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Assay Detail

CHEMBL1799575

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

Binding
Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellum homogenate by scintillation counting
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Cerebellum
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis of new opioid derivatives with a propellane skeleton and their pharmacology: part 1.
Yamamoto N, Fujii H, Nemoto T, Nakajima R, Momen S, Izumimoto N, Hasebe K, Mochizuki H, Nagase H.
Bioorg Med Chem Lett (2011) 21 : 4104 -4107
PubMed 21641798 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 8.51 10.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1797687 1 10.52
CHEMBL1797689 1 10.42
CHEMBL490665 NALFURAFINE HYDROCHLORIDE 4.0 1 9.64
CHEMBL1797688 1 9.47
CHEMBL560 1 8.44
CHEMBL1797684 1 7.76
CHEMBL1797686 1 7.66
CHEMBL70 MORPHINE 4.0 1 7.33
CHEMBL963 OXYMORPHONE 4.0 1 7.24
CHEMBL1797685 1 6.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1797687 Ki = 0.03 nM 10.52
CHEMBL1797689 Ki = 0.038 nM 10.42
CHEMBL490665 NALFURAFINE HYDROCHLORIDE Ki = 0.23 nM 9.64
CHEMBL1797688 Ki = 0.34 nM 9.47
CHEMBL560 Ki = 3.6 nM 8.44
CHEMBL1797684 Ki = 17.4 nM 7.76
CHEMBL1797686 Ki = 21.7 nM 7.66
CHEMBL70 MORPHINE Ki = 46.9 nM 7.33
CHEMBL963 OXYMORPHONE Ki = 57.6 nM 7.24
CHEMBL1797685 Ki = 255.0 nM 6.59