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Assay Detail

CHEMBL3787928

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

Binding
Displacement of [3H]U-69,593 from human kappa opioid receptor expressed in CHO cell membranes
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and evaluation of novel opioid ligands with a C-homomorphinan skeleton.
Ishikawa K, Mochizuki Y, Hirayama S, Nemoto T, Nagai K, Itoh K, Fujii H.
Bioorg Med Chem (2016) 24 : 2199 -2205
PubMed 27079125 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 8.24 9.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1797689 1 9.19
CHEMBL3786675 1 9.13
CHEMBL3785854 1 8.53
CHEMBL3787263 1 8.49
CHEMBL3787663 1 8.37
CHEMBL3787016 1 8.18
CHEMBL3786218 1 8.04
CHEMBL3785265 1 8.02
CHEMBL3786083 1 7.76
CHEMBL252172 BNTX 1 7.55
CHEMBL3786970 1 7.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1797689 Ki = 0.648 nM 9.19
CHEMBL3786675 Ki = 0.748 nM 9.13
CHEMBL3785854 Ki = 2.97 nM 8.53
CHEMBL3787263 Ki = 3.22 nM 8.49
CHEMBL3787663 Ki = 4.3 nM 8.37
CHEMBL3787016 Ki = 6.63 nM 8.18
CHEMBL3786218 Ki = 9.11 nM 8.04
CHEMBL3785265 Ki = 9.65 nM 8.02
CHEMBL3786083 Ki = 17.5 nM 7.76
CHEMBL252172 BNTX Ki = 28.3 nM 7.55
CHEMBL3786970 Ki = 39.1 nM 7.41