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Assay Detail

CHEMBL754624

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

Binding
Binding affinity to Opioid receptor kappa 1 in guinea pig cortex using [3H]EKC as radioligand
9
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Kappa-type opioid receptor (CHEMBL3952)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Synthesis and analgesic properties of N-substituted trans-4a-aryldecahydroisoquinolines.
Zimmerman DM, Cantrell BE, Swartzendruber JK, Jones ND, Mendelsohn LG, Leander JD, Nickander RC.
J Med Chem (1988) 31 : 555 -560
PubMed 2831363 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 7.35 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL56585 CYCLAZOCINE 2.0 1 8.89
CHEMBL153538 1 8.60
CHEMBL415284 NALORPHINE 2.0 1 7.82
CHEMBL155216 2 7.21
CHEMBL60542 (+)-PENTAZOCINE 1 7.12
CHEMBL359363 1 7.05
CHEMBL70 MORPHINE 4.0 1 6.78
CHEMBL150667 1 6.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL56585 CYCLAZOCINE Ki = 1.3 nM 8.89
CHEMBL153538 Ki = 2.5 nM 8.60
CHEMBL415284 NALORPHINE Ki = 15.0 nM 7.82
CHEMBL155216 Ki = 61.0 nM 7.21
CHEMBL60542 (+)-PENTAZOCINE Ki = 75.0 nM 7.12
CHEMBL359363 Ki = 89.0 nM 7.05
CHEMBL70 MORPHINE Ki = 167.0 nM 6.78
CHEMBL155216 Ki = 433.0 nM 6.36
CHEMBL150667 Ki = 529.0 nM 6.28