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Assay Detail

CHEMBL929786

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

Binding
Displacement of [3H]etorphine from opioid receptor in rat cerebrum
11
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

The influence of esters and carboxylic acids as the N-substituent of opioids. Part 1: Benzomorphans.
Metcalf MD, Aceto MD, Harris LS, Woods JH, Traynor JR, Coop A, May EL.
Bioorg Med Chem (2008) 16 : 869 -873
PubMed 17962026 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 7.40 9.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL19019 NALTREXONE 4.0 1 9.20
CHEMBL80 NALOXONE 4.0 1 8.20
CHEMBL415284 NALORPHINE 2.0 1 7.70
CHEMBL70 MORPHINE 4.0 1 7.63
CHEMBL401590 1 5.99
CHEMBL403062 1 5.68
CHEMBL271025 1 -
CHEMBL271026 1 -
CHEMBL401778 1 -
CHEMBL402200 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL19019 NALTREXONE EC50 = 0.63 nM 9.20
CHEMBL80 NALOXONE EC50 = 6.26 nM 8.20
CHEMBL415284 NALORPHINE EC50 = 20.0 nM 7.70
CHEMBL70 MORPHINE EC50 = 23.6 nM 7.63
CHEMBL401590 EC50 = 1020.0 nM 5.99
CHEMBL403062 EC50 = 2080.0 nM 5.68
CHEMBL271025 EC50 - -
CHEMBL271026 EC50 > 6000.0 nM -
CHEMBL401778 EC50 > 6000.0 nM -
CHEMBL402200 EC50 > 6.0 nM -
CHEMBL402200 EC50 > 6000.0 nM -