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Assay Detail

CHEMBL755869

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

Binding
Displacement of [3H]U-69593 from Opioid receptor kappa 1 of guinea pig brain membranes
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Kappa-type opioid receptor (CHEMBL3952)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

8-Carboxamidocyclazocine analogues: redefining the structure-activity relationships of 2,6-methano-3-benzazocines.
Wentland MP, Lou R, Ye Y, Cohen DJ, Richardson GP, Bidlack JM.
Bioorg Med Chem Lett (2001) 11 : 623 -626
PubMed 11266156 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 8.24 10.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL56585 CYCLAZOCINE 2.0 1 10.28
CHEMBL3085528 1 9.74
CHEMBL2368218 1 9.55
CHEMBL58646 1 9.28
CHEMBL279968 ETHYLKETOCYCLAZOCINE 1 9.21
CHEMBL60869 1 9.15
CHEMBL160924 1 8.70
CHEMBL157301 1 8.59
CHEMBL160677 1 7.51
CHEMBL157313 1 7.17
CHEMBL154255 1 7.15
CHEMBL2021605 1 7.12
CHEMBL293103 1 6.34
CHEMBL346813 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL56585 CYCLAZOCINE Ki = 0.052 nM 10.28
CHEMBL3085528 Ki = 0.18 nM 9.74
CHEMBL2368218 Ki = 0.28 nM 9.55
CHEMBL58646 Ki = 0.53 nM 9.28
CHEMBL279968 ETHYLKETOCYCLAZOCINE Ki = 0.62 nM 9.21
CHEMBL60869 Ki = 0.7 nM 9.15
CHEMBL160924 Ki = 2.0 nM 8.70
CHEMBL157301 Ki = 2.6 nM 8.59
CHEMBL160677 Ki = 31.0 nM 7.51
CHEMBL157313 Ki = 67.0 nM 7.17
CHEMBL154255 Ki = 71.0 nM 7.15
CHEMBL2021605 Ki = 76.0 nM 7.12
CHEMBL293103 Ki = 460.0 nM 6.34
CHEMBL346813 Ki = 2500.0 nM 5.60