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Assay Detail

CHEMBL757516

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

Functional
Agonistic activity for Opioid receptor mu 1 as inhibitory activity towards electrically stimulated guinea pig ileum
10
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Probes for narcotic receptor-mediated phenomena. 21. Novel derivatives of 3-(1,2,3,4,5,11-hexahydro-3-methyl-2,6-methano-6H-azocino[4,5-b]indol- 6-yl)-phenols with improved delta opioid receptor selectivity.
Bertha CM, Ellis M, Flippen-Anderson JL, Porreca F, Rothman RB, Davis P, Xu H, Becketts K, Rice KC.
J Med Chem (1996) 39 : 2081 -2086
PubMed 8642567 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.63 7.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL340032 DADLE 1 7.54
CHEMBL440123 1 6.06
CHEMBL302454 2 5.71
CHEMBL290301 1 5.68
CHEMBL2111529 1 5.63
CHEMBL13470 SNC-80 1 5.26
CHEMBL65348 2 5.17
CHEMBL31421 1 5.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL340032 DADLE IC50 = 28.8 nM 7.54
CHEMBL440123 IC50 = 862.0 nM 6.06
CHEMBL302454 IC50 = 1949.0 nM 5.71
CHEMBL290301 IC50 = 2073.0 nM 5.68
CHEMBL2111529 IC50 = 2345.0 nM 5.63
CHEMBL302454 IC50 = 2893.0 nM 5.54
CHEMBL13470 SNC-80 IC50 = 5457.0 nM 5.26
CHEMBL65348 IC50 = 6767.0 nM 5.17
CHEMBL31421 IC50 = 7300.0 nM 5.14
CHEMBL65348 IC50 = 25901.0 nM 4.59