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Assay Detail

CHEMBL890206

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

Functional
Antagonist activity at human mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay
11
Total Activities
11
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthetic studies of neoclerodane diterpenes from Salvia divinorum: preparation and opioid receptor activity of salvinicin analogues.
Simpson DS, Katavic PL, Lozama A, Harding WW, Parrish D, Deschamps JR, Dersch CM, Partilla JS, Rothman RB, Navarro H, Prisinzano TE.
J Med Chem (2007) 50 : 3596 -3603
PubMed 17580847 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 5.84 6.37
Ke 4 - -
Activity 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL210564 1 6.37
CHEMBL226784 1 5.86
CHEMBL226731 1 5.82
CHEMBL226732 1 5.63
CHEMBL434746 1 5.53
CHEMBL445332 SALVINORIN A 1.0 1 -
CHEMBL390935 1 -
CHEMBL427280 1 -
CHEMBL226785 1 -
CHEMBL226943 SALVIDIVIN A 1 -
CHEMBL440765 U-69593 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL210564 Ki = 430.0 nM 6.37
CHEMBL226784 Ki = 1370.0 nM 5.86
CHEMBL226731 Ki = 1530.0 nM 5.82
CHEMBL226732 Ki = 2320.0 nM 5.63
CHEMBL434746 Ki = 2930.0 nM 5.53
CHEMBL445332 SALVINORIN A Ke - -
CHEMBL390935 Ke - -
CHEMBL427280 Activity - -
CHEMBL226785 Activity - -
CHEMBL226943 SALVIDIVIN A Ke = 760.0 nM -
CHEMBL440765 U-69593 Ke - -