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Assay Detail

CHEMBL747228

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

Binding
Binding constant towards human Opioid receptor kappa 1 was reported
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis, biological evaluation, and receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as kappa-opioid receptor agonists endowed with antinociceptive and antiamnesic activity.
Anzini M, Canullo L, Braile C, Cappelli A, Gallelli A, Vomero S, Menziani MC, De Benedetti PG, Rizzo M, Collina S, Azzolina O, Sbacchi M, Ghelardini C, Galeotti N.
J Med Chem (2003) 46 : 3853 -3864
PubMed 12930147 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 9.12 9.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2111838 1 9.77
CHEMBL123898 1 9.60
CHEMBL341056 1 9.55
CHEMBL127463 1 9.52
CHEMBL341529 1 9.44
CHEMBL2111836 1 9.37
CHEMBL126688 1 9.35
CHEMBL338391 1 9.32
CHEMBL334156 1 9.27
CHEMBL127968 1 9.26
CHEMBL2111837 1 9.16
CHEMBL340001 1 8.88
CHEMBL126282 1 8.81
CHEMBL126596 1 8.42
CHEMBL338393 1 8.36
CHEMBL127619 1 7.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2111838 Ki = 0.1698 nM 9.77
CHEMBL123898 Ki = 0.2512 nM 9.60
CHEMBL341056 Ki = 0.2818 nM 9.55
CHEMBL127463 Ki = 0.302 nM 9.52
CHEMBL341529 Ki = 0.3631 nM 9.44
CHEMBL2111836 Ki = 0.4266 nM 9.37
CHEMBL126688 Ki = 0.4467 nM 9.35
CHEMBL338391 Ki = 0.4786 nM 9.32
CHEMBL334156 Ki = 0.537 nM 9.27
CHEMBL127968 Ki = 0.5495 nM 9.26
CHEMBL2111837 Ki = 0.6918 nM 9.16
CHEMBL340001 Ki = 1.318 nM 8.88
CHEMBL126282 Ki = 1.549 nM 8.81
CHEMBL126596 Ki = 3.802 nM 8.42
CHEMBL338393 Ki = 4.365 nM 8.36
CHEMBL127619 Ki = 13.49 nM 7.87