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Assay Detail

CHEMBL861054

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

Binding
Displacement of [3H]deltorphin II from rat delta opioid receptor in brain P2 synaptosomes
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Conversion of the potent delta-opioid agonist H-Dmt-Tic-NH-CH(2)-bid into delta-opioid antagonists by N(1)-benzimidazole alkylation(1).
Balboni G, Guerrini R, Salvadori S, Negri L, Giannini E, Bryant SD, Jinsmaa Y, Lazarus LH.
J Med Chem (2005) 48 : 8112 -8114
PubMed 16366592 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 9.61 10.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL354966 1 10.68
CHEMBL109390 1 10.46
CHEMBL197183 1 9.92
CHEMBL354392 1 9.89
CHEMBL422547 1 9.80
CHEMBL322300 1 9.80
CHEMBL436063 1 9.70
CHEMBL317956 DELTORPHIN C 1 9.62
CHEMBL173884 1 9.44
CHEMBL278789 DERMORPHIN 1 6.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL354966 Ki = 0.021 nM 10.68
CHEMBL109390 Ki = 0.035 nM 10.46
CHEMBL197183 Ki = 0.12 nM 9.92
CHEMBL354392 Ki = 0.13 nM 9.89
CHEMBL422547 Ki = 0.16 nM 9.80
CHEMBL322300 Ki = 0.16 nM 9.80
CHEMBL436063 Ki = 0.2 nM 9.70
CHEMBL317956 DELTORPHIN C Ki = 0.24 nM 9.62
CHEMBL173884 Ki = 0.36 nM 9.44
CHEMBL278789 DERMORPHIN Ki = 178.6 nM 6.75