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Assay Detail

CHEMBL4430768

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Binding
Displacement of [3H]DAMGO from MOR in HEK293 cells
10
Total Activities
10
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

An LP1 analogue, selective MOR agonist with a peculiar pharmacological profile, used to scrutiny the ligand binding domain.
Ronsisvalle S, Aricò G, Panarello F, Spadaro A, Pasquinucci L, Pappalardo MS, Parenti C, Ronsisvalle N.
Bioorg Med Chem (2016) 24 : 5280 -5290
PubMed 27624520 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 7.66 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4575464 1 9.30
CHEMBL38874 DAMGO 1 9.22
CHEMBL3759092 1 9.08
CHEMBL4442357 1 7.08
CHEMBL4545050 1 7.02
CHEMBL4453773 1 6.80
CHEMBL4562025 1 6.42
CHEMBL4464491 1 6.33
CHEMBL31421 1 -
CHEMBL290543 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4575464 Ki = 0.5 nM 9.30
CHEMBL38874 DAMGO Ki = 0.6 nM 9.22
CHEMBL3759092 Ki = 0.83 nM 9.08
CHEMBL4442357 Ki = 84.0 nM 7.08
CHEMBL4545050 Ki = 96.0 nM 7.02
CHEMBL4453773 Ki = 160.0 nM 6.80
CHEMBL4562025 Ki = 380.0 nM 6.42
CHEMBL4464491 Ki = 470.0 nM 6.33
CHEMBL31421 Ki - -
CHEMBL290543 Ki - -