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Assay Detail

CHEMBL3635647

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

Binding
Displacement of [3H]diprenorphine from rat mu-opioid receptor expressed in C6 cell membrane for 1 hr by liquid scintillation counting analysis
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type C6
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mu-type opioid receptor (CHEMBL270)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Further Optimization and Evaluation of Bioavailable, Mixed-Efficacy μ-Opioid Receptor (MOR) Agonists/δ-Opioid Receptor (DOR) Antagonists: Balancing MOR and DOR Affinities.
Harland AA, Yeomans L, Griggs NW, Anand JP, Pogozheva ID, Jutkiewicz EM, Traynor JR, Mosberg HI.
J Med Chem (2015) 58 : 8952 -8969
PubMed 26524472 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 10.13 10.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3634251 1 10.92
CHEMBL3634258 1 10.52
CHEMBL3634250 1 10.52
CHEMBL3634252 1 10.40
CHEMBL3634249 1 10.37
CHEMBL3634248 1 10.35
CHEMBL3634257 1 10.30
CHEMBL3634256 1 10.30
CHEMBL3634254 1 10.22
CHEMBL3634253 1 10.22
CHEMBL2322562 1 10.11
CHEMBL3634247 1 9.89
CHEMBL2322563 1 9.80
CHEMBL2322568 1 9.66
CHEMBL3634255 1 9.41
CHEMBL2322561 1 9.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3634251 Ki = 0.012 nM 10.92
CHEMBL3634258 Ki = 0.03 nM 10.52
CHEMBL3634250 Ki = 0.03 nM 10.52
CHEMBL3634252 Ki = 0.04 nM 10.40
CHEMBL3634249 Ki = 0.043 nM 10.37
CHEMBL3634248 Ki = 0.045 nM 10.35
CHEMBL3634257 Ki = 0.05 nM 10.30
CHEMBL3634256 Ki = 0.05 nM 10.30
CHEMBL3634254 Ki = 0.06 nM 10.22
CHEMBL3634253 Ki = 0.06 nM 10.22
CHEMBL2322562 Ki = 0.078 nM 10.11
CHEMBL3634247 Ki = 0.13 nM 9.89
CHEMBL2322563 Ki = 0.16 nM 9.80
CHEMBL2322568 Ki = 0.22 nM 9.66
CHEMBL3634255 Ki = 0.39 nM 9.41
CHEMBL2322561 Ki = 0.76 nM 9.12