.0 nM -