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Assay Detail

CHEMBL755486

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

Binding
Inhibition against binding of radioligand [N-allyl-2-3-3H]-naloxone to membrane of baby hamster kidney cells infected with forest virus encoding the cDNAs for rat Opioid receptor kappa 1
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type kidney
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Kappa-type opioid receptor (CHEMBL3614)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

ORL1 receptor ligands: structure-activity relationships of 8-cycloalkyl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-ones.
Röver S, Wichmann J, Jenck F, Adam G, Cesura AM.
Bioorg Med Chem Lett (2000) 10 : 831 -834
PubMed 10782696 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 7.85 9.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL354545 1 9.09
CHEMBL354291 1 8.68
CHEMBL354652 1 8.54
CHEMBL440928 1 8.41
CHEMBL353990 1 8.04
CHEMBL165885 1 7.92
CHEMBL355202 1 7.70
CHEMBL166387 1 7.58
CHEMBL354065 1 7.54
CHEMBL168578 1 7.51
CHEMBL436243 1 7.42
CHEMBL169947 1 7.24
CHEMBL166445 1 7.24
CHEMBL263575 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL354545 Ki = 0.82 nM 9.09
CHEMBL354291 Ki = 2.1 nM 8.68
CHEMBL354652 Ki = 2.9 nM 8.54
CHEMBL440928 Ki = 3.9 nM 8.41
CHEMBL353990 Ki = 9.1 nM 8.04
CHEMBL165885 Ki = 12.0 nM 7.92
CHEMBL355202 Ki = 20.0 nM 7.70
CHEMBL166387 Ki = 26.0 nM 7.58
CHEMBL354065 Ki = 29.0 nM 7.54
CHEMBL168578 Ki = 31.0 nM 7.51
CHEMBL436243 Ki = 38.0 nM 7.42
CHEMBL169947 Ki = 57.0 nM 7.24
CHEMBL166445 Ki = 57.0 nM 7.24
CHEMBL263575 Ki = 100.0 nM 7.00