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Assay Detail

CHEMBL757333

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

Binding
Affinity for opioid receptor delta sites
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

(1S)-1-(aminomethyl)-2-(arylacetyl)-1,2,3,4-tetrahydroisoquinoline and heterocycle-condensed tetrahydropyridine derivatives: members of a novel class of very potent kappa opioid analgesics.
Vecchietti V, Clarke GD, Colle R, Giardina G, Petrone G, Sbacchi M.
J Med Chem (1991) 34 : 2624 -2633
PubMed 1652025 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 6.51 6.95

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2114223 1 6.95
CHEMBL89307 1 6.82
CHEMBL88168 1 6.44
CHEMBL70 MORPHINE 4.0 1 6.34
CHEMBL71294 1 6.00
CHEMBL87010 1 -
CHEMBL330449 1 -
CHEMBL290543 1 -
CHEMBL329114 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2114223 Ki = 113.0 nM 6.95
CHEMBL89307 Ki = 153.0 nM 6.82
CHEMBL88168 Ki = 362.0 nM 6.44
CHEMBL70 MORPHINE Ki = 456.0 nM 6.34
CHEMBL71294 Ki = 1000.0 nM 6.00
CHEMBL87010 Ki > 1000.0 nM -
CHEMBL330449 Ki > 1000.0 nM -
CHEMBL290543 Ki > 10000.0 nM -
CHEMBL329114 Ki > 1000.0 nM -