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Assay Detail

CHEMBL3614957

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

Binding
Displacement of [3H]DAMGO from MOR in guinea pig cerebellum membranes
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Cerebellum
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mu-type opioid receptor (CHEMBL4354)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Synthesis of new opioid derivatives with a propellane skeleton and their pharmacologies: Part 5, novel pentacyclic propellane derivatives with a 6-amide side chain.
Nakajima R, Yamamoto N, Hirayama S, Iwai T, Saitoh A, Nagumo Y, Fujii H, Nagase H.
Bioorg Med Chem (2015) 23 : 6271 -6279
PubMed 26346669 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 8.56 9.71

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3613173 1 9.71
CHEMBL3613172 1 9.64
CHEMBL3613171 1 9.63
CHEMBL3613174 1 9.55
CHEMBL3613165 1 9.38
CHEMBL490665 NALFURAFINE HYDROCHLORIDE 4.0 1 9.37
CHEMBL3613164 1 9.29
CHEMBL3613163 1 9.24
CHEMBL3613166 1 8.57
CHEMBL3613168 1 8.36
CHEMBL3613280 1 7.94
CHEMBL3613169 1 7.91
CHEMBL3613167 1 7.86
CHEMBL3613170 1 7.32
CHEMBL3613175 1 7.32
CHEMBL3613282 1 7.25
CHEMBL3613281 1 7.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3613173 Ki = 0.197 nM 9.71
CHEMBL3613172 Ki = 0.229 nM 9.64
CHEMBL3613171 Ki = 0.232 nM 9.63
CHEMBL3613174 Ki = 0.28 nM 9.55
CHEMBL3613165 Ki = 0.42 nM 9.38
CHEMBL490665 NALFURAFINE HYDROCHLORIDE Ki = 0.431 nM 9.37
CHEMBL3613164 Ki = 0.51 nM 9.29
CHEMBL3613163 Ki = 0.57 nM 9.24
CHEMBL3613166 Ki = 2.7 nM 8.57
CHEMBL3613168 Ki = 4.36 nM 8.36
CHEMBL3613280 Ki = 11.5 nM 7.94
CHEMBL3613169 Ki = 12.2 nM 7.91
CHEMBL3613167 Ki = 13.9 nM 7.86
CHEMBL3613170 Ki = 47.6 nM 7.32
CHEMBL3613175 Ki = 47.9 nM 7.32
CHEMBL3613282 Ki = 56.0 nM 7.25
CHEMBL3613281 Ki = 59.6 nM 7.22