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Assay Detail

CHEMBL844032

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

Functional
Tested for opioid receptor agonistic activity in guinea pig ileum
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Ileum
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Opioid receptors; mu/kappa/delta (CHEMBL2095181)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

N-terminal alkylated derivatives of [D-Pro10]dynorphin A-(1-11) are highly selective for kappa-opioid receptors.
Choi H, Murray TF, DeLander GE, Caldwell V, Aldrich JV.
J Med Chem (1992) 35 : 4638 -4639
PubMed 1361580 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.80 9.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL384584 1 9.66
CHEMBL425806 1 8.67
CHEMBL290543 1 8.58
CHEMBL265387 1 7.74
CHEMBL413160 1 6.16
CHEMBL407529 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL384584 IC50 = 0.22 nM 9.66
CHEMBL425806 IC50 = 2.16 nM 8.67
CHEMBL290543 IC50 = 2.61 nM 8.58
CHEMBL265387 IC50 = 18.3 nM 7.74
CHEMBL413160 IC50 = 687.0 nM 6.16
CHEMBL407529 IC50 = 990.0 nM 6.00