Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL2051428

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 HEK-293 cells by scintillation counting
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

NOpiates: Novel Dual Action Neuronal Nitric Oxide Synthase Inhibitors with μ-Opioid Agonist Activity.
Renton P, Green B, Maddaford S, Rakhit S, Andrews JS.
ACS Med Chem Lett (2012) 3 : 227 -231
PubMed 24900459 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 7.60 9.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3215669 1 9.37
CHEMBL70 MORPHINE 4.0 1 8.66
CHEMBL3216999 1 8.27
CHEMBL3215668 1 8.12
CHEMBL3217001 1 8.11
CHEMBL3217210 1 7.92
CHEMBL3215667 1 7.57
CHEMBL3216560 1 7.38
CHEMBL3217211 1 7.32
CHEMBL3217000 1 6.96
CHEMBL1201776 TAPENTADOL 4.0 1 6.80
CHEMBL3216780 1 6.77
CHEMBL3215885 1 5.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3215669 Ki = 0.43 nM 9.37
CHEMBL70 MORPHINE Ki = 2.2 nM 8.66
CHEMBL3216999 Ki = 5.41 nM 8.27
CHEMBL3215668 Ki = 7.5 nM 8.12
CHEMBL3217001 Ki = 7.8 nM 8.11
CHEMBL3217210 Ki = 12.0 nM 7.92
CHEMBL3215667 Ki = 27.0 nM 7.57
CHEMBL3216560 Ki = 42.0 nM 7.38
CHEMBL3217211 Ki = 48.0 nM 7.32
CHEMBL3217000 Ki = 110.0 nM 6.96
CHEMBL1201776 TAPENTADOL Ki = 160.0 nM 6.80
CHEMBL3216780 Ki = 170.0 nM 6.77
CHEMBL3215885 Ki = 2900.0 nM 5.54