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Assay Detail

CHEMBL2189108

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

Binding
Displacement of [3H]DSLET from delta opioid receptor in rat brain membranes after 2 hrs
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Subcellular Brain membranes
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Delta-type opioid receptor (CHEMBL269)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Variation of the net charge, lipophilicity, and side chain flexibility in Dmt(1)-DALDA: Effect on Opioid Activity and Biodistribution.
Novoa A, Van Dorpe S, Wynendaele E, Spetea M, Bracke N, Stalmans S, Betti C, Chung NN, Lemieux C, Zuegg J, Cooper MA, Tourwé D, De Spiegeleer B, Schiller PW, Ballet S.
J Med Chem (2012) 55 : 9549 -9561
PubMed 23102273 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 7.67 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1782140 1 9.22
CHEMBL2181191 1 8.50
CHEMBL2181199 1 8.40
CHEMBL2181195 1 8.30
CHEMBL2181193 1 8.13
CHEMBL2181201 1 7.82
CHEMBL2181197 1 7.80
CHEMBL2181194 1 7.41
CHEMBL2181196 1 7.41
CHEMBL2181200 1 7.30
CHEMBL2181192 1 7.25
CHEMBL2181198 1 6.51
CHEMBL2181202 1 5.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1782140 Ki = 0.6 nM 9.22
CHEMBL2181191 Ki = 3.18 nM 8.50
CHEMBL2181199 Ki = 3.98 nM 8.40
CHEMBL2181195 Ki = 5.03 nM 8.30
CHEMBL2181193 Ki = 7.46 nM 8.13
CHEMBL2181201 Ki = 15.2 nM 7.82
CHEMBL2181197 Ki = 16.0 nM 7.80
CHEMBL2181194 Ki = 38.6 nM 7.41
CHEMBL2181196 Ki = 39.2 nM 7.41
CHEMBL2181200 Ki = 50.0 nM 7.30
CHEMBL2181192 Ki = 56.9 nM 7.25
CHEMBL2181198 Ki = 309.0 nM 6.51
CHEMBL2181202 Ki = 2100.0 nM 5.68