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Assay Detail

CHEMBL2340176

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

Binding
Displacement of [3H]-diprenorphine from rat recombinant MOR expressed in rat C6 cells after 2 hrs
ChEMBL ↗
39
Total Activities
39
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

Orvinols with mixed kappa/mu opioid receptor agonist activity.
Greedy BM, Bradbury F, Thomas MP, Grivas K, Cami-Kobeci G, Archambeau A, Bosse K, Clark MJ, Aceto M, Lewis JW, Traynor JR, Husbands SM.
J Med Chem (2013) 56 : 3207 -3216
PubMed 23438330 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 39 9.72 10.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2338718 — — 1 10.54
CHEMBL2338729 — — 1 10.54
CHEMBL2338728 — — 1 10.52
CHEMBL2338739 — — 1 10.51
CHEMBL2338717 — — 1 10.42
CHEMBL2338742 — — 1 10.37
CHEMBL2338738 — — 1 10.27
CHEMBL2338716 — — 1 10.22
CHEMBL2338756 — — 1 10.04
CHEMBL2338721 — — 1 9.92
CHEMBL2338743 — — 1 9.82
CHEMBL2338752 — — 1 9.82
CHEMBL2338741 — — 1 9.82
CHEMBL2338732 — — 1 9.74
CHEMBL2338714 ISOPENTYL ORVINOL M320 — 1 9.74
CHEMBL2338730 — — 1 9.72
CHEMBL511142 BUPRENORPHINE 4.0 1 9.72
CHEMBL2338744 — — 1 9.70
CHEMBL2338749 — — 1 9.68
CHEMBL2338731 — — 1 9.68
CHEMBL2338746 — — 1 9.68
CHEMBL2338745 — — 1 9.66
CHEMBL2338727 — — 1 9.64
CHEMBL2338726 — — 1 9.57
CHEMBL2338747 — — 1 9.54
CHEMBL2338740 — — 1 9.51
CHEMBL2338753 — — 1 9.49
CHEMBL2338737 — — 1 9.48
CHEMBL2338750 — — 1 9.47
CHEMBL2338723 — — 1 9.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2338718 — Ki = 0.029 nM 10.54
CHEMBL2338729 — Ki = 0.029 nM 10.54
CHEMBL2338728 — Ki = 0.03 nM 10.52
CHEMBL2338739 — Ki = 0.031 nM 10.51
CHEMBL2338717 — Ki = 0.038 nM 10.42
CHEMBL2338742 — Ki = 0.043 nM 10.37
CHEMBL2338738 — Ki = 0.054 nM 10.27
CHEMBL2338716 — Ki = 0.06 nM 10.22
CHEMBL2338756 — Ki = 0.091 nM 10.04
CHEMBL2338721 — Ki = 0.12 nM 9.92
CHEMBL2338752 — Ki = 0.15 nM 9.82
CHEMBL2338741 — Ki = 0.15 nM 9.82
CHEMBL2338743 — Ki = 0.15 nM 9.82
CHEMBL2338732 — Ki = 0.18 nM 9.74
CHEMBL2338714 ISOPENTYL ORVINOL M320 Ki = 0.18 nM 9.74
CHEMBL2338730 — Ki = 0.19 nM 9.72
CHEMBL511142 BUPRENORPHINE Ki = 0.19 nM 9.72
CHEMBL2338744 — Ki = 0.2 nM 9.70
CHEMBL2338746 — Ki = 0.21 nM 9.68
CHEMBL2338731 — Ki = 0.21 nM 9.68
CHEMBL2338749 — Ki = 0.21 nM 9.68
CHEMBL2338745 — Ki = 0.22 nM 9.66
CHEMBL2338727 — Ki = 0.23 nM 9.64
CHEMBL2338726 — Ki = 0.27 nM 9.57
CHEMBL2338747 — Ki = 0.29 nM 9.54
CHEMBL2338740 — Ki = 0.31 nM 9.51
CHEMBL2338753 — Ki = 0.32 nM 9.49
CHEMBL2338737 — Ki = 0.33 nM 9.48
CHEMBL2338750 — Ki = 0.34 nM 9.47
CHEMBL2338723 — Ki = 0.36 nM 9.44
CHEMBL2338733 — Ki = 0.37 nM 9.43
CHEMBL2338725 — Ki = 0.41 nM 9.39
CHEMBL2338734 — Ki = 0.47 nM 9.33
CHEMBL2338724 — Ki = 0.49 nM 9.31
CHEMBL2338748 — Ki = 0.62 nM 9.21
CHEMBL2338720 — Ki = 0.68 nM 9.17
CHEMBL2338719 — Ki = 0.88 nM 9.06
CHEMBL2338751 — Ki = 1.0 nM 9.00
CHEMBL2338722 — Ki = 1.0 nM 9.00