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Assay Detail

CHEMBL757977

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

Binding
Inhibition of [3H]DAGO binding to Opioid receptor mu 1 of rat brain P2 synaptosomes
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 9 — Direct single protein target
Curated By Expert

Target

Mu-type opioid receptor (CHEMBL270)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Potent delta-opioid receptor agonists containing the Dmt-Tic pharmacophore.
Balboni G, Salvadori S, Guerrini R, Negri L, Giannini E, Jinsmaa Y, Bryant SD, Lazarus LH.
J Med Chem (2002) 45 : 5556 -5563
PubMed 12459023 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 7.88 9.63

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL606603 1 9.63
CHEMBL607479 1 9.39
CHEMBL109390 1 9.30
CHEMBL278789 DERMORPHIN 1 8.91
CHEMBL607403 1 8.26
CHEMBL607480 1 8.16
CHEMBL607401 1 7.66
CHEMBL607402 1 7.33
CHEMBL606601 1 7.32
CHEMBL442577 1 7.27
CHEMBL607481 1 7.09
CHEMBL26861 1 6.57
CHEMBL606602 1 5.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL606603 Ki = 0.233 nM 9.63
CHEMBL607479 Ki = 0.411 nM 9.39
CHEMBL109390 Ki = 0.5 nM 9.30
CHEMBL278789 DERMORPHIN Ki = 1.22 nM 8.91
CHEMBL607403 Ki = 5.49 nM 8.26
CHEMBL607480 Ki = 6.92 nM 8.16
CHEMBL607401 Ki = 21.68 nM 7.66
CHEMBL607402 Ki = 47.1 nM 7.33
CHEMBL606601 Ki = 47.5 nM 7.32
CHEMBL442577 Ki = 53.9 nM 7.27
CHEMBL607481 Ki = 80.3 nM 7.09
CHEMBL26861 Ki = 272.0 nM 6.57
CHEMBL606602 Ki = 2565.0 nM 5.59