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Assay Detail

CHEMBL1055013

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

Binding
Displacement of [3H]DAMGO from mu opioid receptor in Sprague-Dawley rat brain P2 synaptosomal membrane
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Influence of the side chain next to C-terminal benzimidazole in opioid pseudopeptides containing the Dmt-Tic pharmacophore.
Balboni G, Trapella C, Sasaki Y, Ambo A, Marczak ED, Lazarus LH, Salvadori S.
J Med Chem (2009) 52 : 5556 -5559
PubMed 19642675 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 9.39 10.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL557346 1 10.11
CHEMBL564083 1 10.02
CHEMBL539386 1 9.92
CHEMBL538457 1 9.89
CHEMBL553461 1 9.89
CHEMBL554838 1 9.89
CHEMBL553221 1 9.85
CHEMBL538456 1 9.80
CHEMBL538699 1 9.64
CHEMBL556063 1 9.60
CHEMBL538384 1 9.52
CHEMBL559088 1 9.43
CHEMBL551937 1 9.39
CHEMBL556230 1 9.30
CHEMBL563304 1 8.88
CHEMBL540724 1 8.84
CHEMBL554625 1 7.70
CHEMBL540972 1 7.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL557346 Ki = 0.077 nM 10.11
CHEMBL564083 Ki = 0.095 nM 10.02
CHEMBL539386 Ki = 0.12 nM 9.92
CHEMBL538457 Ki = 0.13 nM 9.89
CHEMBL553461 Ki = 0.13 nM 9.89
CHEMBL554838 Ki = 0.13 nM 9.89
CHEMBL553221 Ki = 0.143 nM 9.85
CHEMBL538456 Ki = 0.16 nM 9.80
CHEMBL538699 Ki = 0.23 nM 9.64
CHEMBL556063 Ki = 0.25 nM 9.60
CHEMBL538384 Ki = 0.3 nM 9.52
CHEMBL559088 Ki = 0.37 nM 9.43
CHEMBL551937 Ki = 0.411 nM 9.39
CHEMBL556230 Ki = 0.5 nM 9.30
CHEMBL563304 Ki = 1.33 nM 8.88
CHEMBL540724 Ki = 1.45 nM 8.84
CHEMBL554625 Ki = 20.2 nM 7.70
CHEMBL540972 Ki = 53.9 nM 7.27