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Assay Detail

CHEMBL3367579

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

Binding
Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction
4
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

'Carba'-carfentanil (trans isomer): a μ opioid receptor (MOR) partial agonist with a distinct binding mode.
Weltrowska G, Lemieux C, Chung NN, Guo JJ, Wilkes BC, Schiller PW.
Bioorg Med Chem (2014) 22 : 4581 -4586
PubMed 25129170 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ke 2 - -
IC50 2 9.13 10.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL290429 CARFENTANIL 2.0 1 10.72
CHEMBL70 MORPHINE 4.0 1 7.53
CHEMBL3325853 1 -
CHEMBL1091995 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL290429 CARFENTANIL IC50 = 0.019 nM 10.72
CHEMBL70 MORPHINE IC50 = 29.3 nM 7.53
CHEMBL3325853 Ke = 4050.0 nM -
CHEMBL1091995 Ke = 1240.0 nM -