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Assay Detail

CHEMBL911094

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

Binding
Displacement of [3H]DAMGO from rat mu opioid receptor expressed in HN9.10 cells
16
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Partial retro-inverso, retro, and inverso modifications of hydrazide linked bifunctional peptides for opioid and cholecystokinin (CCK) receptors.
Lee YS, Agnes RS, Davis P, Ma SW, Badghisi H, Lai J, Porreca F, Hruby VJ.
J Med Chem (2007) 50 : 165 -168
PubMed 17201419 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.96 9.30
IC50 8 7.60 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL407198 2 9.30
CHEMBL375359 2 8.52
CHEMBL218651 2 8.47
CHEMBL386212 2 7.89
CHEMBL414087 2 7.51
CHEMBL386186 2 7.47
CHEMBL217957 2 7.28
CHEMBL218600 2 7.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL407198 Ki = 0.5 nM 9.30
CHEMBL407198 IC50 = 1.202 nM 8.92
CHEMBL375359 Ki = 3.0 nM 8.52
CHEMBL218651 Ki = 3.4 nM 8.47
CHEMBL375359 IC50 = 6.918 nM 8.16
CHEMBL218651 IC50 = 7.943 nM 8.10
CHEMBL386212 Ki = 13.0 nM 7.89
CHEMBL386212 IC50 = 28.84 nM 7.54
CHEMBL414087 Ki = 31.0 nM 7.51
CHEMBL386186 Ki = 34.0 nM 7.47
CHEMBL217957 Ki = 52.0 nM 7.28
CHEMBL218600 Ki = 56.0 nM 7.25
CHEMBL414087 IC50 = 64.57 nM 7.19
CHEMBL386186 IC50 = 79.43 nM 7.10
CHEMBL217957 IC50 = 120.23 nM 6.92
CHEMBL218600 IC50 = 131.83 nM 6.88