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Assay Detail

CHEMBL756181

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Binding
Displacement of [3H]DADLE from Opioid receptor delta 1
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Derivatives of 17-(2-methylallyl)-substituted noroxymorphone: variation of the delta address and its effects on affinity and selectivity for the delta opioid receptor.
Ullrich T, Dersch CM, Rothman RB, Jacobson AE, Rice KC.
Bioorg Med Chem Lett (2001) 11 : 2883 -2885
PubMed 11597422 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 7.22 9.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL567175 NALTRINDOLE 1 9.66
CHEMBL95319 1 8.33
CHEMBL329719 1 8.09
CHEMBL317536 1 7.80
CHEMBL316930 1 7.40
CHEMBL98324 1 7.39
CHEMBL95408 1 7.36
CHEMBL319592 1 6.68
CHEMBL318957 1 6.58
CHEMBL441270 1 6.30
CHEMBL95847 1 5.62
CHEMBL319589 1 5.47
CHEMBL329473 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL567175 NALTRINDOLE Ki = 0.22 nM 9.66
CHEMBL95319 Ki = 4.7 nM 8.33
CHEMBL329719 Ki = 8.2 nM 8.09
CHEMBL317536 Ki = 16.0 nM 7.80
CHEMBL316930 Ki = 40.0 nM 7.40
CHEMBL98324 Ki = 41.0 nM 7.39
CHEMBL95408 Ki = 44.0 nM 7.36
CHEMBL319592 Ki = 210.0 nM 6.68
CHEMBL318957 Ki = 260.0 nM 6.58
CHEMBL441270 Ki = 500.0 nM 6.30
CHEMBL95847 Ki = 2400.0 nM 5.62
CHEMBL319589 Ki = 3400.0 nM 5.47
CHEMBL329473 Ki > 7200.0 nM -