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Assay Detail

CHEMBL758175

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

Binding
Binding affinity towards Opioid receptor delta 1 from guinea pig brain using [3H]naltrindole as radioligand
52
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Delta-type opioid receptor (CHEMBL236)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Syntheses and opioid receptor binding affinities of 8-amino-2,6-methano-3-benzazocines.
Wentland MP, Ye Y, Cioffi CL, Lou R, Zhou Q, Xu G, Duan W, Dehnhardt CM, Sun X, Cohen DJ, Bidlack JM.
J Med Chem (2003) 46 : 838 -849
PubMed 12593663 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 52 7.13 9.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL56585 CYCLAZOCINE 2.0 2 9.24
CHEMBL279968 ETHYLKETOCYCLAZOCINE 3 8.96
CHEMBL2367604 1 8.60
CHEMBL2367916 3 8.28
CHEMBL355403 1 8.21
CHEMBL169346 3 8.12
CHEMBL169536 1 8.08
CHEMBL422567 1 7.96
CHEMBL2367918 1 7.92
CHEMBL169345 1 7.89
CHEMBL55851 1 7.72
CHEMBL354172 1 7.70
CHEMBL422563 1 7.68
CHEMBL169030 1 7.58
CHEMBL168392 1 7.54
CHEMBL422560 1 7.54
CHEMBL2368318 1 7.46
CHEMBL352965 1 7.43
CHEMBL301835 2 7.27
CHEMBL352827 1 7.21
CHEMBL440196 1 7.12
CHEMBL168913 1 7.10
CHEMBL353303 1 7.01
CHEMBL353938 1 7.00
CHEMBL52399 1 6.96
CHEMBL56165 1 6.80
CHEMBL352365 1 6.77
CHEMBL169670 1 6.75
CHEMBL354322 1 6.66
CHEMBL168409 1 6.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL56585 CYCLAZOCINE Ki = 0.58 nM 9.24
CHEMBL56585 CYCLAZOCINE Ki = 1.1 nM 8.96
CHEMBL279968 ETHYLKETOCYCLAZOCINE Ki = 1.1 nM 8.96
CHEMBL2367604 Ki = 2.5 nM 8.60
CHEMBL279968 ETHYLKETOCYCLAZOCINE Ki = 3.4 nM 8.47
CHEMBL2367916 Ki = 5.2 nM 8.28
CHEMBL355403 Ki = 6.2 nM 8.21
CHEMBL169346 Ki = 7.6 nM 8.12
CHEMBL169536 Ki = 8.3 nM 8.08
CHEMBL2367916 Ki = 9.4 nM 8.03
CHEMBL422567 Ki = 11.0 nM 7.96
CHEMBL2367918 Ki = 12.0 nM 7.92
CHEMBL169345 Ki = 13.0 nM 7.89
CHEMBL55851 Ki = 19.0 nM 7.72
CHEMBL354172 Ki = 20.0 nM 7.70
CHEMBL422563 Ki = 21.0 nM 7.68
CHEMBL169030 Ki = 26.0 nM 7.58
CHEMBL422560 Ki = 29.0 nM 7.54
CHEMBL168392 Ki = 29.0 nM 7.54
CHEMBL2368318 Ki = 35.0 nM 7.46
CHEMBL352965 Ki = 37.0 nM 7.43
CHEMBL169346 Ki = 51.0 nM 7.29
CHEMBL301835 Ki = 54.0 nM 7.27
CHEMBL301835 Ki = 57.0 nM 7.24
CHEMBL352827 Ki = 61.0 nM 7.21
CHEMBL440196 Ki = 75.0 nM 7.12
CHEMBL168913 Ki = 80.0 nM 7.10
CHEMBL169346 Ki = 81.0 nM 7.09
CHEMBL353303 Ki = 98.0 nM 7.01
CHEMBL353938 Ki = 100.0 nM 7.00
CHEMBL52399 Ki = 110.0 nM 6.96
CHEMBL56165 Ki = 160.0 nM 6.80
CHEMBL352365 Ki = 170.0 nM 6.77
CHEMBL169670 Ki = 180.0 nM 6.75
CHEMBL354322 Ki = 220.0 nM 6.66
CHEMBL168409 Ki = 240.0 nM 6.62
CHEMBL55392 Ki = 250.0 nM 6.60
CHEMBL170384 Ki = 250.0 nM 6.60
CHEMBL2367916 Ki = 270.0 nM 6.57
CHEMBL2368317 Ki = 370.0 nM 6.43
CHEMBL55434 Ki = 460.0 nM 6.34
CHEMBL291751 Ki = 470.0 nM 6.33
CHEMBL293951 Ki = 570.0 nM 6.24
CHEMBL299114 Ki = 810.0 nM 6.09
CHEMBL2368320 Ki = 920.0 nM 6.04
CHEMBL2021605 Ki = 1100.0 nM 5.96
CHEMBL279968 ETHYLKETOCYCLAZOCINE Ki = 1300.0 nM 5.89
CHEMBL299114 Ki = 1500.0 nM 5.82
CHEMBL55948 Ki = 1800.0 nM 5.75
CHEMBL55248 Ki = 2800.0 nM 5.55