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Assay Detail

CHEMBL1657628

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

Binding
Displacement of [3H]DPDPE from human delta opioid receptor expressed in mouse HN9.10 cells
26
Total Activities
13
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Delta-type opioid receptor (CHEMBL236)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of potent μ and δ opioid agonists with high lipophilicity.
Lee YS, Kulkarani V, Cowell SM, Ma SW, Davis P, Hanlon KE, Vanderah TW, Lai J, Porreca F, Vardanyan R, Hruby VJ.
J Med Chem (2011) 54 : 382 -386
PubMed 21128594 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 8.82 10.19
Ki 13 9.16 10.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1649946 2 10.52
CHEMBL1649941 2 10.10
CHEMBL1649948 2 9.96
CHEMBL1649943 2 9.85
CHEMBL1649938 2 9.74
CHEMBL392185 2 9.44
CHEMBL1649942 2 9.40
CHEMBL1649947 2 9.32
CHEMBL1649939 2 8.96
CHEMBL1649945 2 8.80
CHEMBL1649940 2 8.77
CHEMBL1649944 2 7.72
CHEMBL235743 2 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1649946 Ki = 0.03 nM 10.52
CHEMBL1649946 IC50 = 0.06457 nM 10.19
CHEMBL1649941 Ki = 0.08 nM 10.10
CHEMBL1649948 Ki = 0.11 nM 9.96
CHEMBL1649943 Ki = 0.14 nM 9.85
CHEMBL1649938 Ki = 0.18 nM 9.74
CHEMBL1649941 IC50 = 0.1862 nM 9.73
CHEMBL1649948 IC50 = 0.257 nM 9.59
CHEMBL1649943 IC50 = 0.302 nM 9.52
CHEMBL392185 Ki = 0.36 nM 9.44
CHEMBL1649938 IC50 = 0.3802 nM 9.42
CHEMBL1649942 Ki = 0.4 nM 9.40
CHEMBL1649947 Ki = 0.48 nM 9.32
CHEMBL392185 IC50 = 0.7943 nM 9.10
CHEMBL1649942 IC50 = 0.8511 nM 9.07
CHEMBL1649947 IC50 = 1.072 nM 8.97
CHEMBL1649939 Ki = 1.1 nM 8.96
CHEMBL1649945 Ki = 1.6 nM 8.80
CHEMBL1649940 Ki = 1.7 nM 8.77
CHEMBL1649939 IC50 = 2.399 nM 8.62
CHEMBL1649945 IC50 = 3.236 nM 8.49
CHEMBL1649940 IC50 = 3.631 nM 8.44
CHEMBL1649944 Ki = 19.0 nM 7.72
CHEMBL1649944 IC50 = 39.81 nM 7.40
CHEMBL235743 Ki = 300.0 nM 6.52
CHEMBL235743 IC50 = 724.44 nM 6.14