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Assay Detail

CHEMBL666300

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

Functional
Agonistic activity towards Opioid receptor delta 1 as inhibitory activity towards electrically stimulated mouse vas deferens
10
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Tissue Vas deferens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Delta-type opioid receptor (CHEMBL3222)
Type SINGLE PROTEIN
Organism Mus musculus

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 6.91 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL13470 SNC-80 1 8.57
CHEMBL31421 1 8.39
CHEMBL2111530 1 7.31
CHEMBL440123 1 6.93
CHEMBL302454 2 6.78
CHEMBL290301 1 6.46
CHEMBL2111529 1 6.41
CHEMBL340032 DADLE 1 6.35
CHEMBL65348 1 5.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL13470 SNC-80 IC50 = 2.7 nM 8.57
CHEMBL31421 IC50 = 4.1 nM 8.39
CHEMBL2111530 IC50 = 49.0 nM 7.31
CHEMBL440123 IC50 = 118.0 nM 6.93
CHEMBL302454 IC50 = 165.0 nM 6.78
CHEMBL302454 IC50 = 270.0 nM 6.57
CHEMBL290301 IC50 = 347.0 nM 6.46
CHEMBL2111529 IC50 = 393.0 nM 6.41
CHEMBL340032 DADLE IC50 = 447.0 nM 6.35
CHEMBL65348 IC50 = 4366.0 nM 5.36