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Assay Detail

CHEMBL890203

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

Binding
Displacement of [125I]IOXY from human kappa opioid receptor expressed in CHO cells
19
Total Activities
19
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 Expert

Target

Kappa-type opioid receptor (CHEMBL237)
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 19 6.80 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL390935 1 8.52
CHEMBL427280 1 8.43
CHEMBL364058 1 7.85
CHEMBL226784 1 7.60
CHEMBL2113278 1 7.40
CHEMBL210564 1 7.25
CHEMBL226785 1 6.90
CHEMBL434746 1 6.75
CHEMBL424698 SALVINORIN B 1 6.55
CHEMBL387772 1 6.52
CHEMBL560302 SALVINICIN A 1 6.41
CHEMBL226732 1 6.38
CHEMBL387557 1 6.36
CHEMBL226677 1 6.04
CHEMBL226731 1 6.00
CHEMBL226730 1 5.47
CHEMBL2113369 SALVINICIN B 1 5.15
CHEMBL226727 1 -
CHEMBL227104 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL390935 Ki = 3.0 nM 8.52
CHEMBL427280 Ki = 3.7 nM 8.43
CHEMBL364058 Ki = 14.0 nM 7.85
CHEMBL226784 Ki = 25.0 nM 7.60
CHEMBL2113278 Ki = 40.0 nM 7.40
CHEMBL210564 Ki = 56.0 nM 7.25
CHEMBL226785 Ki = 125.0 nM 6.90
CHEMBL434746 Ki = 180.0 nM 6.75
CHEMBL424698 SALVINORIN B Ki = 280.0 nM 6.55
CHEMBL387772 Ki = 300.0 nM 6.52
CHEMBL560302 SALVINICIN A Ki = 390.0 nM 6.41
CHEMBL226732 Ki = 420.0 nM 6.38
CHEMBL387557 Ki = 440.0 nM 6.36
CHEMBL226677 Ki = 910.0 nM 6.04
CHEMBL226731 Ki = 990.0 nM 6.00
CHEMBL226730 Ki = 3400.0 nM 5.47
CHEMBL2113369 SALVINICIN B Ki = 7020.0 nM 5.15
CHEMBL226727 Ki > 10000.0 nM -
CHEMBL227104 Ki > 10000.0 nM -