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Assay Detail

CHEMBL757502

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Binding
Binding affinity of compound evaluated for Opioid receptor delta 1 isolated from rat brain
23
Total Activities
22
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 (CHEMBL269)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

3-(alphaR)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl)-N-alkyl-N-arylbenzamides: potent, non-peptidic agonists of both the micro and delta opioid receptors.
Bishop MJ, Garrido DM, Boswell GE, Collins MA, Harris PA, McNutt RW, O'Neill SJ, Wei K, Chang KJ.
J Med Chem (2003) 46 : 623 -633
PubMed 12570383 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 8.52 9.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL155892 2 9.74
CHEMBL345683 1 8.97
CHEMBL157660 1 8.93
CHEMBL158205 1 8.90
CHEMBL156584 1 8.86
CHEMBL434075 1 8.85
CHEMBL157294 1 8.77
CHEMBL156440 1 8.76
CHEMBL25230 1 8.74
CHEMBL422877 1 8.73
CHEMBL157095 1 8.72
CHEMBL346514 1 8.70
CHEMBL348415 1 8.68
CHEMBL349120 1 8.66
CHEMBL156230 1 8.64
CHEMBL345431 1 8.62
CHEMBL348585 1 8.56
CHEMBL155797 1 8.56
CHEMBL346987 1 8.16
CHEMBL155748 1 8.04
CHEMBL70 MORPHINE 4.0 1 7.05
CHEMBL596 FENTANYL 4.0 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL155892 Ki = 0.18 nM 9.74
CHEMBL345683 Ki = 1.06 nM 8.97
CHEMBL157660 Ki = 1.18 nM 8.93
CHEMBL158205 Ki = 1.26 nM 8.90
CHEMBL156584 Ki = 1.37 nM 8.86
CHEMBL434075 Ki = 1.4 nM 8.85
CHEMBL157294 Ki = 1.69 nM 8.77
CHEMBL156440 Ki = 1.75 nM 8.76
CHEMBL25230 Ki = 1.8 nM 8.74
CHEMBL422877 Ki = 1.88 nM 8.73
CHEMBL157095 Ki = 1.92 nM 8.72
CHEMBL346514 Ki = 2.01 nM 8.70
CHEMBL348415 Ki = 2.1 nM 8.68
CHEMBL349120 Ki = 2.17 nM 8.66
CHEMBL156230 Ki = 2.31 nM 8.64
CHEMBL345431 Ki = 2.41 nM 8.62
CHEMBL348585 Ki = 2.75 nM 8.56
CHEMBL155797 Ki = 2.73 nM 8.56
CHEMBL346987 Ki = 6.95 nM 8.16
CHEMBL155748 Ki = 9.2 nM 8.04
CHEMBL155892 Ki = 11.39 nM 7.94
CHEMBL70 MORPHINE Ki = 90.0 nM 7.05
CHEMBL596 FENTANYL Ki = 400.0 nM 6.40