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Assay Detail

CHEMBL754468

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

Binding
In vitro binding affinity to Opioid receptor delta 1 in rat brain membranes by [3H]DADLE (Tyr-D-Ala-Gly-Phe-D-Leu) displacement.
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Subcellular Brain membranes
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Probes for narcotic receptor mediated phenomena. 26. Synthesis and biological evaluation of diarylmethylpiperazines and diarylmethylpiperidines as novel, nonpeptidic delta opioid receptor ligands.
Zhang X, Rice KC, Calderon SN, Kayakiri H, Smith L, Coop A, Jacobson AE, Rothman RB, Davis P, Dersch CM, Porreca F.
J Med Chem (1999) 42 : 5455 -5463
PubMed 10639287 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 7.66 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL153648 1 9.30
CHEMBL150609 1 8.83
CHEMBL13470 SNC-80 1 8.40
CHEMBL338980 1 8.31
CHEMBL542267 1 8.30
CHEMBL544641 1 7.98
CHEMBL545335 1 7.92
CHEMBL544638 1 7.70
CHEMBL346625 1 7.57
CHEMBL555570 1 7.57
CHEMBL555571 1 7.37
CHEMBL150430 1 7.36
CHEMBL552849 1 6.61
CHEMBL150785 1 6.59
CHEMBL541349 1 6.48
CHEMBL153183 1 6.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL153648 Ki = 0.5 nM 9.30
CHEMBL150609 Ki = 1.48 nM 8.83
CHEMBL13470 SNC-80 Ki = 4.0 nM 8.40
CHEMBL338980 Ki = 4.85 nM 8.31
CHEMBL542267 Ki = 5.0 nM 8.30
CHEMBL544641 Ki = 10.5 nM 7.98
CHEMBL545335 Ki = 12.0 nM 7.92
CHEMBL544638 Ki = 20.0 nM 7.70
CHEMBL346625 Ki = 27.0 nM 7.57
CHEMBL555570 Ki = 27.0 nM 7.57
CHEMBL555571 Ki = 43.2 nM 7.37
CHEMBL150430 Ki = 44.2 nM 7.36
CHEMBL552849 Ki = 248.0 nM 6.61
CHEMBL150785 Ki = 258.0 nM 6.59
CHEMBL541349 Ki = 328.0 nM 6.48
CHEMBL153183 Ki = 622.0 nM 6.21