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Assay Detail

CHEMBL752033

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

Functional
Antagonist activity against Opioid receptor mu 1 iin a guinea pig ileum assay
5
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Ileum
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Mu-type opioid receptor (CHEMBL4354)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Evolution of the Dmt-Tic pharmacophore: N-terminal methylated derivatives with extraordinary delta opioid antagonist activity.
Salvadori S, Balboni G, Guerrini R, Tomatis R, Bianchi C, Bryant SD, Cooper PS, Lazarus LH.
J Med Chem (1997) 40 : 3100 -3108
PubMed 9301674 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 4 5.97 6.30
pA2 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL106853 1 6.30
CHEMBL104436 1 5.80
CHEMBL2370386 1 5.80
CHEMBL107386 1 -
CHEMBL567175 NALTRINDOLE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL106853 Kd = 501.19 nM 6.30
CHEMBL104436 Kd = 1584.89 nM 5.80
CHEMBL2370386 Kd = 1584.89 nM 5.80
CHEMBL107386 Kd = 100000000.0 nM -
CHEMBL567175 NALTRINDOLE pA2 = 7.3 nM -