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Assay Detail

CHEMBL660013

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

Binding
Compound was evaluated for the inhibition of [3H]WIN-55212-2 binding in rat cerebellum membranes
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Cerebellum
Subcellular Membrane
Confidence 4 — Cell-line / Tissue
Curated By Expert

Target

Cannabinoid receptor (CHEMBL2111385)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

C-Attached aminoalkylindoles: potent cannabinoid mimetics
D'Ambra TE, Eissenstat MA, Abt J, Ackerman JH, Bacon ER, Bell MR, Carabateas PM, Josef KA, Kumar V, Weaver JD, Arnold R, Casiano FM, Chippari SM, Haycock DA, Kuster JE, Luttinger DA, Stevenson JI, Ward SJ, Hill W, Khanolkar A, Makriyannis A
Bioorg Med Chem Lett (1996) 6 : 17 -22
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.64 8.91

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL68641 1 8.91
CHEMBL302251 1 8.52
CHEMBL68642 1 8.27
CHEMBL465 DRONABINOL 4.0 1 8.24
CHEMBL68533 1 8.19
CHEMBL70952 1 8.18
CHEMBL13078 1 8.11
CHEMBL69593 1 8.01
CHEMBL302948 1 7.29
CHEMBL424042 1 6.30
CHEMBL421497 1 6.16
CHEMBL13178 PRAVADOLINE 2.0 1 5.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL68641 IC50 = 1.22 nM 8.91
CHEMBL302251 IC50 = 3.0 nM 8.52
CHEMBL68642 IC50 = 5.4 nM 8.27
CHEMBL465 DRONABINOL IC50 = 5.8 nM 8.24
CHEMBL68533 IC50 = 6.5 nM 8.19
CHEMBL70952 IC50 = 6.6 nM 8.18
CHEMBL13078 IC50 = 7.8 nM 8.11
CHEMBL69593 IC50 = 9.7 nM 8.01
CHEMBL302948 IC50 = 51.0 nM 7.29
CHEMBL424042 IC50 = 497.0 nM 6.30
CHEMBL421497 IC50 = 699.0 nM 6.16
CHEMBL13178 PRAVADOLINE IC50 = 3155.0 nM 5.50