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Assay Detail

CHEMBL923550

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

Binding
Displacement of [125I]IOXY from human recombinant mu opioid receptor expressed in CHO cells
24
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Herkinorin analogues with differential beta-arrestin-2 interactions.
Tidgewell K, Groer CE, Harding WW, Lozama A, Schmidt M, Marquam A, Hiemstra J, Partilla JS, Dersch CM, Rothman RB, Bohn LM, Prisinzano TE.
J Med Chem (2008) 51 : 2421 -2431
PubMed 18380425 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 24 6.92 8.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL259658 1 8.51
CHEMBL260121 1 8.00
CHEMBL259299 1 8.00
CHEMBL264967 1 8.00
CHEMBL410436 1 8.00
CHEMBL363324 HERKINORIN 1 7.92
CHEMBL260485 1 7.52
CHEMBL260286 1 7.16
CHEMBL407155 1 6.96
CHEMBL261024 1 6.96
CHEMBL261807 1 6.75
CHEMBL265195 1 6.58
CHEMBL262346 1 6.54
CHEMBL258754 1 5.99
CHEMBL429685 1 5.79
CHEMBL213155 1 5.38
CHEMBL445332 SALVINORIN A 1.0 2 5.36
CHEMBL408775 1 5.12
CHEMBL424698 SALVINORIN B 1 -
CHEMBL260809 1 -
CHEMBL408900 1 -
CHEMBL409414 1 -
CHEMBL438561 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL259658 Ki = 3.1 nM 8.51
CHEMBL260121 Ki = 10.0 nM 8.00
CHEMBL259299 Ki = 10.0 nM 8.00
CHEMBL264967 Ki = 10.0 nM 8.00
CHEMBL410436 Ki = 10.0 nM 8.00
CHEMBL363324 HERKINORIN Ki = 12.0 nM 7.92
CHEMBL260485 Ki = 30.0 nM 7.52
CHEMBL260286 Ki = 70.0 nM 7.16
CHEMBL407155 Ki = 110.0 nM 6.96
CHEMBL261024 Ki = 110.0 nM 6.96
CHEMBL261807 Ki = 180.0 nM 6.75
CHEMBL265195 Ki = 260.0 nM 6.58
CHEMBL262346 Ki = 290.0 nM 6.54
CHEMBL258754 Ki = 1030.0 nM 5.99
CHEMBL429685 Ki = 1640.0 nM 5.79
CHEMBL213155 Ki = 4180.0 nM 5.38
CHEMBL445332 SALVINORIN A Ki = 4370.0 nM 5.36
CHEMBL408775 Ki = 7550.0 nM 5.12
CHEMBL445332 SALVINORIN A Ki > 1000.0 nM -
CHEMBL424698 SALVINORIN B Ki > 10000.0 nM -
CHEMBL260809 Ki > 10000.0 nM -
CHEMBL408900 Ki > 10000.0 nM -
CHEMBL409414 Ki > 10000.0 nM -
CHEMBL438561 Ki > 10000.0 nM -