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Assay Detail

CHEMBL852357

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

Binding
Binding affinity for Mu opioid receptor of rat brain
13
Total Activities
10
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

Rationale, design, and synthesis of novel phenyl imidazoles as opioid receptor agonists for gastrointestinal disorders.
Breslin HJ, Miskowski TA, Rafferty BM, Coutinho SV, Palmer JM, Wallace NH, Schneider CR, Kimball ES, Zhang SP, Li J, Colburn RW, Stone DJ, Martinez RP, He W.
J Med Chem (2004) 47 : 5009 -5020
PubMed 15456245 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 7.92 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL841 LOPERAMIDE 4.0 1 9.80
CHEMBL366311 1 8.82
CHEMBL408680 1 7.94
CHEMBL361033 2 7.68
CHEMBL186527 1 7.64
CHEMBL361274 1 7.26
CHEMBL188558 1 7.16
CHEMBL188565 1 -
CHEMBL440380 2 -
CHEMBL362514 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL841 LOPERAMIDE Ki = 0.16 nM 9.80
CHEMBL366311 Ki = 1.5 nM 8.82
CHEMBL408680 Ki = 11.6 nM 7.94
CHEMBL361033 Ki = 20.7 nM 7.68
CHEMBL186527 Ki = 23.1 nM 7.64
CHEMBL361274 Ki = 54.7 nM 7.26
CHEMBL188558 Ki = 69.0 nM 7.16
CHEMBL361033 Ki = 85.6 nM 7.07
CHEMBL188565 Ki > 100.0 nM -
CHEMBL440380 Ki > 100.0 nM -
CHEMBL362514 Ki > 100.0 nM -
CHEMBL440380 Ki > 100.0 nM -
CHEMBL362514 Ki > 100.0 nM -