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Assay Detail

CHEMBL752204

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Binding
Binding affinity against Opioid receptor kappa 1
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Kappa-type opioid receptor (CHEMBL237)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Molecular docking reveals a novel binding site model for fentanyl at the mu-opioid receptor.
Subramanian G, Paterlini MG, Portoghese PS, Ferguson DM.
J Med Chem (2000) 43 : 381 -391
PubMed 10669565 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.09 7.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL290429 CARFENTANIL 2.0 1 7.37
CHEMBL12391 1 7.24
CHEMBL609147 1 7.20
CHEMBL331883 1 6.91
CHEMBL596 FENTANYL 4.0 1 6.71
CHEMBL435380 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL290429 CARFENTANIL Ki = 43.1 nM 7.37
CHEMBL12391 Ki = 57.4 nM 7.24
CHEMBL609147 Ki = 63.0 nM 7.20
CHEMBL331883 Ki = 122.2 nM 6.91
CHEMBL596 FENTANYL Ki = 196.5 nM 6.71
CHEMBL435380 Ki > 500.0 nM -