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Assay Detail

CHEMBL3615232

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

Binding
Displacement of [3H]-diprenorphine from zebrafish mu opioid receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Danio rerio
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mu opioid receptor-like OR2 (CHEMBL3611961)
Type SINGLE PROTEIN
Organism Danio rerio

Publication

Design, synthesis, pharmacological evaluation and molecular dynamics of β-amino acids morphan-derivatives as novel ligands for opioid receptors.
Nieto CT, Gonzalez-Nunez V, Rodríguez RE, Diez D, Garrido NM.
Eur J Med Chem (2015) 101 : 150 -162
PubMed 26134550 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 4.82 6.73

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL70 MORPHINE 4.0 1 6.73
CHEMBL3612241 1 5.08
CHEMBL3612242 1 5.02
CHEMBL3612243 1 4.90
CHEMBL3612240 1 4.50
CHEMBL3612238 1 4.45
CHEMBL3612239 1 4.43
CHEMBL3612245 1 4.12
CHEMBL3612244 1 4.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL70 MORPHINE Ki = 187.4 nM 6.73
CHEMBL3612241 Ki = 8240.0 nM 5.08
CHEMBL3612242 Ki = 9520.0 nM 5.02
CHEMBL3612243 Ki = 12660.0 nM 4.90
CHEMBL3612240 Ki = 32000.0 nM 4.50
CHEMBL3612238 Ki = 35280.0 nM 4.45
CHEMBL3612239 Ki = 36980.0 nM 4.43
CHEMBL3612245 Ki = 75780.0 nM 4.12
CHEMBL3612244 Ki = 78020.0 nM 4.11