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Assay Detail

CHEMBL1799577

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

Binding
Displacement of [3H]DAMGO from mu opioid receptor in guinea pig forebrain 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 Brain
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mu-type opioid receptor (CHEMBL4354)
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 8.80 9.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1797689 1 9.85
CHEMBL1797688 1 9.80
CHEMBL1797687 1 9.70
CHEMBL963 OXYMORPHONE 4.0 1 9.27
CHEMBL490665 NALFURAFINE HYDROCHLORIDE 4.0 1 9.24
CHEMBL70 MORPHINE 4.0 1 8.96
CHEMBL1797685 1 8.44
CHEMBL560 1 8.34
CHEMBL1797684 1 7.24
CHEMBL1797686 1 7.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1797689 Ki = 0.14 nM 9.85
CHEMBL1797688 Ki = 0.16 nM 9.80
CHEMBL1797687 Ki = 0.2 nM 9.70
CHEMBL963 OXYMORPHONE Ki = 0.54 nM 9.27
CHEMBL490665 NALFURAFINE HYDROCHLORIDE Ki = 0.58 nM 9.24
CHEMBL70 MORPHINE Ki = 1.1 nM 8.96
CHEMBL1797685 Ki = 3.6 nM 8.44
CHEMBL560 Ki = 4.6 nM 8.34
CHEMBL1797684 Ki = 58.2 nM 7.24
CHEMBL1797686 Ki = 77.7 nM 7.11