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Assay Detail

CHEMBL757327

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

Binding
Displacement of [3H]nalotrexone from rat-brain Opioid receptors
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Opioid receptor (CHEMBL2094129)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Potential affinity labels for the opiate receptor based on fentanyl and related compounds.
Maryanoff BE, Simon EJ, Gioannini T, Gorissen H.
J Med Chem (1982) 25 : 913 -919
PubMed 6288945 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.82 9.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL28198 1 9.60
CHEMBL12391 1 8.89
CHEMBL658 SUFENTANIL 4.0 1 8.64
CHEMBL2304164 1 8.60
CHEMBL539579 1 8.30
CHEMBL535806 1 7.80
CHEMBL556159 1 7.77
CHEMBL596 FENTANYL 4.0 1 7.60
CHEMBL70 MORPHINE 4.0 1 7.57
CHEMBL174189 1 7.16
CHEMBL537622 1 6.97
CHEMBL171932 1 6.82
CHEMBL172034 1 6.00
CHEMBL173897 1 -
CHEMBL556549 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL28198 IC50 = 0.25 nM 9.60
CHEMBL12391 IC50 = 1.3 nM 8.89
CHEMBL658 SUFENTANIL IC50 = 2.3 nM 8.64
CHEMBL2304164 IC50 = 2.5 nM 8.60
CHEMBL539579 IC50 = 5.0 nM 8.30
CHEMBL535806 IC50 = 16.0 nM 7.80
CHEMBL556159 IC50 = 17.0 nM 7.77
CHEMBL596 FENTANYL IC50 = 25.0 nM 7.60
CHEMBL70 MORPHINE IC50 = 27.0 nM 7.57
CHEMBL174189 IC50 = 70.0 nM 7.16
CHEMBL537622 IC50 = 107.0 nM 6.97
CHEMBL171932 IC50 = 152.0 nM 6.82
CHEMBL172034 IC50 = 1000.0 nM 6.00
CHEMBL173897 IC50 > 1000.0 nM -
CHEMBL556549 IC50 > 1000.0 nM -