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Assay Detail

CHEMBL997203

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

Binding
Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cannabinoid receptor 1 (CHEMBL218)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Rational design, synthesis, and pharmacological properties of new 1,8-naphthyridin-2(1H)-on-3-carboxamide derivatives as highly selective cannabinoid-2 receptor agonists.
Manera C, Saccomanni G, Adinolfi B, Benetti V, Ligresti A, Cascio MG, Tuccinardi T, Lucchesi V, Martinelli A, Nieri P, Masini E, Di Marzo V, Ferrarini PL.
J Med Chem (2009) 52 : 3644 -3651
PubMed 19435366 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 6.31 8.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL467896 1 8.02
CHEMBL467475 1 7.75
CHEMBL508336 1 7.25
CHEMBL466651 1 6.70
CHEMBL466047 1 6.70
CHEMBL512063 1 6.52
CHEMBL381689 SR-144528 1 6.36
CHEMBL466623 1 6.25
CHEMBL446993 1 6.25
CHEMBL371214 1 6.17
CHEMBL511253 1 6.02
CHEMBL466223 1 6.00
CHEMBL467681 1 5.82
CHEMBL467476 1 5.80
CHEMBL467680 1 5.28
CHEMBL513298 1 5.25
CHEMBL466429 1 5.16
CHEMBL466428 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL467896 Ki = 9.6 nM 8.02
CHEMBL467475 Ki = 18.0 nM 7.75
CHEMBL508336 Ki = 56.0 nM 7.25
CHEMBL466651 Ki = 200.0 nM 6.70
CHEMBL466047 Ki = 200.0 nM 6.70
CHEMBL512063 Ki = 300.0 nM 6.52
CHEMBL381689 SR-144528 Ki = 437.0 nM 6.36
CHEMBL466623 Ki = 560.0 nM 6.25
CHEMBL446993 Ki = 560.0 nM 6.25
CHEMBL371214 Ki = 677.0 nM 6.17
CHEMBL511253 Ki = 960.0 nM 6.02
CHEMBL466223 Ki = 1000.0 nM 6.00
CHEMBL467681 Ki = 1519.0 nM 5.82
CHEMBL467476 Ki = 1600.0 nM 5.80
CHEMBL467680 Ki = 5255.0 nM 5.28
CHEMBL513298 Ki = 5600.0 nM 5.25
CHEMBL466429 Ki = 6947.0 nM 5.16
CHEMBL466428 Ki - -