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Assay Detail

CHEMBL829038

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

Binding
Inhibition of DAMGO (Tyr-[D-Ala]-Gly-[NMe-Phe]-Gly-ol) binding to rat brain mu opioid receptor
17
Total Activities
17
Compounds Tested
1
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

Ligand-based prediction of active conformation by 3D-QSAR flexibility descriptors and their application in 3+3D-QSAR models.
Martinek TA, Otvös F, Dervarics M, Tóth G, Fülöp F.
J Med Chem (2005) 48 : 3239 -3250
PubMed 15857130 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.64 10.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL365983 1 10.85
CHEMBL331325 1 9.68
CHEMBL317264 1 9.51
CHEMBL192372 1 9.46
CHEMBL436039 1 8.78
CHEMBL364703 1 8.38
CHEMBL333357 ENDOMORPHIN 2 1 8.02
CHEMBL423466 1 7.34
CHEMBL163334 1 7.16
CHEMBL362991 MORPHICEPTIN 1 7.10
CHEMBL349738 1 6.98
CHEMBL423794 1 6.97
CHEMBL365581 1 6.78
CHEMBL355141 1 6.60
CHEMBL365984 1 5.79
CHEMBL355367 1 5.31
CHEMBL166108 1 5.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL365983 Ki = 0.014 nM 10.85
CHEMBL331325 Ki = 0.21 nM 9.68
CHEMBL317264 Ki = 0.31 nM 9.51
CHEMBL192372 Ki = 0.35 nM 9.46
CHEMBL436039 Ki = 1.667 nM 8.78
CHEMBL364703 Ki = 4.21 nM 8.38
CHEMBL333357 ENDOMORPHIN 2 Ki = 9.53 nM 8.02
CHEMBL423466 Ki = 45.3 nM 7.34
CHEMBL163334 Ki = 69.5 nM 7.16
CHEMBL362991 MORPHICEPTIN Ki = 80.0 nM 7.10
CHEMBL349738 Ki = 104.0 nM 6.98
CHEMBL423794 Ki = 106.0 nM 6.97
CHEMBL365581 Ki = 166.67 nM 6.78
CHEMBL355141 Ki = 250.0 nM 6.60
CHEMBL365984 Ki = 1610.0 nM 5.79
CHEMBL355367 Ki = 4910.0 nM 5.31
CHEMBL166108 Ki = 7090.0 nM 5.15