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Assay Detail

CHEMBL758176

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Binding
Binding affinity towards Opioid receptor delta 1 in guinea pig brain membranes using [3H]naltrindole as radioligand
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Brain
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine abuse: synthesis and opioid receptor binding affinity of N-substituted derivatives of morphinan.
Neumeyer JL, Gu XH, van Vliet LA, DeNunzio NJ, Rusovici DE, Cohen DJ, Negus SS, Mello NK, Bidlack JM.
Bioorg Med Chem Lett (2001) 11 : 2735 -2740
PubMed 11591513 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 29 7.95 9.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL49269 CYCLORPHAN 1 9.66
CHEMBL90667 1 9.27
CHEMBL1790045 1 9.21
CHEMBL419511 1 9.07
CHEMBL301160 BUTORPHAN 1 8.89
CHEMBL93731 1 8.59
CHEMBL327935 1 8.51
CHEMBL327576 1 8.51
CHEMBL279968 ETHYLKETOCYCLAZOCINE 1 8.47
CHEMBL328269 1 8.39
CHEMBL592 LEVORPHANOL 4.0 1 8.38
CHEMBL420995 1 8.25
CHEMBL90463 1 8.25
CHEMBL327309 1 8.16
CHEMBL328236 1 8.07
CHEMBL327885 1 8.00
CHEMBL430833 1 7.64
CHEMBL2115245 1 7.57
CHEMBL314294 1 7.57
CHEMBL327490 1 7.54
CHEMBL2114257 1 7.48
CHEMBL92774 1 7.48
CHEMBL91231 1 7.38
CHEMBL329020 1 7.29
CHEMBL329453 1 7.16
CHEMBL90305 1 6.96
CHEMBL92349 1 6.89
CHEMBL96785 1 6.38
CHEMBL290543 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL49269 CYCLORPHAN Ki = 0.22 nM 9.66
CHEMBL90667 Ki = 0.54 nM 9.27
CHEMBL1790045 Ki = 0.62 nM 9.21
CHEMBL419511 Ki = 0.85 nM 9.07
CHEMBL301160 BUTORPHAN Ki = 1.3 nM 8.89
CHEMBL93731 Ki = 2.6 nM 8.59
CHEMBL327935 Ki = 3.1 nM 8.51
CHEMBL327576 Ki = 3.1 nM 8.51
CHEMBL279968 ETHYLKETOCYCLAZOCINE Ki = 3.4 nM 8.47
CHEMBL328269 Ki = 4.1 nM 8.39
CHEMBL592 LEVORPHANOL Ki = 4.2 nM 8.38
CHEMBL420995 Ki = 5.6 nM 8.25
CHEMBL90463 Ki = 5.6 nM 8.25
CHEMBL327309 Ki = 6.9 nM 8.16
CHEMBL328236 Ki = 8.5 nM 8.07
CHEMBL327885 Ki = 10.0 nM 8.00
CHEMBL430833 Ki = 23.0 nM 7.64
CHEMBL2115245 Ki = 27.0 nM 7.57
CHEMBL314294 Ki = 27.0 nM 7.57
CHEMBL327490 Ki = 29.0 nM 7.54
CHEMBL2114257 Ki = 33.0 nM 7.48
CHEMBL92774 Ki = 33.0 nM 7.48
CHEMBL91231 Ki = 42.0 nM 7.38
CHEMBL329020 Ki = 51.0 nM 7.29
CHEMBL329453 Ki = 69.0 nM 7.16
CHEMBL90305 Ki = 110.0 nM 6.96
CHEMBL92349 Ki = 130.0 nM 6.89
CHEMBL96785 Ki = 420.0 nM 6.38
CHEMBL290543 Ki = 2500.0 nM 5.60