Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL2340175

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

Binding
Displacement of [3H]-diprenorphine from human KOR expressed in CHO cells
ChEMBL ↗
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Kappa-type opioid receptor (CHEMBL237) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

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 40 10.12 10.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2338742 — — 1 10.82
CHEMBL2338716 — — 1 10.72
CHEMBL2338717 — — 1 10.70
CHEMBL2338718 — — 1 10.60
CHEMBL2338739 — — 1 10.48
CHEMBL2338728 — — 1 10.39
CHEMBL2338729 — — 1 10.33
CHEMBL2338743 — — 1 10.29
CHEMBL2338750 — — 1 10.29
CHEMBL2338720 — — 1 10.24
CHEMBL2338738 — — 1 10.23
CHEMBL2338745 — — 1 10.22
CHEMBL2338724 — — 1 10.21
CHEMBL2338753 — — 1 10.19
CHEMBL2338721 — — 1 10.17
CHEMBL2338737 — — 1 10.17
CHEMBL511142 BUPRENORPHINE 4.0 1 10.17
CHEMBL2338747 — — 1 10.16
CHEMBL2338746 — — 1 10.13
CHEMBL2338740 — — 1 10.11
CHEMBL2338714 ISOPENTYL ORVINOL M320 — 1 10.09
CHEMBL2338752 — — 1 10.09
CHEMBL2338723 — — 1 10.07
CHEMBL2338722 — — 1 10.07
CHEMBL2338727 — — 1 10.07
CHEMBL2338741 — — 1 10.05
CHEMBL2338744 — — 1 10.04
CHEMBL2338749 — — 1 10.00
CHEMBL2338730 — — 1 9.96
CHEMBL2338756 — — 1 9.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2338742 — Ki = 0.015 nM 10.82
CHEMBL2338716 — Ki = 0.019 nM 10.72
CHEMBL2338717 — Ki = 0.02 nM 10.70
CHEMBL2338718 — Ki = 0.025 nM 10.60
CHEMBL2338739 — Ki = 0.033 nM 10.48
CHEMBL2338728 — Ki = 0.041 nM 10.39
CHEMBL2338729 — Ki = 0.047 nM 10.33
CHEMBL2338743 — Ki = 0.051 nM 10.29
CHEMBL2338750 — Ki = 0.051 nM 10.29
CHEMBL2338720 — Ki = 0.057 nM 10.24
CHEMBL2338738 — Ki = 0.059 nM 10.23
CHEMBL2338745 — Ki = 0.06 nM 10.22
CHEMBL2338724 — Ki = 0.062 nM 10.21
CHEMBL2338753 — Ki = 0.065 nM 10.19
CHEMBL511142 BUPRENORPHINE Ki = 0.067 nM 10.17
CHEMBL2338721 — Ki = 0.067 nM 10.17
CHEMBL2338737 — Ki = 0.067 nM 10.17
CHEMBL2338747 — Ki = 0.069 nM 10.16
CHEMBL2338746 — Ki = 0.074 nM 10.13
CHEMBL2338740 — Ki = 0.078 nM 10.11
CHEMBL2338714 ISOPENTYL ORVINOL M320 Ki = 0.082 nM 10.09
CHEMBL2338752 — Ki = 0.082 nM 10.09
CHEMBL2338723 — Ki = 0.086 nM 10.07
CHEMBL2338722 — Ki = 0.086 nM 10.07
CHEMBL2338727 — Ki = 0.086 nM 10.07
CHEMBL2338741 — Ki = 0.09 nM 10.05
CHEMBL2338744 — Ki = 0.092 nM 10.04
CHEMBL2338749 — Ki = 0.1 nM 10.00
CHEMBL2338730 — Ki = 0.11 nM 9.96
CHEMBL2338756 — Ki = 0.11 nM 9.96
CHEMBL2338726 — Ki = 0.12 nM 9.92
CHEMBL2338748 — Ki = 0.12 nM 9.92
CHEMBL2338725 — Ki = 0.12 nM 9.92
CHEMBL2338731 — Ki = 0.15 nM 9.82
CHEMBL2338732 — Ki = 0.15 nM 9.82
CHEMBL2338734 — Ki = 0.16 nM 9.80
CHEMBL2338719 — Ki = 0.16 nM 9.80
CHEMBL2338751 — Ki = 0.18 nM 9.74
CHEMBL2338733 — Ki = 0.22 nM 9.66
CHEMBL2338715 — Ki = 0.39 nM 9.41