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Assay Detail

CHEMBL1217618

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

Binding
Displacement of [3H]DPDPE from human delta opioid receptor
14
Total Activities
9
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

Biological and conformational evaluation of bifunctional compounds for opioid receptor agonists and neurokinin 1 receptor antagonists possessing two penicillamines.
Yamamoto T, Nair P, Jacobsen NE, Kulkarni V, Davis P, Ma SW, Navratilova E, Yamamura HI, Vanderah TW, Porreca F, Lai J, Hruby VJ.
J Med Chem (2010) 53 : 5491 -5501
PubMed 20617791 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 8.13 9.30
IC50 5 7.36 8.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL31421 1 9.30
CHEMBL595972 1 9.18
CHEMBL507340 2 9.18
CHEMBL1214024 2 8.77
CHEMBL200199 BIPHALIN 1 8.59
CHEMBL1214076 1 7.80
CHEMBL1214025 2 7.42
CHEMBL1214026 2 6.82
CHEMBL1214027 2 6.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL31421 Ki = 0.5 nM 9.30
CHEMBL595972 Ki = 0.66 nM 9.18
CHEMBL507340 Ki = 0.66 nM 9.18
CHEMBL507340 IC50 = 1.445 nM 8.84
CHEMBL1214024 Ki = 1.7 nM 8.77
CHEMBL200199 BIPHALIN Ki = 2.6 nM 8.59
CHEMBL1214024 IC50 = 3.631 nM 8.44
CHEMBL1214076 Ki = 16.0 nM 7.80
CHEMBL1214025 Ki = 38.0 nM 7.42
CHEMBL1214025 IC50 = 72.44 nM 7.14
CHEMBL1214026 Ki = 150.0 nM 6.82
CHEMBL1214026 IC50 = 316.23 nM 6.50
CHEMBL1214027 Ki = 720.0 nM 6.14
CHEMBL1214027 IC50 = 1380.38 nM 5.86