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Assay Detail

CHEMBL4731085

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

Binding
Displacement of [3H]-DAMGO from human MOR expressed in HEK293 cells after 60 mins by microbeta counting based assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Mu-type opioid receptor (CHEMBL233)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Exception That Proves the Rule: Investigation of Privileged Stereochemistry in Designing Dopamine DR Bitopic Agonists.
Battiti FO,Newman AH,Bonifazi A
ACS Med Chem Lett (2020) 11 : 1956 -1964
PubMed 33062179 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 4.85 6.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4764883 1 6.13
CHEMBL4791884 1 4.91
CHEMBL4778398 1 4.91
CHEMBL4551160 1 4.77
CHEMBL4744811 1 4.66
CHEMBL70565 1 4.44
CHEMBL97424 1 4.11
CHEMBL4464060 1 -
CHEMBL317493 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4764883 Ki = 739.0 nM 6.13
CHEMBL4791884 Ki = 12300.0 nM 4.91
CHEMBL4778398 Ki = 12400.0 nM 4.91
CHEMBL4551160 Ki = 16900.0 nM 4.77
CHEMBL4744811 Ki = 21900.0 nM 4.66
CHEMBL70565 Ki = 36600.0 nM 4.44
CHEMBL97424 Ki = 77900.0 nM 4.11
CHEMBL4464060 Ki > 100000.0 nM -
CHEMBL317493 Ki - -