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Assay Detail

CHEMBL751214

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

Binding
Binding affinity was determined against Opioid receptor mu 1 obtained from guinea pig brain membranes using [3H]DAMGO as radioligand
21
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

8-Aminocyclazocine analogues: synthesis and structure-activity relationships.
Wentland MP, Xu G, Cioffi CL, Ye Y, Duan W, Cohen DJ, Colasurdo AM, Bidlack JM.
Bioorg Med Chem Lett (2000) 10 : 183 -187
PubMed 10673107 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 7.77 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL56585 CYCLAZOCINE 2.0 1 10.00
CHEMBL3085528 1 9.49
CHEMBL301835 2 9.17
CHEMBL2367916 3 8.96
CHEMBL52399 3 8.74
CHEMBL55851 1 8.29
CHEMBL56165 1 8.05
CHEMBL291751 1 7.89
CHEMBL55392 1 7.68
CHEMBL293951 1 7.25
CHEMBL299114 1 7.09
CHEMBL55434 1 6.62
CHEMBL2021605 1 6.44
CHEMBL55248 1 6.19
CHEMBL55948 1 6.11
CHEMBL543563 1 6.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL56585 CYCLAZOCINE Ki = 0.1 nM 10.00
CHEMBL3085528 Ki = 0.32 nM 9.49
CHEMBL301835 Ki = 0.67 nM 9.17
CHEMBL2367916 Ki = 1.1 nM 8.96
CHEMBL2367916 Ki = 1.3 nM 8.89
CHEMBL301835 Ki = 1.5 nM 8.82
CHEMBL52399 Ki = 1.8 nM 8.74
CHEMBL55851 Ki = 5.1 nM 8.29
CHEMBL56165 Ki = 9.0 nM 8.05
CHEMBL52399 Ki = 9.5 nM 8.02
CHEMBL291751 Ki = 13.0 nM 7.89
CHEMBL55392 Ki = 21.0 nM 7.68
CHEMBL2367916 Ki = 46.0 nM 7.34
CHEMBL293951 Ki = 56.0 nM 7.25
CHEMBL299114 Ki = 82.0 nM 7.09
CHEMBL55434 Ki = 240.0 nM 6.62
CHEMBL2021605 Ki = 360.0 nM 6.44
CHEMBL55248 Ki = 650.0 nM 6.19
CHEMBL55948 Ki = 770.0 nM 6.11
CHEMBL52399 Ki = 780.0 nM 6.11
CHEMBL543563 Ki = 950.0 nM 6.02