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Assay Detail

CHEMBL4044350

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

Binding
Displacement of [3H]U-69,593 from human kappa opioid receptor expressed in CHO cell membranes by microbeta scintillation counting analysis
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Antitrichomonal activity of δ opioid receptor antagonists, 7-benzylidenenaltrexone derivatives.
Kutsumura N, Koyama Y, Nagumo Y, Nakajima R, Miyata Y, Yamamoto N, Saitoh T, Yoshida N, Iwata S, Nagase H.
Bioorg Med Chem (2017) 25 : 4375 -4383
PubMed 28662966 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 7.17 7.56

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2059382 1 7.56
CHEMBL3632690 1 7.54
CHEMBL252172 BNTX 1 7.48
CHEMBL4105306 1 7.46
CHEMBL4081053 1 7.31
CHEMBL4071324 1 7.15
CHEMBL4070277 1 7.11
CHEMBL2059381 1 6.97
CHEMBL4092119 1 6.90
CHEMBL4061882 1 6.75
CHEMBL4089193 1 6.68
CHEMBL137 METRONIDAZOLE 4.0 1 -
CHEMBL4090365 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2059382 Ki = 27.8 nM 7.56
CHEMBL3632690 Ki = 28.6 nM 7.54
CHEMBL252172 BNTX Ki = 32.8 nM 7.48
CHEMBL4105306 Ki = 35.1 nM 7.46
CHEMBL4081053 Ki = 49.0 nM 7.31
CHEMBL4071324 Ki = 70.4 nM 7.15
CHEMBL4070277 Ki = 78.6 nM 7.11
CHEMBL2059381 Ki = 108.0 nM 6.97
CHEMBL4092119 Ki = 126.0 nM 6.90
CHEMBL4061882 Ki = 176.0 nM 6.75
CHEMBL4089193 Ki = 209.0 nM 6.68
CHEMBL137 METRONIDAZOLE Ki - -
CHEMBL4090365 Ki > 1000.0 nM -