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Assay Detail

CHEMBL858889

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

Binding
Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cells
25
Total Activities
25
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 Expert

Target

Mu-type opioid receptor (CHEMBL233)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and preliminary in vitro investigation of bivalent ligands containing homo- and heterodimeric pharmacophores at mu, delta, and kappa opioid receptors.
Peng X, Knapp BI, Bidlack JM, Neumeyer JL.
J Med Chem (2006) 49 : 256 -262
PubMed 16392810 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 8.89 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL199832 1 11.00
CHEMBL49269 CYCLORPHAN 1 10.21
CHEMBL147511 1 10.05
CHEMBL203251 1 9.80
CHEMBL146756 1 9.70
CHEMBL592 LEVORPHANOL 4.0 1 9.68
CHEMBL199931 1 9.66
CHEMBL301160 BUTORPHAN 1 9.64
CHEMBL201271 1 9.47
CHEMBL199827 1 9.36
CHEMBL200881 1 9.19
CHEMBL369919 1 9.17
CHEMBL383320 1 9.15
CHEMBL70 MORPHINE 4.0 1 9.06
CHEMBL193039 1 8.66
CHEMBL381750 1 8.55
CHEMBL372598 1 8.48
CHEMBL49143 1 8.43
CHEMBL201220 1 8.24
CHEMBL201219 1 7.89
CHEMBL372823 1 7.85
CHEMBL381117 1 7.22
CHEMBL200295 1 6.89
CHEMBL201038 1 5.96
CHEMBL1790045 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL199832 Ki = 0.01 nM 11.00
CHEMBL49269 CYCLORPHAN Ki = 0.062 nM 10.21
CHEMBL147511 Ki = 0.09 nM 10.05
CHEMBL203251 Ki = 0.16 nM 9.80
CHEMBL146756 Ki = 0.2 nM 9.70
CHEMBL592 LEVORPHANOL Ki = 0.21 nM 9.68
CHEMBL199931 Ki = 0.22 nM 9.66
CHEMBL301160 BUTORPHAN Ki = 0.23 nM 9.64
CHEMBL201271 Ki = 0.34 nM 9.47
CHEMBL199827 Ki = 0.44 nM 9.36
CHEMBL200881 Ki = 0.65 nM 9.19
CHEMBL369919 Ki = 0.67 nM 9.17
CHEMBL383320 Ki = 0.71 nM 9.15
CHEMBL70 MORPHINE Ki = 0.88 nM 9.06
CHEMBL193039 Ki = 2.2 nM 8.66
CHEMBL381750 Ki = 2.8 nM 8.55
CHEMBL372598 Ki = 3.3 nM 8.48
CHEMBL49143 Ki = 3.7 nM 8.43
CHEMBL201220 Ki = 5.7 nM 8.24
CHEMBL201219 Ki = 13.0 nM 7.89
CHEMBL372823 Ki = 14.0 nM 7.85
CHEMBL381117 Ki = 60.0 nM 7.22
CHEMBL200295 Ki = 130.0 nM 6.89
CHEMBL201038 Ki = 1100.0 nM 5.96
CHEMBL1790045 Ki = 0.003 nM -