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Assay Detail

CHEMBL684127

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

Functional
Functional antagonism was obtained by the ability of compound to inhibit stimulation of [35S]GTP gamma S binding produced by selective agonists SNC-80 in guinea pig caudate membranes
5
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Confidence 1 — Organism
Curated By Intermediate

Target

Cavia porcellus (CHEMBL369)
Type ORGANISM
Organism Cavia porcellus

Publication

Importance of phenolic address groups in opioid kappa receptor selective antagonists.
Thomas JB, Fix SE, Rothman RB, Mascarella SW, Dersch CM, Cantrell BE, Zimmerman DM, Carroll FI.
J Med Chem (2004) 47 : 1070 -1073
PubMed 14761209 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 7.00 7.99

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL573214 NORBINALTORPHIMINE 2 7.99
CHEMBL10872 1 6.67
CHEMBL10986 1 6.35
CHEMBL415247 JDTIC 1.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL573214 NORBINALTORPHIMINE Ki = 10.2 nM 7.99
CHEMBL10872 Ki = 213.0 nM 6.67
CHEMBL10986 Ki = 450.0 nM 6.35
CHEMBL415247 JDTIC Ki > 300.0 nM -
CHEMBL573214 NORBINALTORPHIMINE Ki > 300.0 nM -