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Assay Detail

CHEMBL5055008

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 assessed as inhibition constant by radioligand binding assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HN9.10
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

C-terminal modified Enkephalin-like tetrapeptides with enhanced affinities at the kappa opioid receptor and monoamine transporters.
Mehr-Un-Nisa, Munawar MA, Rankin D, Hruby VJ, Porreca F, Lee YS.
Bioorg Med Chem (2021) 51 : 116509 -116509
PubMed 34798381 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 8.77 9.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5089012 1 9.49
CHEMBL5094499 1 9.27
CHEMBL5091642 1 9.24
CHEMBL5086370 1 9.24
CHEMBL5078669 1 9.13
CHEMBL5081245 1 8.96
CHEMBL5090705 1 8.92
CHEMBL5083183 1 8.68
CHEMBL2311114 1 8.62
CHEMBL5077561 1 8.44
CHEMBL235743 1 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5089012 Ki = 0.32 nM 9.49
CHEMBL5094499 Ki = 0.54 nM 9.27
CHEMBL5091642 Ki = 0.57 nM 9.24
CHEMBL5086370 Ki = 0.58 nM 9.24
CHEMBL5078669 Ki = 0.74 nM 9.13
CHEMBL5081245 Ki = 1.1 nM 8.96
CHEMBL5090705 Ki = 1.2 nM 8.92
CHEMBL5083183 Ki = 2.1 nM 8.68
CHEMBL2311114 Ki = 2.4 nM 8.62
CHEMBL5077561 Ki = 3.6 nM 8.44
CHEMBL235743 Ki = 300.0 nM 6.52