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Assay Detail

CHEMBL753666

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

Binding
Binding affinity against opioid receptor delta 1 using [3H]naltrindole as radioligand in guinea pig brain membranes.
37
Total Activities
37
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

10-Ketomorphinan and 3-substituted-3-desoxymorphinan analogues as mixed kappa and micro opioid ligands: synthesis and biological evaluation of their binding affinity at opioid receptors.
Zhang A, Xiong W, Bidlack JM, Hilbert JE, Knapp BI, Wentland MP, Neumeyer JL.
J Med Chem (2004) 47 : 165 -174
PubMed 14695830 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 37 7.03 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL300033 1 9.00
CHEMBL301804 1 9.00
CHEMBL49269 CYCLORPHAN 1 8.72
CHEMBL279968 ETHYLKETOCYCLAZOCINE 1 8.47
CHEMBL433272 1 8.40
CHEMBL592 LEVORPHANOL 4.0 1 8.38
CHEMBL301160 BUTORPHAN 1 8.23
CHEMBL48390 1 8.01
CHEMBL297292 1 7.89
CHEMBL297467 1 7.80
CHEMBL296282 1 7.30
CHEMBL299220 1 6.82
CHEMBL298027 1 6.82
CHEMBL49143 1 6.75
CHEMBL48241 1 6.58
CHEMBL49106 1 6.42
CHEMBL298688 1 6.39
CHEMBL300877 1 6.22
CHEMBL295237 1 6.16
CHEMBL299189 1 6.10
CHEMBL295402 1 5.96
CHEMBL432120 1 5.92
CHEMBL48420 1 5.82
CHEMBL48974 1 5.75
CHEMBL48157 1 5.72
CHEMBL298571 1 5.64
CHEMBL49318 1 5.60
CHEMBL299132 1 -
CHEMBL47488 1 -
CHEMBL296328 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL300033 Ki = 1.0 nM 9.00
CHEMBL301804 Ki = 1.0 nM 9.00
CHEMBL49269 CYCLORPHAN Ki = 1.9 nM 8.72
CHEMBL279968 ETHYLKETOCYCLAZOCINE Ki = 3.4 nM 8.47
CHEMBL433272 Ki = 4.0 nM 8.40
CHEMBL592 LEVORPHANOL Ki = 4.2 nM 8.38
CHEMBL301160 BUTORPHAN Ki = 5.9 nM 8.23
CHEMBL48390 Ki = 9.7 nM 8.01
CHEMBL297292 Ki = 13.0 nM 7.89
CHEMBL297467 Ki = 16.0 nM 7.80
CHEMBL296282 Ki = 50.0 nM 7.30
CHEMBL299220 Ki = 150.0 nM 6.82
CHEMBL298027 Ki = 150.0 nM 6.82
CHEMBL49143 Ki = 180.0 nM 6.75
CHEMBL48241 Ki = 260.0 nM 6.58
CHEMBL49106 Ki = 380.0 nM 6.42
CHEMBL298688 Ki = 410.0 nM 6.39
CHEMBL300877 Ki = 600.0 nM 6.22
CHEMBL295237 Ki = 690.0 nM 6.16
CHEMBL299189 Ki = 800.0 nM 6.10
CHEMBL295402 Ki = 1100.0 nM 5.96
CHEMBL432120 Ki = 1200.0 nM 5.92
CHEMBL48420 Ki = 1500.0 nM 5.82
CHEMBL48974 Ki = 1800.0 nM 5.75
CHEMBL48157 Ki = 1900.0 nM 5.72
CHEMBL298571 Ki = 2300.0 nM 5.64
CHEMBL49318 Ki = 2500.0 nM 5.60
CHEMBL296304 Ki > 1000.0 nM -
CHEMBL300023 Ki > 10000.0 nM -
CHEMBL42055 E-FLUPENTIXOL Ki > 10000.0 nM -
CHEMBL46320 Ki > 10000.0 nM -
CHEMBL298446 Ki > 10000.0 nM -
CHEMBL48816 Ki > 10000.0 nM -
CHEMBL48936 Ki > 10000.0 nM -
CHEMBL296328 Ki > 10000.0 nM -
CHEMBL47488 Ki > 10000.0 nM -
CHEMBL299132 Ki > 10000.0 nM -