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Assay Detail

CHEMBL1019877

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

Binding
Displacement of [3H]Naltrindole form human delta opioid receptor expressed in CHO cells
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.
Wentland MP, Lou R, Lu Q, Bu Y, VanAlstine MA, Cohen DJ, Bidlack JM.
Bioorg Med Chem Lett (2009) 19 : 203 -208
PubMed 19027293 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 29 7.25 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL464230 1 8.92
CHEMBL56585 CYCLAZOCINE 2.0 1 8.70
CHEMBL511142 BUPRENORPHINE 4.0 1 8.54
CHEMBL3275494 1 8.30
CHEMBL297428 1 8.28
CHEMBL1237044 TRAMADOL 4.0 1 8.03
CHEMBL982 NALMEFENE 4.0 1 8.03
CHEMBL33986 BUTORPHANOL 4.0 1 7.92
CHEMBL517779 1 7.85
CHEMBL573214 NORBINALTORPHIMINE 1 7.62
CHEMBL140278 1 7.28
CHEMBL517567 1 7.27
CHEMBL468469 1 7.25
CHEMBL19019 NALTREXONE 4.0 1 7.22
CHEMBL518083 1 7.17
CHEMBL415284 NALORPHINE 2.0 1 6.92
CHEMBL80 NALOXONE 4.0 1 6.92
CHEMBL257661 METAZOCINE 2.0 1 6.85
CHEMBL560 1 6.75
CHEMBL461227 1 6.66
CHEMBL511884 1 6.50
CHEMBL56695 1 6.26
CHEMBL506457 1 6.00
CHEMBL464250 1 6.00
CHEMBL443601 1 5.62
CHEMBL1400 O-DESMETHYL TRAMADOL 1 5.54
CHEMBL516552 1 -
CHEMBL442719 1 -
CHEMBL511588 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL464230 Ki = 1.2 nM 8.92
CHEMBL56585 CYCLAZOCINE Ki = 2.0 nM 8.70
CHEMBL511142 BUPRENORPHINE Ki = 2.9 nM 8.54
CHEMBL3275494 Ki = 5.0 nM 8.30
CHEMBL297428 Ki = 5.2 nM 8.28
CHEMBL1237044 TRAMADOL Ki = 9.4 nM 8.03
CHEMBL982 NALMEFENE Ki = 9.3 nM 8.03
CHEMBL33986 BUTORPHANOL Ki = 12.0 nM 7.92
CHEMBL517779 Ki = 14.0 nM 7.85
CHEMBL573214 NORBINALTORPHIMINE Ki = 24.0 nM 7.62
CHEMBL140278 Ki = 53.0 nM 7.28
CHEMBL517567 Ki = 54.0 nM 7.27
CHEMBL468469 Ki = 56.0 nM 7.25
CHEMBL19019 NALTREXONE Ki = 60.0 nM 7.22
CHEMBL518083 Ki = 67.0 nM 7.17
CHEMBL415284 NALORPHINE Ki = 120.0 nM 6.92
CHEMBL80 NALOXONE Ki = 120.0 nM 6.92
CHEMBL257661 METAZOCINE Ki = 140.0 nM 6.85
CHEMBL560 Ki = 180.0 nM 6.75
CHEMBL461227 Ki = 220.0 nM 6.66
CHEMBL511884 Ki = 320.0 nM 6.50
CHEMBL56695 Ki = 550.0 nM 6.26
CHEMBL506457 Ki = 1000.0 nM 6.00
CHEMBL464250 Ki = 1000.0 nM 6.00
CHEMBL443601 Ki = 2400.0 nM 5.62
CHEMBL1400 O-DESMETHYL TRAMADOL Ki = 2900.0 nM 5.54
CHEMBL516552 Ki > 10000.0 nM -
CHEMBL442719 Ki > 10000.0 nM -
CHEMBL511588 Ki > 10000.0 nM -